Cayman
Showing 38101–38250 of 45550 results
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Ro 4929097 is a potent inhibitor of γ-secretase (IC50 = 4 nM) that blocks both Aβ40 and Notch processing (IC50s = 14 and 5 nM, respectively).{32226} It displays greater than 100-fold selectivity for γ-secretase over a panel of 75 other enzymes, receptors, and ion channels. Ro 4929097 does not block tumor cell growth or induce apoptosis but instead produces a less transformed, flattened, slower-growing phenotype.{32226} It is orally active against cancer xenograft models, altering gene expression related to angiogenesis and cell differentiation.{32226} Ro 4929097 also reduces tumor initiating potential of melanoma cells in vivo by blocking Notch-dependent gene expression.{32225}
Brand:CaymanSKU:19996 -Available on backorder
Ro 5126766 is a dual inhibitor of MEK1 (IC50 = 160 nM) and Raf kinases (IC50s = 56, 19, and 8.2 nM for C-RAF, B-RAF, and B-RAFV600E, respectively).{45986} It is selective for these kinases over a panel of 254 additional kinases at 10 µM. Ro 5126766 (1 µM) decreases MEK and ERK phosphorylation in a panel of seven cancer cell lines expressing mutant K-RasG13D, K-RasQ61K, K-RasG12D, H-RasG12D, or B-RAFV600E at 1 µM. It inhibits proliferation of SK-MEL-28, SK-MEL-2, MIA PaCa-2, SW480, and HCT116 cancer cells (IC50s = 65, 28, 40, 46, and 277 nM, respectively) but not A549, HCT15, or PC3 cancer cells (IC50s = >1,000 nM for all).{45987} Oral administration of Ro 5126766 (25 mg/kg four times per day) reduces tumor growth in an HCT116 mouse xenograft model.{45986}
Brand:CaymanSKU:29197 - 1 mgAvailable on backorder
Ro 5126766 is a dual inhibitor of MEK1 (IC50 = 160 nM) and Raf kinases (IC50s = 56, 19, and 8.2 nM for C-RAF, B-RAF, and B-RAFV600E, respectively).{45986} It is selective for these kinases over a panel of 254 additional kinases at 10 µM. Ro 5126766 (1 µM) decreases MEK and ERK phosphorylation in a panel of seven cancer cell lines expressing mutant K-RasG13D, K-RasQ61K, K-RasG12D, H-RasG12D, or B-RAFV600E at 1 µM. It inhibits proliferation of SK-MEL-28, SK-MEL-2, MIA PaCa-2, SW480, and HCT116 cancer cells (IC50s = 65, 28, 40, 46, and 277 nM, respectively) but not A549, HCT15, or PC3 cancer cells (IC50s = >1,000 nM for all).{45987} Oral administration of Ro 5126766 (25 mg/kg four times per day) reduces tumor growth in an HCT116 mouse xenograft model.{45986}
Brand:CaymanSKU:29197 - 5 mgAvailable on backorder
Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2 that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50s = 447, 0.9, and 32 nM, respectively).{52211} It is selective for human 5-HT2A and 5-HT2C (Kis = 32 and 1 nM, respectively) over human 5-HT1A, 5-HT1D, 5-HT6, and 5-HT7, rat 5-HT1B and 5-HT3, and guinea pig 5-HT4 receptors (Kis = ≥1,995 nM), as well as adenosine A1 and A2, histamine H1-3, dopamine D1-5, α1-, α2-, and β1-adrenergic, M1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC50s = >1,000 nM), but does bind to β2-adrenergic receptors (IC50 = 251 nM). {52212} In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED50s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT2C antagonist SB-242084 (Item No. 10096) or the 5-HT2A antagonist MDL 100,907 (volinanserin; Item No. 15936).{52213}
Brand:CaymanSKU:29520 - 1 mgAvailable on backorder
Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2 that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50s = 447, 0.9, and 32 nM, respectively).{52211} It is selective for human 5-HT2A and 5-HT2C (Kis = 32 and 1 nM, respectively) over human 5-HT1A, 5-HT1D, 5-HT6, and 5-HT7, rat 5-HT1B and 5-HT3, and guinea pig 5-HT4 receptors (Kis = ≥1,995 nM), as well as adenosine A1 and A2, histamine H1-3, dopamine D1-5, α1-, α2-, and β1-adrenergic, M1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC50s = >1,000 nM), but does bind to β2-adrenergic receptors (IC50 = 251 nM). {52212} In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED50s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT2C antagonist SB-242084 (Item No. 10096) or the 5-HT2A antagonist MDL 100,907 (volinanserin; Item No. 15936).{52213}
Brand:CaymanSKU:29520 - 10 mgAvailable on backorder
Ro 60-0175 is an agonist of the serotonin (5-HT) receptor subtype 5-HT2 that stimulates increases in intracellular calcium levels in CHO-K1 cells expressing human 5-HT2A, 5-HT2B, and 5-HT2C receptors (EC50s = 447, 0.9, and 32 nM, respectively).{52211} It is selective for human 5-HT2A and 5-HT2C (Kis = 32 and 1 nM, respectively) over human 5-HT1A, 5-HT1D, 5-HT6, and 5-HT7, rat 5-HT1B and 5-HT3, and guinea pig 5-HT4 receptors (Kis = ≥1,995 nM), as well as adenosine A1 and A2, histamine H1-3, dopamine D1-5, α1-, α2-, and β1-adrenergic, M1-5 muscarinic, nicotinic, kainate, AMPA, and μ-, δ-, and κ-opioid receptors (IC50s = >1,000 nM), but does bind to β2-adrenergic receptors (IC50 = 251 nM). {52212} In vivo, Ro 60-0175 increases plasma levels of corticosterone, oxytocin, and prolactin in rats (ED50s = 2.43, 4.19, and 4.03 mg/kg, respectively), effects that are not inhibited by the 5-HT2C antagonist SB-242084 (Item No. 10096) or the 5-HT2A antagonist MDL 100,907 (volinanserin; Item No. 15936).{52213}
Brand:CaymanSKU:29520 - 5 mgAvailable on backorder
The kynurenine pathway mediates the metabolism of L-tryptophan to NAD+ and is particularly important in neurophysiology. Ro 61-8048 is a potent inhibitor of kynurenine 3-hydroxylase (IC50 = 37 nM), preventing the conversion of kynurenine (Item No. 11305) to 3-hydroxy kynurenine.{24463} Ro 61-8048 inhibition of kynurenine 3-hydroxylase reduces ischemia-mediated neuronal damage in tissues.{24463,24465} Ro 61-8048 can be used in vivo by direct injection.{24464}
