Chemicals
Showing 13501–13650 of 41137 results
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N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM).{18096} It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors.{18096} CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.{18096}
Brand:CaymanSKU:- N-Methyl-D-aspartate (NMDA) receptors are Ca2+ permeable ligand-gated channels of the central nervous system that are activated after binding of the co-agonists glutamate and glycine. CAY10608 is a propanolamine that potently, selectively, and non-competitively antagonizes the NR2B subunit of NMDA receptors (IC50 = 50 nM).{18096} It does not inhibit NR1, NR2A, NR2C, and NR2D subunits and has no significant effects on α-amino-3-hydroxy-5-methyl-4-isoxazolepropioinic acid (AMPA) or kainate receptors.{18096} CAY10608 is neuroprotective, since it prevents NMDA-triggered release of lactate dehydrogenase from cultured cortical neurons. Also, CAY10608, when administered intraperitoneally, reduces brain infarct volume resulting from transient ischemia via carotid artery occlusion.{18096}
Brand:CaymanSKU:-
Lipid A is a lipid-rich component of endotoxin, also known as lipopolysaccharide (LPS), which in turn is part of the outer membrane of Gram-negative bacteria. Lipid A activates toll-like receptor 4 (TLR4), initiating an immune response. CAY10614 is an antagonist of lipid A activation of TLR4, exhibiting an IC50 value of 1.68 μM in a cell-based assay using modified human embryonic kidney (HEK) cells.{17575} It does not significantly affect HEK cell viability. In a model of sepsis, CAY10614 dramatically and significantly improves survival of mice given intraperitoneal LPS.{17575}
Brand:CaymanSKU:- Lipid A is a lipid-rich component of endotoxin, also known as lipopolysaccharide (LPS), which in turn is part of the outer membrane of Gram-negative bacteria. Lipid A activates toll-like receptor 4 (TLR4), initiating an immune response. CAY10614 is an antagonist of lipid A activation of TLR4, exhibiting an IC50 value of 1.68 μM in a cell-based assay using modified human embryonic kidney (HEK) cells.{17575} It does not significantly affect HEK cell viability. In a model of sepsis, CAY10614 dramatically and significantly improves survival of mice given intraperitoneal LPS.{17575}
Brand:CaymanSKU:- Lipid A is a lipid-rich component of endotoxin, also known as lipopolysaccharide (LPS), which in turn is part of the outer membrane of Gram-negative bacteria. Lipid A activates toll-like receptor 4 (TLR4), initiating an immune response. CAY10614 is an antagonist of lipid A activation of TLR4, exhibiting an IC50 value of 1.68 μM in a cell-based assay using modified human embryonic kidney (HEK) cells.{17575} It does not significantly affect HEK cell viability. In a model of sepsis, CAY10614 dramatically and significantly improves survival of mice given intraperitoneal LPS.{17575}
Brand:CaymanSKU:- Lipid A is a lipid-rich component of endotoxin, also known as lipopolysaccharide (LPS), which in turn is part of the outer membrane of Gram-negative bacteria. Lipid A activates toll-like receptor 4 (TLR4), initiating an immune response. CAY10614 is an antagonist of lipid A activation of TLR4, exhibiting an IC50 value of 1.68 μM in a cell-based assay using modified human embryonic kidney (HEK) cells.{17575} It does not significantly affect HEK cell viability. In a model of sepsis, CAY10614 dramatically and significantly improves survival of mice given intraperitoneal LPS.{17575}
Brand:CaymanSKU:-
Resveratrol is a natural polyphenolic antioxidant that has anti-cancer properties. CAY10616 is an analog of resveratrol which potently induces apoptosis in promyelocytic leukemia HL-60 cells (IC50 = 40 nM, vs. 50 μM for resveratrol).{17129} In addition, CAY10599 induces apoptosis (IC50 = 30 nM) in HL-60R, a cell line derived from HL-60 that expresses a multidrug-resistance phenotype (resistant to daunorubicin, etoposide, and citarabine).{17129}