Brand:CaymanSKU:- The kynurenine pathway mediates the metabolism of L-tryptophan to NAD+ and is particularly important in neurophysiology. Ro 61-8048 is a potent inhibitor of kynurenine 3-hydroxylase (IC50 = 37 nM), preventing the conversion of kynurenine (Item No. 11305) to 3-hydroxy kynurenine.{24463} Ro 61-8048 inhibition of kynurenine 3-hydroxylase reduces ischemia-mediated neuronal damage in tissues.{24463,24465} Ro 61-8048 can be used in vivo by direct injection.{24464}
Brand:CaymanSKU:- The kynurenine pathway mediates the metabolism of L-tryptophan to NAD+ and is particularly important in neurophysiology. Ro 61-8048 is a potent inhibitor of kynurenine 3-hydroxylase (IC50 = 37 nM), preventing the conversion of kynurenine (Item No. 11305) to 3-hydroxy kynurenine.{24463} Ro 61-8048 inhibition of kynurenine 3-hydroxylase reduces ischemia-mediated neuronal damage in tissues.{24463,24465} Ro 61-8048 can be used in vivo by direct injection.{24464}
Brand:CaymanSKU:- The kynurenine pathway mediates the metabolism of L-tryptophan to NAD+ and is particularly important in neurophysiology. Ro 61-8048 is a potent inhibitor of kynurenine 3-hydroxylase (IC50 = 37 nM), preventing the conversion of kynurenine (Item No. 11305) to 3-hydroxy kynurenine.{24463} Ro 61-8048 inhibition of kynurenine 3-hydroxylase reduces ischemia-mediated neuronal damage in tissues.{24463,24465} Ro 61-8048 can be used in vivo by direct injection.{24464}
Brand:CaymanSKU:-
Ro 67-4853 is a positive allosteric modulator of metabotropic glutamate 1 receptors (mGluR1), enhancing glutamate-induced calcium signaling through both the human and mouse mGlu1a receptors (pEC50 = 7.16).{22051,22050} While only mildly potentiating mGluR5 signaling, this compound is without effect at mGluR2, mGluR4, or mGluR8, as well as at several other neural receptors.{22051} Ro 67-4853 can also directly activate mGluR1 signaling in baby hamster kidney cells, leading to phosphorylation of ERK1/2 (EC50 = 6.2 nM) and activation of adenylate cyclase (EC50 = 11.7 μM).{22053} Ro 67-4853 can also be used to enhance neuronal stimulation in response to the mGluR1/mGluR5 agonist DHPG, both in vivo and in vitro (EC50 = 95 nM).{22051,22052}
Brand:CaymanSKU:11992 - 1 mgAvailable on backorder
Ro 67-4853 is a positive allosteric modulator of metabotropic glutamate 1 receptors (mGluR1), enhancing glutamate-induced calcium signaling through both the human and mouse mGlu1a receptors (pEC50 = 7.16).{22051,22050} While only mildly potentiating mGluR5 signaling, this compound is without effect at mGluR2, mGluR4, or mGluR8, as well as at several other neural receptors.{22051} Ro 67-4853 can also directly activate mGluR1 signaling in baby hamster kidney cells, leading to phosphorylation of ERK1/2 (EC50 = 6.2 nM) and activation of adenylate cyclase (EC50 = 11.7 μM).{22053} Ro 67-4853 can also be used to enhance neuronal stimulation in response to the mGluR1/mGluR5 agonist DHPG, both in vivo and in vitro (EC50 = 95 nM).{22051,22052}
Brand:CaymanSKU:11992 - 10 mgAvailable on backorder
Ro 67-4853 is a positive allosteric modulator of metabotropic glutamate 1 receptors (mGluR1), enhancing glutamate-induced calcium signaling through both the human and mouse mGlu1a receptors (pEC50 = 7.16).{22051,22050} While only mildly potentiating mGluR5 signaling, this compound is without effect at mGluR2, mGluR4, or mGluR8, as well as at several other neural receptors.{22051} Ro 67-4853 can also directly activate mGluR1 signaling in baby hamster kidney cells, leading to phosphorylation of ERK1/2 (EC50 = 6.2 nM) and activation of adenylate cyclase (EC50 = 11.7 μM).{22053} Ro 67-4853 can also be used to enhance neuronal stimulation in response to the mGluR1/mGluR5 agonist DHPG, both in vivo and in vitro (EC50 = 95 nM).{22051,22052}
Brand:CaymanSKU:11992 - 5 mgAvailable on backorder
Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 μM).{22051} It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 μM. Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5 in the Purkinje cells of rat cerebellar slices. It activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50 = 163.3 nM).{22053}
Brand:CaymanSKU:11993 - 1 mgAvailable on backorder
Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 μM).{22051} It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 μM. Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5 in the Purkinje cells of rat cerebellar slices. It activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50 = 163.3 nM).{22053}
Brand:CaymanSKU:11993 - 10 mgAvailable on backorder
Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 μM).{22051} It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 μM. Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5 in the Purkinje cells of rat cerebellar slices. It activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50 = 163.3 nM).{22053}
Brand:CaymanSKU:11993 - 25 mgAvailable on backorder
Ro 67-7476 is a positive allosteric modulator of metabotropic glutamate receptor 1 (mGluR1) that enhances glutamate-induced calcium release in HEK293 cells expressing rat mGluR1a (EC50 = 1.74 μM).{22051} It is selective for rat mGluR1 over rat mGluR2, mGluR4, and mGluR8 at a concentration of 10 μM. Ro 67-7476 increases the amplitude of mGluR1 excitatory postsynaptic potentials (EPSCs) evoked by 2,3-dihydroxy-6-nitro-7-sulfamoylbenzoquionxaline, picrotoxin, or AP5 in the Purkinje cells of rat cerebellar slices. It activates ERK1/2 phosphorylation in the absence of exogenously added glutamate (EC50 = 163.3 nM).{22053}
Brand:CaymanSKU:11993 - 5 mgAvailable on backorder