Brand:CaymanSKU:- Resveratrol is a natural polyphenolic antioxidant that has anti-cancer properties. CAY10616 is an analog of resveratrol which potently induces apoptosis in promyelocytic leukemia HL-60 cells (IC50 = 40 nM, vs. 50 μM for resveratrol).{17129} In addition, CAY10599 induces apoptosis (IC50 = 30 nM) in HL-60R, a cell line derived from HL-60 that expresses a multidrug-resistance phenotype (resistant to daunorubicin, etoposide, and citarabine).{17129}
Brand:CaymanSKU:- Resveratrol is a natural polyphenolic antioxidant that has anti-cancer properties. CAY10616 is an analog of resveratrol which potently induces apoptosis in promyelocytic leukemia HL-60 cells (IC50 = 40 nM, vs. 50 μM for resveratrol).{17129} In addition, CAY10599 induces apoptosis (IC50 = 30 nM) in HL-60R, a cell line derived from HL-60 that expresses a multidrug-resistance phenotype (resistant to daunorubicin, etoposide, and citarabine).{17129}
Brand:CaymanSKU:- Resveratrol is a natural polyphenolic antioxidant that has anti-cancer properties. CAY10616 is an analog of resveratrol which potently induces apoptosis in promyelocytic leukemia HL-60 cells (IC50 = 40 nM, vs. 50 μM for resveratrol).{17129} In addition, CAY10599 induces apoptosis (IC50 = 30 nM) in HL-60R, a cell line derived from HL-60 that expresses a multidrug-resistance phenotype (resistant to daunorubicin, etoposide, and citarabine).{17129}
Brand:CaymanSKU:-
CAY10621 is an inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 3.3 μM).{17183} It is selective for SPHK1 over SPHK2 at 10 μM and PKC at concentrations less than 100 μM. CAY10621 inhibits SPHK1 activity by 70% in U937 cells when used at a concentration of 5 μM.
Brand:CaymanSKU:- CAY10621 is an inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 3.3 μM).{17183} It is selective for SPHK1 over SPHK2 at 10 μM and PKC at concentrations less than 100 μM. CAY10621 inhibits SPHK1 activity by 70% in U937 cells when used at a concentration of 5 μM.
Brand:CaymanSKU:- CAY10621 is an inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 3.3 μM).{17183} It is selective for SPHK1 over SPHK2 at 10 μM and PKC at concentrations less than 100 μM. CAY10621 inhibits SPHK1 activity by 70% in U937 cells when used at a concentration of 5 μM.
Brand:CaymanSKU:- CAY10621 is an inhibitor of sphingosine kinase 1 (SPHK1; IC50 = 3.3 μM).{17183} It is selective for SPHK1 over SPHK2 at 10 μM and PKC at concentrations less than 100 μM. CAY10621 inhibits SPHK1 activity by 70% in U937 cells when used at a concentration of 5 μM.
Brand:CaymanSKU:-
Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal.{17734,17735,17322} CAY10622 is a potent, ureidobenzamide inhibitor of ROCK-I and ROCK-II kinases with IC50 values of 6 and 4 nM, respectively.{17910} It is inactive (showing greater then 100-fold selectivity) against an additional 44 kinases.{17910}
Brand:CaymanSKU:- Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal.{17734,17735,17322} CAY10622 is a potent, ureidobenzamide inhibitor of ROCK-I and ROCK-II kinases with IC50 values of 6 and 4 nM, respectively.{17910} It is inactive (showing greater then 100-fold selectivity) against an additional 44 kinases.{17910}
Brand:CaymanSKU:- Two Rho-associated kinases (ROCK), ROCK-I and ROCK-II, act downstream of the G protein Rho to regulate cytoskeletal stability. The ROCKs play important roles in diverse cellular functions including cell adhesion and proliferation, smooth muscle contraction, and stem cell renewal.{17734,17735,17322} CAY10622 is a potent, ureidobenzamide inhibitor of ROCK-I and ROCK-II kinases with IC50 values of 6 and 4 nM, respectively.{17910} It is inactive (showing greater then 100-fold selectivity) against an additional 44 kinases.{17910}
Brand:CaymanSKU:-
Survivin is a cellular protein implicated in cell survival by interacting with and inhibiting the apoptotic function of several proteins including Smac/DIABLO, caspase-3, and caspase-7.{18220,12862} Survivin also plays a role in the regulation of the cell cycle as part of a protein complex that includes INCENP, Aurora B kinase, and Borealin. CAY10625 is an antagonist of the interaction between survivin and the apoptosis-promoting protein Smac/DIABLO, exhibiting an IC50 value of 2.2 µM.{18017} It inhibits the interaction of survivin with INCENP less effectively with an IC50 value of 20 µM. CAY10625 is cell-permeable and sensitizes cells to the induction of apoptosis by doxorubicin.{18017}
Brand:CaymanSKU:- Survivin is a cellular protein implicated in cell survival by interacting with and inhibiting the apoptotic function of several proteins including Smac/DIABLO, caspase-3, and caspase-7.{18220,12862} Survivin also plays a role in the regulation of the cell cycle as part of a protein complex that includes INCENP, Aurora B kinase, and Borealin. CAY10625 is an antagonist of the interaction between survivin and the apoptosis-promoting protein Smac/DIABLO, exhibiting an IC50 value of 2.2 µM.{18017} It inhibits the interaction of survivin with INCENP less effectively with an IC50 value of 20 µM. CAY10625 is cell-permeable and sensitizes cells to the induction of apoptosis by doxorubicin.{18017}
Brand:CaymanSKU:- Survivin is a cellular protein implicated in cell survival by interacting with and inhibiting the apoptotic function of several proteins including Smac/DIABLO, caspase-3, and caspase-7.{18220,12862} Survivin also plays a role in the regulation of the cell cycle as part of a protein complex that includes INCENP, Aurora B kinase, and Borealin. CAY10625 is an antagonist of the interaction between survivin and the apoptosis-promoting protein Smac/DIABLO, exhibiting an IC50 value of 2.2 µM.{18017} It inhibits the interaction of survivin with INCENP less effectively with an IC50 value of 20 µM. CAY10625 is cell-permeable and sensitizes cells to the induction of apoptosis by doxorubicin.{18017}
Brand:CaymanSKU:-
Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3′ hydroxyl position of PIs to produce PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3, important second messengers that modulate the activity of downstream targets Akt and mTOR.{8039} Aberrant PI3K/Akt is associated with many human cancers. CAY10626 is a potent, dual PI3Kα/mTOR inhibitor with IC50 values of 0.9 and 0.6 nM for the two respective kinases.{18031} In a tumor cell growth inhibition assay, CAY10626 demonstrates IC50 values of 50 mg/k to MD361 xenograft mice, phosphorylation of the downstream targets of PI3Kα and mTOR (Akt T308, Akt S473, and S6K) was suppressed, and significant tumor regression was observed.{18031}
Brand:CaymanSKU:- Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3′ hydroxyl position of PIs to produce PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3, important second messengers that modulate the activity of downstream targets Akt and mTOR.{8039} Aberrant PI3K/Akt is associated with many human cancers. CAY10626 is a potent, dual PI3Kα/mTOR inhibitor with IC50 values of 0.9 and 0.6 nM for the two respective kinases.{18031} In a tumor cell growth inhibition assay, CAY10626 demonstrates IC50 values of 50 mg/k to MD361 xenograft mice, phosphorylation of the downstream targets of PI3Kα and mTOR (Akt T308, Akt S473, and S6K) was suppressed, and significant tumor regression was observed.{18031}
Brand:CaymanSKU:- Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3′ hydroxyl position of PIs to produce PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3, important second messengers that modulate the activity of downstream targets Akt and mTOR.{8039} Aberrant PI3K/Akt is associated with many human cancers. CAY10626 is a potent, dual PI3Kα/mTOR inhibitor with IC50 values of 0.9 and 0.6 nM for the two respective kinases.{18031} In a tumor cell growth inhibition assay, CAY10626 demonstrates IC50 values of 50 mg/k to MD361 xenograft mice, phosphorylation of the downstream targets of PI3Kα and mTOR (Akt T308, Akt S473, and S6K) was suppressed, and significant tumor regression was observed.{18031}