Ro 90-7501 is a bi-benzimidazole compound that was first found to retard the formation of mature amyloid β42 fibrils in a cell-based assay.{30566} Instead, extended polymeric sheets and fibrillary intermediates of amyloid β42 accumulated in response to Ro 90-7501 treatment, resulting in reduced cytotoxicity (EC50 = 2 µM).{30566} More recently, Ro 90-7501 was shown to modulate signaling in cells stimulated with polyinosinic-polycytidylic acid (poly(I:C); Item No. 16881), a toll-like receptor 3 (TLR3), and RIG-1-like receptor agonist.{30567} Ro 90-7501 (10 µM) enhanced poly(I:C)-induced IFN-β expression, decreased NF-κB activation, and amplified the suppression of vesicular stomatitis virus replication by poly(I:C) in HEK293 cells expressing TLR3.{30567}
Brand:CaymanSKU:-Available on backorder
Ro 90-7501 is a bi-benzimidazole compound that was first found to retard the formation of mature amyloid β42 fibrils in a cell-based assay.{30566} Instead, extended polymeric sheets and fibrillary intermediates of amyloid β42 accumulated in response to Ro 90-7501 treatment, resulting in reduced cytotoxicity (EC50 = 2 µM).{30566} More recently, Ro 90-7501 was shown to modulate signaling in cells stimulated with polyinosinic-polycytidylic acid (poly(I:C); Item No. 16881), a toll-like receptor 3 (TLR3), and RIG-1-like receptor agonist.{30567} Ro 90-7501 (10 µM) enhanced poly(I:C)-induced IFN-β expression, decreased NF-κB activation, and amplified the suppression of vesicular stomatitis virus replication by poly(I:C) in HEK293 cells expressing TLR3.{30567}
Brand:CaymanSKU:-Available on backorder
Ro 90-7501 is a bi-benzimidazole compound that was first found to retard the formation of mature amyloid β42 fibrils in a cell-based assay.{30566} Instead, extended polymeric sheets and fibrillary intermediates of amyloid β42 accumulated in response to Ro 90-7501 treatment, resulting in reduced cytotoxicity (EC50 = 2 µM).{30566} More recently, Ro 90-7501 was shown to modulate signaling in cells stimulated with polyinosinic-polycytidylic acid (poly(I:C); Item No. 16881), a toll-like receptor 3 (TLR3), and RIG-1-like receptor agonist.{30567} Ro 90-7501 (10 µM) enhanced poly(I:C)-induced IFN-β expression, decreased NF-κB activation, and amplified the suppression of vesicular stomatitis virus replication by poly(I:C) in HEK293 cells expressing TLR3.{30567}
Brand:CaymanSKU:-Available on backorder
Ro 90-7501 is a bi-benzimidazole compound that was first found to retard the formation of mature amyloid β42 fibrils in a cell-based assay.{30566} Instead, extended polymeric sheets and fibrillary intermediates of amyloid β42 accumulated in response to Ro 90-7501 treatment, resulting in reduced cytotoxicity (EC50 = 2 µM).{30566} More recently, Ro 90-7501 was shown to modulate signaling in cells stimulated with polyinosinic-polycytidylic acid (poly(I:C); Item No. 16881), a toll-like receptor 3 (TLR3), and RIG-1-like receptor agonist.{30567} Ro 90-7501 (10 µM) enhanced poly(I:C)-induced IFN-β expression, decreased NF-κB activation, and amplified the suppression of vesicular stomatitis virus replication by poly(I:C) in HEK293 cells expressing TLR3.{30567}
Brand:CaymanSKU:-Available on backorder
RO-3 is a dual antagonist of the purinergic receptor subtypes P2X3 and P2X2/3 (IC50s = 0.1 and 1.26 μM, respectively).{48818} It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 receptors (IC50s = >10 μM for all) but is an antagonist of ML1-type melatonin receptors (IC50 = 0.398 μM).
Brand:CaymanSKU:29635 - 10 mgAvailable on backorder
RO-3 is a dual antagonist of the purinergic receptor subtypes P2X3 and P2X2/3 (IC50s = 0.1 and 1.26 μM, respectively).{48818} It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 receptors (IC50s = >10 μM for all) but is an antagonist of ML1-type melatonin receptors (IC50 = 0.398 μM).
Brand:CaymanSKU:29635 - 25 mgAvailable on backorder
RO-3 is a dual antagonist of the purinergic receptor subtypes P2X3 and P2X2/3 (IC50s = 0.1 and 1.26 μM, respectively).{48818} It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 receptors (IC50s = >10 μM for all) but is an antagonist of ML1-type melatonin receptors (IC50 = 0.398 μM).
Brand:CaymanSKU:29635 - 5 mgAvailable on backorder
RO-3 is a dual antagonist of the purinergic receptor subtypes P2X3 and P2X2/3 (IC50s = 0.1 and 1.26 μM, respectively).{48818} It is selective for P2X3 and P2X2/3 over P2X1, P2X2, P2X4, P2X5, and P2X7 receptors (IC50s = >10 μM for all) but is an antagonist of ML1-type melatonin receptors (IC50 = 0.398 μM).
Brand:CaymanSKU:29635 - 50 mgAvailable on backorder
RO4987655 is a MEK inhibitor (IC50 = 5 nM).{42750} It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.
Brand:CaymanSKU:-Available on backorder
RO4987655 is a MEK inhibitor (IC50 = 5 nM).{42750} It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.
Brand:CaymanSKU:-Available on backorder
RO4987655 is a MEK inhibitor (IC50 = 5 nM).{42750} It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.
Brand:CaymanSKU:-Available on backorder
RO4987655 is a MEK inhibitor (IC50 = 5 nM).{42750} It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.
Brand:CaymanSKU:-Available on backorder
RO5028442 is a brain-penetrant antagonist of vasopressin V1a receptors (Kis = 1 and 39 nM for the human and mouse receptors, respectively).{58074} It is greater than 30,000-fold selective for V1 over V2 receptors, as well as over a panel of 120 receptors, ion channels, and enzymes at 3 µM.
Brand:CaymanSKU:31452 - 10 mgAvailable on backorder
RO5028442 is a brain-penetrant antagonist of vasopressin V1a receptors (Kis = 1 and 39 nM for the human and mouse receptors, respectively).{58074} It is greater than 30,000-fold selective for V1 over V2 receptors, as well as over a panel of 120 receptors, ion channels, and enzymes at 3 µM.
Brand:CaymanSKU:31452 - 100 mgAvailable on backorder
RO5028442 is a brain-penetrant antagonist of vasopressin V1a receptors (Kis = 1 and 39 nM for the human and mouse receptors, respectively).{58074} It is greater than 30,000-fold selective for V1 over V2 receptors, as well as over a panel of 120 receptors, ion channels, and enzymes at 3 µM.
Brand:CaymanSKU:31452 - 250 mgAvailable on backorder
RO5028442 is a brain-penetrant antagonist of vasopressin V1a receptors (Kis = 1 and 39 nM for the human and mouse receptors, respectively).{58074} It is greater than 30,000-fold selective for V1 over V2 receptors, as well as over a panel of 120 receptors, ion channels, and enzymes at 3 µM.
Brand:CaymanSKU:31452 - 50 mgAvailable on backorder
RO8191 is an agonist of interferon (IFN) α receptor type 2 (IFNAR2) with antiviral activity (EC50 = 200 nM in an anti-hepatitis C virus (HCV) replicon assay).{39290} It exhibits 1:1 binding to the IFNAR2 extracellular domain, indicating RO8191 and IFNAR2 interact at the cell surface. RO8191 induces expression of IFN-stimulated genes, without induction of genes encoding inflammatory cytokines and chemokines, in HCV replicon cells, several cancer cell lines, and human primary hepatocytes. RO8191 induces expression of IFN-stimulated genes in vivo without induction of inflammatory cytokine and chemokine expression in mice. It also reduces HCV titer in HCV-infected humanized liver mice following oral administration.
Brand:CaymanSKU:20449 -Available on backorder
RO8191 is an agonist of interferon (IFN) α receptor type 2 (IFNAR2) with antiviral activity (EC50 = 200 nM in an anti-hepatitis C virus (HCV) replicon assay).{39290} It exhibits 1:1 binding to the IFNAR2 extracellular domain, indicating RO8191 and IFNAR2 interact at the cell surface. RO8191 induces expression of IFN-stimulated genes, without induction of genes encoding inflammatory cytokines and chemokines, in HCV replicon cells, several cancer cell lines, and human primary hepatocytes. RO8191 induces expression of IFN-stimulated genes in vivo without induction of inflammatory cytokine and chemokine expression in mice. It also reduces HCV titer in HCV-infected humanized liver mice following oral administration.
Brand:CaymanSKU:20449 -Available on backorder
RO8191 is an agonist of interferon (IFN) α receptor type 2 (IFNAR2) with antiviral activity (EC50 = 200 nM in an anti-hepatitis C virus (HCV) replicon assay).{39290} It exhibits 1:1 binding to the IFNAR2 extracellular domain, indicating RO8191 and IFNAR2 interact at the cell surface. RO8191 induces expression of IFN-stimulated genes, without induction of genes encoding inflammatory cytokines and chemokines, in HCV replicon cells, several cancer cell lines, and human primary hepatocytes. RO8191 induces expression of IFN-stimulated genes in vivo without induction of inflammatory cytokine and chemokine expression in mice. It also reduces HCV titer in HCV-infected humanized liver mice following oral administration.
Brand:CaymanSKU:20449 -Available on backorder
RO8191 is an agonist of interferon (IFN) α receptor type 2 (IFNAR2) with antiviral activity (EC50 = 200 nM in an anti-hepatitis C virus (HCV) replicon assay).{39290} It exhibits 1:1 binding to the IFNAR2 extracellular domain, indicating RO8191 and IFNAR2 interact at the cell surface. RO8191 induces expression of IFN-stimulated genes, without induction of genes encoding inflammatory cytokines and chemokines, in HCV replicon cells, several cancer cell lines, and human primary hepatocytes. RO8191 induces expression of IFN-stimulated genes in vivo without induction of inflammatory cytokine and chemokine expression in mice. It also reduces HCV titer in HCV-infected humanized liver mice following oral administration.
Brand:CaymanSKU:20449 -Available on backorder
RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM).{47193} It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.
Brand:CaymanSKU:25674 - 1 mgAvailable on backorder
RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM).{47193} It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.
Brand:CaymanSKU:25674 - 10 mgAvailable on backorder
RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM).{47193} It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.
Brand:CaymanSKU:25674 - 25 mgAvailable on backorder
RO8994 is an inhibitor of the protein-protein interaction between MDM2 and the tumor suppressor p53 in a homogeneous time-resolved fluorescence (HTRF) binding assay (IC50 = 5 nM).{47193} It inhibits the proliferation of SJSA-1, RKO, and HCT116 cells with an average IC50 value of 20 nM and increases apoptosis in SJSA-1 cells in a concentration-dependent manner. RO8994 reduces tumor growth and induces tumor regression in an SJSA-1 osteosarcoma mouse xenograft model when administered at doses of 1.56 and 6.25 mg/kg, respectively.