Brand:CaymanSKU:- Phosphatidylinositol 3-kinase (PI3K) catalyzes the phosphorylation of the 3′ hydroxyl position of PIs to produce PtdIns-(3,4)-P2 and PtdIns-(3,4,5)-P3, important second messengers that modulate the activity of downstream targets Akt and mTOR.{8039} Aberrant PI3K/Akt is associated with many human cancers. CAY10626 is a potent, dual PI3Kα/mTOR inhibitor with IC50 values of 0.9 and 0.6 nM for the two respective kinases.{18031} In a tumor cell growth inhibition assay, CAY10626 demonstrates IC50 values of 50 mg/k to MD361 xenograft mice, phosphorylation of the downstream targets of PI3Kα and mTOR (Akt T308, Akt S473, and S6K) was suppressed, and significant tumor regression was observed.{18031}
Brand:CaymanSKU:-
Very long chain polyunsaturated fatty acids (VLCPUFA) are present in retina, sperm, and brain.{18974,237,19225} Though little is known of their biosynthesis or functional roles in these tissues, recent studies using the elongation of very long-chain FA-4 protein suggest a unique role for VLCPUFA in retinal development and macular degeneration.{18972,18973} CAY10632 is a C32:6 VLCPUFA whose specific biological actions are largely unknown, but are thought to involve normal photoreceptor cell function in the retina.{18972,19234}
Brand:CaymanSKU:10497 - 1 mgAvailable on backorder
Very long chain polyunsaturated fatty acids (VLCPUFA) are present in retina, sperm, and brain.{18974,237,19225} Though little is known of their biosynthesis or functional roles in these tissues, recent studies using the elongation of very long-chain FA-4 protein suggest a unique role for VLCPUFA in retinal development and macular degeneration.{18972,18973} CAY10632 is a C32:6 VLCPUFA whose specific biological actions are largely unknown, but are thought to involve normal photoreceptor cell function in the retina.{18972,19234}
Brand:CaymanSKU:10497 - 500 µgAvailable on backorder
Prostaglandins have a short life in vivo because NAD+-dependent 15-hydroxy prostaglandin dehydrogenase (15-PGDH) catalyzes their oxidation to 15-keto metabolites with greatly reduced biological activity.{340} Thiazolidinediones (TZDs) are a class of PPARγ agonists that have potent 15-PGDH inhibitory activity.{10583,17925} CAY10638 is a TZD derivative that inhibits 15-PGDH activity with an IC50 value of 31 nM.{17925}
Brand:CaymanSKU:- Prostaglandins have a short life in vivo because NAD+-dependent 15-hydroxy prostaglandin dehydrogenase (15-PGDH) catalyzes their oxidation to 15-keto metabolites with greatly reduced biological activity.{340} Thiazolidinediones (TZDs) are a class of PPARγ agonists that have potent 15-PGDH inhibitory activity.{10583,17925} CAY10638 is a TZD derivative that inhibits 15-PGDH activity with an IC50 value of 31 nM.{17925}
Brand:CaymanSKU:- Prostaglandins have a short life in vivo because NAD+-dependent 15-hydroxy prostaglandin dehydrogenase (15-PGDH) catalyzes their oxidation to 15-keto metabolites with greatly reduced biological activity.{340} Thiazolidinediones (TZDs) are a class of PPARγ agonists that have potent 15-PGDH inhibitory activity.{10583,17925} CAY10638 is a TZD derivative that inhibits 15-PGDH activity with an IC50 value of 31 nM.{17925}
Brand:CaymanSKU:- Prostaglandins have a short life in vivo because NAD+-dependent 15-hydroxy prostaglandin dehydrogenase (15-PGDH) catalyzes their oxidation to 15-keto metabolites with greatly reduced biological activity.{340} Thiazolidinediones (TZDs) are a class of PPARγ agonists that have potent 15-PGDH inhibitory activity.{10583,17925} CAY10638 is a TZD derivative that inhibits 15-PGDH activity with an IC50 value of 31 nM.{17925}