Brand:CaymanSKU:25674 - 5 mgAvailable on backorder
Sonic hedgehog (Shh) is the most widely characterized of the three vertebrate Hedgehog homologs, and is essential for proper embryonic development.{20489} Shh binds to its receptor, Patched (Ptch1), resulting in the de-repression of Smoothened.{3776,21773} This leads to the activation of Gli2, which regulates the transcription of target genes that include Gli1 and Ptch1. Robotnikinin is the first identified small molecule inhibitor of Shh signaling that acts upstream of Smo, binding directly to Shh with a Kd value of 3.1 μM.{16805,22122} Robotnikinin represses Gli-mediated transcription in primary human keratinocytes and synthetic human skin in a concentration-dependent manner.{16805}
Brand:CaymanSKU:-
Rocaglamide is an anti-inflammatory, insecticidal, and anticancer tetrahydrobenzofuran isolated from Aglaia species. It has been shown to inhibit both TNF-α and the activation of NF-κB in Jurkat T cells with IC50 values in the nanomolar range.{23675} At 25 nM, rocaglamide induces apoptosis in various human leukemia cell lines, activating p38 MAPK/JNK and suppressing ERK.{23676} Rocaglamide also reduces IFN-γ, TNF-α, IL-2, and IL-4 production in peripheral blood T cells at a concentration of 50 nM.{23677} Furthermore, rocaglamide can inhibit the T cell expression of the immune response transcription factor, nuclear factor of activated T cells.{23677}
Brand:CaymanSKU:- Rocaglamide is an anti-inflammatory, insecticidal, and anticancer tetrahydrobenzofuran isolated from Aglaia species. It has been shown to inhibit both TNF-α and the activation of NF-κB in Jurkat T cells with IC50 values in the nanomolar range.{23675} At 25 nM, rocaglamide induces apoptosis in various human leukemia cell lines, activating p38 MAPK/JNK and suppressing ERK.{23676} Rocaglamide also reduces IFN-γ, TNF-α, IL-2, and IL-4 production in peripheral blood T cells at a concentration of 50 nM.{23677} Furthermore, rocaglamide can inhibit the T cell expression of the immune response transcription factor, nuclear factor of activated T cells.{23677}
Brand:CaymanSKU:-
Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.{53422,53423} It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 µg/ml for both).{53422} Roccellic acid (100 µg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.{53423}
Brand:CaymanSKU:29909 - 1 mgAvailable on backorder
Roccellic acid is a lichen secondary metabolite that has been found in R. montagnei and has antibacterial and anticancer activities.{53422,53423} It is active against the bacteria S. gordonii and P. gingivalis (MIC = 46.9 µg/ml for both).{53422} Roccellic acid (100 µg/ml) inhibits proliferation of MDA-MB-231, MCF-7, and DLD-1 cancer cells by 65.3, 75.8, and 87.9%, respectively.{53423}
Brand:CaymanSKU:29909 - 5 mgAvailable on backorder
Rocuronium is a non-depolarizing muscle relaxant.{37222} It selectively induces neuromuscular blockade in cats (ED50s = 153, 185, 1,329, and 4,119 μg/kg for tibialis, soleus, and vagus muscles, and nictitating membranes, respectively) with a more rapid onset time than vecuronium (Item No. 15603). Formulations containing rocuronium have been used for surgical anesthesia.{37223}
Brand:CaymanSKU:23698 - 10 mgAvailable on backorder
Rocuronium is a non-depolarizing muscle relaxant.{37222} It selectively induces neuromuscular blockade in cats (ED50s = 153, 185, 1,329, and 4,119 μg/kg for tibialis, soleus, and vagus muscles, and nictitating membranes, respectively) with a more rapid onset time than vecuronium (Item No. 15603). Formulations containing rocuronium have been used for surgical anesthesia.{37223}
Brand:CaymanSKU:23698 - 25 mgAvailable on backorder
Rocuronium is a non-depolarizing muscle relaxant.{37222} It selectively induces neuromuscular blockade in cats (ED50s = 153, 185, 1,329, and 4,119 μg/kg for tibialis, soleus, and vagus muscles, and nictitating membranes, respectively) with a more rapid onset time than vecuronium (Item No. 15603). Formulations containing rocuronium have been used for surgical anesthesia.{37223}
Brand:CaymanSKU:23698 - 5 mgAvailable on backorder
Rocuronium is a non-depolarizing muscle relaxant.{37222} It selectively induces neuromuscular blockade in cats (ED50s = 153, 185, 1,329, and 4,119 μg/kg for tibialis, soleus, and vagus muscles, and nictitating membranes, respectively) with a more rapid onset time than vecuronium (Item No. 15603). Formulations containing rocuronium have been used for surgical anesthesia.{37223}
Brand:CaymanSKU:23698 - 50 mgAvailable on backorder
Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2; Item No. 14010) in CHO cells expressing the recombinant human enzymes.{12018} In vivo, rofecoxib inhibits carrageenan-induced paw edema and hyperalgesia (ID50s = 1.5 and 1.0 mg/kg, respectively), LPS-induced pyresis (ID50 = 0.24 mg/kg), and M. butyricum-induced arthritis (ID50 = 0.74 mg/kg/day per day) in rats. Formulations containing rofecoxib were previously used in the treatment of pain and arthritis.
Brand:CaymanSKU:10010260 - 100 mgAvailable on backorder
Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2; Item No. 14010) in CHO cells expressing the recombinant human enzymes.{12018} In vivo, rofecoxib inhibits carrageenan-induced paw edema and hyperalgesia (ID50s = 1.5 and 1.0 mg/kg, respectively), LPS-induced pyresis (ID50 = 0.24 mg/kg), and M. butyricum-induced arthritis (ID50 = 0.74 mg/kg/day per day) in rats. Formulations containing rofecoxib were previously used in the treatment of pain and arthritis.
Brand:CaymanSKU:10010260 - 250 mgAvailable on backorder
Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2; Item No. 14010) in CHO cells expressing the recombinant human enzymes.{12018} In vivo, rofecoxib inhibits carrageenan-induced paw edema and hyperalgesia (ID50s = 1.5 and 1.0 mg/kg, respectively), LPS-induced pyresis (ID50 = 0.24 mg/kg), and M. butyricum-induced arthritis (ID50 = 0.74 mg/kg/day per day) in rats. Formulations containing rofecoxib were previously used in the treatment of pain and arthritis.
Brand:CaymanSKU:10010260 - 50 mgAvailable on backorder
Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2; Item No. 14010) in CHO cells expressing the recombinant human enzymes.{12018} In vivo, rofecoxib inhibits carrageenan-induced paw edema and hyperalgesia (ID50s = 1.5 and 1.0 mg/kg, respectively), LPS-induced pyresis (ID50 = 0.24 mg/kg), and M. butyricum-induced arthritis (ID50 = 0.74 mg/kg/day per day) in rats. Formulations containing rofecoxib were previously used in the treatment of pain and arthritis.
Brand:CaymanSKU:10010260 - 500 mgAvailable on backorder
Rofecoxib-d5 is intended for use as an internal standard for the quantification of rofecoxib (Item No. 10010260) by GC- or LC-MS. Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2; Item No. 14010) in CHO cells expressing the recombinant human enzymes.{12018} In vivo, rofecoxib inhibits carrageenan-induced paw edema and hyperalgesia (ID50s = 1.5 and 1.0 mg/kg, respectively), LPS-induced pyresis (ID50 = 0.24 mg/kg), and M. butyricum-induced arthritis (ID50 = 0.74 mg/kg per day) in rats. Formulations containing rofecoxib were previously used in the treatment of pain and arthritis.
Brand:CaymanSKU:28900 - 1 mgAvailable on backorder
Rofecoxib-d5 is intended for use as an internal standard for the quantification of rofecoxib (Item No. 10010260) by GC- or LC-MS. Rofecoxib is a non-steroidal anti-inflammatory drug (NSAID) that selectively inhibits COX-2 over COX-1 with IC50 values of 0.018 and >15 µM, respectively, for production of prostaglandin E2 (PGE2; Item No. 14010) in CHO cells expressing the recombinant human enzymes.{12018} In vivo, rofecoxib inhibits carrageenan-induced paw edema and hyperalgesia (ID50s = 1.5 and 1.0 mg/kg, respectively), LPS-induced pyresis (ID50 = 0.24 mg/kg), and M. butyricum-induced arthritis (ID50 = 0.74 mg/kg per day) in rats. Formulations containing rofecoxib were previously used in the treatment of pain and arthritis.
Brand:CaymanSKU:28900 - 500 µgAvailable on backorder
Type 4 cyclic nucleotide phosphodiesterase (PDE4) isoforms selectively inactivate the second messenger cAMP by hydrolyzing the phosphodiester bond, producing AMP.{22523} Roflumilast is a potent, cell-permeable inhibitor of PDE4 (IC50 = 50 values against other PDE forms being greater than 10 μM.{24530} Roflumilast demonstrates good bioavailability and has applications in respiratory diseases, including asthma and chronic obstructive pulmonary disease.{18127,23597}
Brand:CaymanSKU:- Type 4 cyclic nucleotide phosphodiesterase (PDE4) isoforms selectively inactivate the second messenger cAMP by hydrolyzing the phosphodiester bond, producing AMP.{22523} Roflumilast is a potent, cell-permeable inhibitor of PDE4 (IC50 = 50 values against other PDE forms being greater than 10 μM.{24530} Roflumilast demonstrates good bioavailability and has applications in respiratory diseases, including asthma and chronic obstructive pulmonary disease.{18127,23597}
Brand:CaymanSKU:- Type 4 cyclic nucleotide phosphodiesterase (PDE4) isoforms selectively inactivate the second messenger cAMP by hydrolyzing the phosphodiester bond, producing AMP.{22523} Roflumilast is a potent, cell-permeable inhibitor of PDE4 (IC50 = 50 values against other PDE forms being greater than 10 μM.{24530} Roflumilast demonstrates good bioavailability and has applications in respiratory diseases, including asthma and chronic obstructive pulmonary disease.{18127,23597}
Brand:CaymanSKU:- Type 4 cyclic nucleotide phosphodiesterase (PDE4) isoforms selectively inactivate the second messenger cAMP by hydrolyzing the phosphodiester bond, producing AMP.{22523} Roflumilast is a potent, cell-permeable inhibitor of PDE4 (IC50 = 50 values against other PDE forms being greater than 10 μM.{24530} Roflumilast demonstrates good bioavailability and has applications in respiratory diseases, including asthma and chronic obstructive pulmonary disease.{18127,23597}
Brand:CaymanSKU:-
Roflumilast-d4 is intended for use as an internal standard for the quantification of roflumilast (Item No. 15141) by GC- or LC-MS. Roflumilast is a potent, cell-permeable inhibitor of PDE4 (IC50 = 50 values against other PDE forms being greater than 10 μM.
Brand:CaymanSKU:-Available on backorder
Roflumilast-d4 is intended for use as an internal standard for the quantification of roflumilast (Item No. 15141) by GC- or LC-MS. Roflumilast is a potent, cell-permeable inhibitor of PDE4 (IC50 = 50 values against other PDE forms being greater than 10 μM.
Brand:CaymanSKU:-Available on backorder
Rolapitant is a potent neurokinin-1 (NK1) receptor antagonist (Ki = 0.66 nM for the human receptor).{35201} It is greater than 1,000-fold selective for NK1 over NK2 and NK3 and lacks activity in a panel of 100 receptors, transporters, enzymes, and ion channels. Rolapitant inhibits GR-73632-induced calcium efflux in CHO cells expressing human NK1 in a concentration-dependent manner. In vivo, rolapitant inhibits GR-73632-induced foot-tapping in gerbils (ID90 = 0.3 mg/kg). It also prevents emesis in ferrets induced by apomorphine (Item No. 16094) and cisplatin (Item No. 13119) with ED50 values of 0.03 and 0.07 mg/kg, respectively. Formulations containing rolapitant have been used to prevent chemotherapy-induced nausea and vomiting.
Brand:CaymanSKU:23906 - 1 mgAvailable on backorder
Rolapitant is a potent neurokinin-1 (NK1) receptor antagonist (Ki = 0.66 nM for the human receptor).{35201} It is greater than 1,000-fold selective for NK1 over NK2 and NK3 and lacks activity in a panel of 100 receptors, transporters, enzymes, and ion channels. Rolapitant inhibits GR-73632-induced calcium efflux in CHO cells expressing human NK1 in a concentration-dependent manner. In vivo, rolapitant inhibits GR-73632-induced foot-tapping in gerbils (ID90 = 0.3 mg/kg). It also prevents emesis in ferrets induced by apomorphine (Item No. 16094) and cisplatin (Item No. 13119) with ED50 values of 0.03 and 0.07 mg/kg, respectively. Formulations containing rolapitant have been used to prevent chemotherapy-induced nausea and vomiting.
Brand:CaymanSKU:23906 - 10 mgAvailable on backorder
Rolapitant is a potent neurokinin-1 (NK1) receptor antagonist (Ki = 0.66 nM for the human receptor).{35201} It is greater than 1,000-fold selective for NK1 over NK2 and NK3 and lacks activity in a panel of 100 receptors, transporters, enzymes, and ion channels. Rolapitant inhibits GR-73632-induced calcium efflux in CHO cells expressing human NK1 in a concentration-dependent manner. In vivo, rolapitant inhibits GR-73632-induced foot-tapping in gerbils (ID90 = 0.3 mg/kg). It also prevents emesis in ferrets induced by apomorphine (Item No. 16094) and cisplatin (Item No. 13119) with ED50 values of 0.03 and 0.07 mg/kg, respectively. Formulations containing rolapitant have been used to prevent chemotherapy-induced nausea and vomiting.