Brand:CaymanSKU:-
Soluble epoxide hydrolase (sEH) inhibitors have important therapeutic use by increasing the in vivo concentration of EETs and other fatty acid epoxides, resulting in anti-inflammatory, antihypertensive, neuroprotective, and cardioprotective effects. CAY10640 is a 1-aryl-3-(1-acylpiperidin-4-yl)urea analog that inhibits recombinant human and mouse sEH with IC50 values both equal to 0.4 nM.{18630} CAY10640 demonstrates a 1,000-fold increase in potency compared to morphine in reducing hyperalgesia in an in vivo carrageenan-induced inflammatory pain model.{18630}
Brand:CaymanSKU:10642 - 1 mgAvailable on backorder
Soluble epoxide hydrolase (sEH) inhibitors have important therapeutic use by increasing the in vivo concentration of EETs and other fatty acid epoxides, resulting in anti-inflammatory, antihypertensive, neuroprotective, and cardioprotective effects. CAY10640 is a 1-aryl-3-(1-acylpiperidin-4-yl)urea analog that inhibits recombinant human and mouse sEH with IC50 values both equal to 0.4 nM.{18630} CAY10640 demonstrates a 1,000-fold increase in potency compared to morphine in reducing hyperalgesia in an in vivo carrageenan-induced inflammatory pain model.{18630}
Brand:CaymanSKU:10642 - 10 mgAvailable on backorder
Soluble epoxide hydrolase (sEH) inhibitors have important therapeutic use by increasing the in vivo concentration of EETs and other fatty acid epoxides, resulting in anti-inflammatory, antihypertensive, neuroprotective, and cardioprotective effects. CAY10640 is a 1-aryl-3-(1-acylpiperidin-4-yl)urea analog that inhibits recombinant human and mouse sEH with IC50 values both equal to 0.4 nM.{18630} CAY10640 demonstrates a 1,000-fold increase in potency compared to morphine in reducing hyperalgesia in an in vivo carrageenan-induced inflammatory pain model.{18630}
Brand:CaymanSKU:10642 - 5 mgAvailable on backorder
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.{14663} CAY10641 is an inactive alcohol derivative of a highly potent (IC50 = 12 nM) cPLA2α inhibitor. {18732} The parent compound demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.{18732} CAY10641 is rapidly cleared from the blood stream (only 0.5 μg/ml remains 30 minutes after 10 mg/kg intravenous administration to mice).{18732} However, no other biological effects have been reported.
Brand:CaymanSKU:10662 - 1 mgAvailable on backorder
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.{14663} CAY10641 is an inactive alcohol derivative of a highly potent (IC50 = 12 nM) cPLA2α inhibitor. {18732} The parent compound demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.{18732} CAY10641 is rapidly cleared from the blood stream (only 0.5 μg/ml remains 30 minutes after 10 mg/kg intravenous administration to mice).{18732} However, no other biological effects have been reported.
Brand:CaymanSKU:10662 - 10 mgAvailable on backorder
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.{14663} CAY10641 is an inactive alcohol derivative of a highly potent (IC50 = 12 nM) cPLA2α inhibitor. {18732} The parent compound demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.{18732} CAY10641 is rapidly cleared from the blood stream (only 0.5 μg/ml remains 30 minutes after 10 mg/kg intravenous administration to mice).{18732} However, no other biological effects have been reported.
Brand:CaymanSKU:10662 - 5 mgAvailable on backorder
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.{14663} CAY10641 is an inactive alcohol derivative of a highly potent (IC50 = 12 nM) cPLA2α inhibitor. {18732} The parent compound demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.{18732} CAY10641 is rapidly cleared from the blood stream (only 0.5 μg/ml remains 30 minutes after 10 mg/kg intravenous administration to mice).{18732} However, no other biological effects have been reported.
Brand:CaymanSKU:10662 - 50 mgAvailable on backorder
CAY10647 is an aryl-benzoyl-imidazole which prevents proliferation of multidrug resistant cancer cells in vitro (IC50 = 28-63 nM) and inhibits melanoma xenograph tumor growth in vivo (10-30 mg/kg).{19224} This compound also binds to tubulin (Ki = 3.4 μM) and prevents tubulin polymerization.{19224}
Brand:CaymanSKU:10791 - 1 mgAvailable on backorder
CAY10647 is an aryl-benzoyl-imidazole which prevents proliferation of multidrug resistant cancer cells in vitro (IC50 = 28-63 nM) and inhibits melanoma xenograph tumor growth in vivo (10-30 mg/kg).{19224} This compound also binds to tubulin (Ki = 3.4 μM) and prevents tubulin polymerization.{19224}
Brand:CaymanSKU:10791 - 10 mgAvailable on backorder
CAY10647 is an aryl-benzoyl-imidazole which prevents proliferation of multidrug resistant cancer cells in vitro (IC50 = 28-63 nM) and inhibits melanoma xenograph tumor growth in vivo (10-30 mg/kg).{19224} This compound also binds to tubulin (Ki = 3.4 μM) and prevents tubulin polymerization.{19224}
Brand:CaymanSKU:10791 - 5 mgAvailable on backorder
Prostaglandin D2 (PGD2) evokes its effects through two receptors, DP1 and CRTH2/DP2. The activation of DP2 leads to eosinophil chemotaxis, activation, and degranulation as well as recruitment of basophils and lymphocytes and, as a result, is important in allergic inflammatory disease. CAY10648 is an intermediate used in the synthesis of potent DP2 receptor antagonists based on a novel spiro-indolinone compound.{15596}
Brand:CaymanSKU:9000549 - 1 mgAvailable on backorder
Prostaglandin D2 (PGD2) evokes its effects through two receptors, DP1 and CRTH2/DP2. The activation of DP2 leads to eosinophil chemotaxis, activation, and degranulation as well as recruitment of basophils and lymphocytes and, as a result, is important in allergic inflammatory disease. CAY10648 is an intermediate used in the synthesis of potent DP2 receptor antagonists based on a novel spiro-indolinone compound.{15596}
Brand:CaymanSKU:9000549 - 10 mgAvailable on backorder
Prostaglandin D2 (PGD2) evokes its effects through two receptors, DP1 and CRTH2/DP2. The activation of DP2 leads to eosinophil chemotaxis, activation, and degranulation as well as recruitment of basophils and lymphocytes and, as a result, is important in allergic inflammatory disease. CAY10648 is an intermediate used in the synthesis of potent DP2 receptor antagonists based on a novel spiro-indolinone compound.{15596}
Brand:CaymanSKU:9000549 - 5 mgAvailable on backorder
5-Lipoxygenase (5-LO) catalyzes the biosynthesis of leukotrienes, which are involved in a variety of inflammatory responses, including neutrophil chemotaxis, vascular permeability, and smooth muscle contraction.{482} CAY10649 is a thiazolinone compound that demonstrates direct inhibition of 5-lipoxygenase (5-LO) product formation in intact polymorphonuclear leukocytes (PMNL) (IC50 = 0.28 μM) and a soluble fraction of a S100 PMNL cell lysate (IC50 = 0.09 μM) after stimulation with calcium and arachidonic acid.{19236}
Brand:CaymanSKU:10804 - 1 mgAvailable on backorder
5-Lipoxygenase (5-LO) catalyzes the biosynthesis of leukotrienes, which are involved in a variety of inflammatory responses, including neutrophil chemotaxis, vascular permeability, and smooth muscle contraction.{482} CAY10649 is a thiazolinone compound that demonstrates direct inhibition of 5-lipoxygenase (5-LO) product formation in intact polymorphonuclear leukocytes (PMNL) (IC50 = 0.28 μM) and a soluble fraction of a S100 PMNL cell lysate (IC50 = 0.09 μM) after stimulation with calcium and arachidonic acid.{19236}
Brand:CaymanSKU:10804 - 10 mgAvailable on backorder
5-Lipoxygenase (5-LO) catalyzes the biosynthesis of leukotrienes, which are involved in a variety of inflammatory responses, including neutrophil chemotaxis, vascular permeability, and smooth muscle contraction.{482} CAY10649 is a thiazolinone compound that demonstrates direct inhibition of 5-lipoxygenase (5-LO) product formation in intact polymorphonuclear leukocytes (PMNL) (IC50 = 0.28 μM) and a soluble fraction of a S100 PMNL cell lysate (IC50 = 0.09 μM) after stimulation with calcium and arachidonic acid.{19236}
Brand:CaymanSKU:10804 - 5 mgAvailable on backorder
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.{14663} CAY10650 is a highly potent (IC50 = 12 nM) cPLA2α inhibitor.{18732} It demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.{18732} The phase I metabolite of this compound, CAY10641 (Item No. 10662), is also available.