Brand:CaymanSKU:23906 - 5 mgAvailable on backorder
Rolitetracycline is a tetracycline antibiotic with bacteriostatic activity at low concentrations (7.8 μg/ml) and bactericidal activity at high concentrations (15.6 μg/ml) against E. coli.{40388} It has additive and synergistic effects with penicillin and cephalothin, respectively, in vitro against 34 E. coli and S. aureus strains. Rolitetracycline is also active against P. falciparum strains (IC50s = 45-208 μM) that are susceptible and resistant to chloroquine (Item No. 14194).{40389} It also reduces amyloid-β (1-40) (Aβ40) fibrilization (IC50 = 59 μM in an immune assay) and completely inhibits Aβ40-induced cellular toxicity at a concentration of 20 μM.{40390}
Brand:CaymanSKU:23479 - 25 mgAvailable on backorder
Rolitetracycline is a tetracycline antibiotic with bacteriostatic activity at low concentrations (7.8 μg/ml) and bactericidal activity at high concentrations (15.6 μg/ml) against E. coli.{40388} It has additive and synergistic effects with penicillin and cephalothin, respectively, in vitro against 34 E. coli and S. aureus strains. Rolitetracycline is also active against P. falciparum strains (IC50s = 45-208 μM) that are susceptible and resistant to chloroquine (Item No. 14194).{40389} It also reduces amyloid-β (1-40) (Aβ40) fibrilization (IC50 = 59 μM in an immune assay) and completely inhibits Aβ40-induced cellular toxicity at a concentration of 20 μM.{40390}
Brand:CaymanSKU:23479 - 5 mgAvailable on backorder
Romidepsin, also known as FK228, is a natural bicyclic depsipeptide that, following reduction, selectively inhibits class I histone deacetylases (HDACs).{10790} Reduction of a disulfide bond on romidepsin within the cell generates a zinc-binding thiol, allowing potent and selective inhibition of HDAC1, 2, 3, and 8 (IC50s = 53, 39, 53, and 26 nM, respectively) over HDAC4, 6, 7, and 9 (IC50s = 470, 330, 3,200, and 12,000 nM, respectively).{28023,15938} Through its effects on HDACs, romidepsin has anti-cancer activities, particularly against certain T cell lymphomas.{28022,28021,28020} Romidepsin also increases mRNA expression and nuclear protein levels of HDAC2, H3 acetylation and transcription of Grin2a, the gene for the NMDA receptor NR2A subunit, and protein levels of the NR2A subunit in the brain of Shank3-deficient mice, a model of autism.{40872} It also increases excitatory postsynaptic currents (EPSCs) in prefrontal cortex pyramidal neurons from Shank3-deficient mice. In addition, romidepsin rescues autism-like social deficits in Shank3-deficient mice for at least three weeks following administration of a 0.25 mg/kg per day dose for three days.
Brand:CaymanSKU:-Out of stock
Romidepsin, also known as FK228, is a natural bicyclic depsipeptide that, following reduction, selectively inhibits class I histone deacetylases (HDACs).{10790} Reduction of a disulfide bond on romidepsin within the cell generates a zinc-binding thiol, allowing potent and selective inhibition of HDAC1, 2, 3, and 8 (IC50s = 53, 39, 53, and 26 nM, respectively) over HDAC4, 6, 7, and 9 (IC50s = 470, 330, 3,200, and 12,000 nM, respectively).{28023,15938} Through its effects on HDACs, romidepsin has anti-cancer activities, particularly against certain T cell lymphomas.{28022,28021,28020} Romidepsin also increases mRNA expression and nuclear protein levels of HDAC2, H3 acetylation and transcription of Grin2a, the gene for the NMDA receptor NR2A subunit, and protein levels of the NR2A subunit in the brain of Shank3-deficient mice, a model of autism.{40872} It also increases excitatory postsynaptic currents (EPSCs) in prefrontal cortex pyramidal neurons from Shank3-deficient mice. In addition, romidepsin rescues autism-like social deficits in Shank3-deficient mice for at least three weeks following administration of a 0.25 mg/kg per day dose for three days.
Brand:CaymanSKU:-Out of stock
Romidepsin, also known as FK228, is a natural bicyclic depsipeptide that, following reduction, selectively inhibits class I histone deacetylases (HDACs).{10790} Reduction of a disulfide bond on romidepsin within the cell generates a zinc-binding thiol, allowing potent and selective inhibition of HDAC1, 2, 3, and 8 (IC50s = 53, 39, 53, and 26 nM, respectively) over HDAC4, 6, 7, and 9 (IC50s = 470, 330, 3,200, and 12,000 nM, respectively).{28023,15938} Through its effects on HDACs, romidepsin has anti-cancer activities, particularly against certain T cell lymphomas.{28022,28021,28020} Romidepsin also increases mRNA expression and nuclear protein levels of HDAC2, H3 acetylation and transcription of Grin2a, the gene for the NMDA receptor NR2A subunit, and protein levels of the NR2A subunit in the brain of Shank3-deficient mice, a model of autism.{40872} It also increases excitatory postsynaptic currents (EPSCs) in prefrontal cortex pyramidal neurons from Shank3-deficient mice. In addition, romidepsin rescues autism-like social deficits in Shank3-deficient mice for at least three weeks following administration of a 0.25 mg/kg per day dose for three days.
Brand:CaymanSKU:-Out of stock
Ropinirole is a potent dopamine D2 receptor agonist (Ki = 29 nM in a radioligand binding assay).{38497} It is selective for D2 over D1 dopamine receptors (Ki = >100,000 nM) as well as a panel of adrenergic, serotonin, benzodiazepine, and GABA receptors (IC50s = >9,000 nM). Ropinirole reduces spontaneous locomotor activity in mice at doses less than 50 mg/kg but increases it at a dose of 100 mg/kg. It also induces contralateral asymmetry in an open field test in 6-OHDA-lesioned mice. Ropinirole (0.01-1 mg/kg) reverses locomotor deficits and restores interest in novel stimuli in a marmoset model of Parkinson’s disease induced by MPTP. Formulations containing ropinirole have been used for the treatment of Parkinson’s disease motor dysfunction.
Brand:CaymanSKU:23871 - 10 mgAvailable on backorder
Ropinirole is a potent dopamine D2 receptor agonist (Ki = 29 nM in a radioligand binding assay).{38497} It is selective for D2 over D1 dopamine receptors (Ki = >100,000 nM) as well as a panel of adrenergic, serotonin, benzodiazepine, and GABA receptors (IC50s = >9,000 nM). Ropinirole reduces spontaneous locomotor activity in mice at doses less than 50 mg/kg but increases it at a dose of 100 mg/kg. It also induces contralateral asymmetry in an open field test in 6-OHDA-lesioned mice. Ropinirole (0.01-1 mg/kg) reverses locomotor deficits and restores interest in novel stimuli in a marmoset model of Parkinson’s disease induced by MPTP. Formulations containing ropinirole have been used for the treatment of Parkinson’s disease motor dysfunction.
Brand:CaymanSKU:23871 - 25 mgAvailable on backorder
Ropinirole is a potent dopamine D2 receptor agonist (Ki = 29 nM in a radioligand binding assay).{38497} It is selective for D2 over D1 dopamine receptors (Ki = >100,000 nM) as well as a panel of adrenergic, serotonin, benzodiazepine, and GABA receptors (IC50s = >9,000 nM). Ropinirole reduces spontaneous locomotor activity in mice at doses less than 50 mg/kg but increases it at a dose of 100 mg/kg. It also induces contralateral asymmetry in an open field test in 6-OHDA-lesioned mice. Ropinirole (0.01-1 mg/kg) reverses locomotor deficits and restores interest in novel stimuli in a marmoset model of Parkinson’s disease induced by MPTP. Formulations containing ropinirole have been used for the treatment of Parkinson’s disease motor dysfunction.
Brand:CaymanSKU:23871 - 50 mgAvailable on backorder
Ropinirole-d7 is intended for use as an internal standard for the quantification of ropinirole (Item No. 23871) by GC- or LC-MS. Ropinirole is a dopamine D2 receptor agonist that induces [35S]GTPγS binding in CHO cells expressing the human receptor (EC50 = 304 nM).{58103} It is selective for dopamine D2 over D1 receptors (Kis = 29 and >100,000 nM, respectively), as well as a panel of adrenergic, serotonin (5-HT), benzodiazepine, and GABA receptors (IC50s = >9,000 nM for all).{38497} Ropinirole reduces spontaneous locomotor activity in mice at doses less than 50 mg/kg but increases it at a dose of 100 mg/kg. It also induces contralateral asymmetry in 6-OHDA-lesioned mice. Ropinirole (0.01-1 mg/kg) reverses locomotor deficits and restores interest in novel stimuli in a marmoset model of Parkinson’s disease induced by MPTP. Formulations containing ropinirole have been used in the treatment of Parkinson’s disease motor dysfunction.
Brand:CaymanSKU:31689 - 1 mgAvailable on backorder
Ropinirole-d7 is intended for use as an internal standard for the quantification of ropinirole (Item No. 23871) by GC- or LC-MS. Ropinirole is a dopamine D2 receptor agonist that induces [35S]GTPγS binding in CHO cells expressing the human receptor (EC50 = 304 nM).{58103} It is selective for dopamine D2 over D1 receptors (Kis = 29 and >100,000 nM, respectively), as well as a panel of adrenergic, serotonin (5-HT), benzodiazepine, and GABA receptors (IC50s = >9,000 nM for all).{38497} Ropinirole reduces spontaneous locomotor activity in mice at doses less than 50 mg/kg but increases it at a dose of 100 mg/kg. It also induces contralateral asymmetry in 6-OHDA-lesioned mice. Ropinirole (0.01-1 mg/kg) reverses locomotor deficits and restores interest in novel stimuli in a marmoset model of Parkinson’s disease induced by MPTP. Formulations containing ropinirole have been used in the treatment of Parkinson’s disease motor dysfunction.
Brand:CaymanSKU:31689 - 500 µgAvailable on backorder
Roquefortine C is a mycotoxin that was first isolated from a strain of P. roqueforti, a species of Penicillium commercially used to ripen blue-veined cheeses.{24904} It has also been isolated from other members of the Penicillium genus found in contaminated food products where it displays neurotoxic properties.{24905} It has been shown to both activate a P-glycoprotein transport system involved in the efflux of xenobiotics and to inhibit cytochrome P450 3A detoxification enzymes.{24907} It has also been used as a biomarker for penitrem A (Item No. 11347) intoxication.{24906}
Brand:CaymanSKU:- Roquefortine C is a mycotoxin that was first isolated from a strain of P. roqueforti, a species of Penicillium commercially used to ripen blue-veined cheeses.{24904} It has also been isolated from other members of the Penicillium genus found in contaminated food products where it displays neurotoxic properties.{24905} It has been shown to both activate a P-glycoprotein transport system involved in the efflux of xenobiotics and to inhibit cytochrome P450 3A detoxification enzymes.{24907} It has also been used as a biomarker for penitrem A (Item No. 11347) intoxication.{24906}
Brand:CaymanSKU:-
Roquefortine E is a diketopiperazine fungal metabolite produced by G. reessii.{36338} It has been found as a contaminant in dried milled silage animal feed.{36339}
Brand:CaymanSKU:23648 - 1 mgAvailable on backorder
Roquefortine E is a diketopiperazine fungal metabolite produced by G. reessii.{36338} It has been found as a contaminant in dried milled silage animal feed.{36339}
Brand:CaymanSKU:23648 - 5 mgAvailable on backorder
Roquinimex is an immunomodulator with diverse biological activities.{46847,46848,46849,46850} In vivo, roquinimex (80 mg/kg) increases the number of myocardial MHC class II-expressing cells, the ratio of cytotoxic to helper T cells, and survival and decreases necrotic lesion area in a mouse model of murine coxsackievirus B3-induced myocarditis.{46847} It induces IFN-γ production, reduces TNF-α and IL-1β production, prevents the development of proteinuria, and ameliorates nephritis in a mouse model of chronic graft versus host disease (GVHD).{46848} Roquinimex (300 mg/kg) decreases colonic myeloperoxidase (MPO) activity and mucosal damage in a mouse model of colitis induced by dextran sulfate (DSS; Item No. 23250).{46849} It also decreases tumor weight and tumor blood flow in a von Hippel-Lindau (VHL) type 2a paraganglioma mouse xenograft model.{46850}
Brand:CaymanSKU:30206 - 10 mgAvailable on backorder
Roquinimex is an immunomodulator with diverse biological activities.{46847,46848,46849,46850} In vivo, roquinimex (80 mg/kg) increases the number of myocardial MHC class II-expressing cells, the ratio of cytotoxic to helper T cells, and survival and decreases necrotic lesion area in a mouse model of murine coxsackievirus B3-induced myocarditis.{46847} It induces IFN-γ production, reduces TNF-α and IL-1β production, prevents the development of proteinuria, and ameliorates nephritis in a mouse model of chronic graft versus host disease (GVHD).{46848} Roquinimex (300 mg/kg) decreases colonic myeloperoxidase (MPO) activity and mucosal damage in a mouse model of colitis induced by dextran sulfate (DSS; Item No. 23250).{46849} It also decreases tumor weight and tumor blood flow in a von Hippel-Lindau (VHL) type 2a paraganglioma mouse xenograft model.{46850}
Brand:CaymanSKU:30206 - 100 mgAvailable on backorder