Brand:CaymanSKU:10743 - 1 mgAvailable on backorder
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.{14663} CAY10650 is a highly potent (IC50 = 12 nM) cPLA2α inhibitor.{18732} It demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.{18732} The phase I metabolite of this compound, CAY10641 (Item No. 10662), is also available.
Brand:CaymanSKU:10743 - 10 mgAvailable on backorder
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.{14663} CAY10650 is a highly potent (IC50 = 12 nM) cPLA2α inhibitor.{18732} It demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.{18732} The phase I metabolite of this compound, CAY10641 (Item No. 10662), is also available.
Brand:CaymanSKU:10743 - 5 mgAvailable on backorder
Cytosolic phospholipase A2α (cPLA2α) specifically catalyzes the hydrolysis of arachidonic acid from the sn-2-ester position of membrane phospholipids, playing a central role in initiating the synthesis of prostaglandins and leukotrienes, both important mediators of the inflammatory process.{14663} CAY10650 is a highly potent (IC50 = 12 nM) cPLA2α inhibitor.{18732} It demonstrates strong anti-inflammatory effects when applied topically at a dose of 0.1 mg/ear in a mouse model of acute irritant contact dermatitis.{18732} The phase I metabolite of this compound, CAY10641 (Item No. 10662), is also available.
Brand:CaymanSKU:10743 - 50 mgAvailable on backorder
The gram-negative pathogen Pseudomonas aeruginosa uses N-acylated-L-homoserine lactones (AHLs) in quorum sensing to modulate transcriptional activators, including LasR, and regulate the expression of virulence factors. The same AHLs suppress the host immune system. CAY10654 is a synthetic analog of natural AHLs that suppresses host immunity without inducing LasR.{19410} It inhibits the proliferation of mouse peripheral blood leukocytes by concanavalin A (EC50 = 9.3 μM) without concurrent cytotoxicity.{19410} LasR is not induced by 100 μM CAY10654, although LasR is potently induced by natural AHL (5 μM) in positive control experiments.{19410}
Brand:CaymanSKU:10857 - 1 mgAvailable on backorder
The gram-negative pathogen Pseudomonas aeruginosa uses N-acylated-L-homoserine lactones (AHLs) in quorum sensing to modulate transcriptional activators, including LasR, and regulate the expression of virulence factors. The same AHLs suppress the host immune system. CAY10654 is a synthetic analog of natural AHLs that suppresses host immunity without inducing LasR.{19410} It inhibits the proliferation of mouse peripheral blood leukocytes by concanavalin A (EC50 = 9.3 μM) without concurrent cytotoxicity.{19410} LasR is not induced by 100 μM CAY10654, although LasR is potently induced by natural AHL (5 μM) in positive control experiments.{19410}
Brand:CaymanSKU:10857 - 10 mgAvailable on backorder
The gram-negative pathogen Pseudomonas aeruginosa uses N-acylated-L-homoserine lactones (AHLs) in quorum sensing to modulate transcriptional activators, including LasR, and regulate the expression of virulence factors. The same AHLs suppress the host immune system. CAY10654 is a synthetic analog of natural AHLs that suppresses host immunity without inducing LasR.{19410} It inhibits the proliferation of mouse peripheral blood leukocytes by concanavalin A (EC50 = 9.3 μM) without concurrent cytotoxicity.{19410} LasR is not induced by 100 μM CAY10654, although LasR is potently induced by natural AHL (5 μM) in positive control experiments.{19410}
Brand:CaymanSKU:10857 - 25 mgAvailable on backorder
The gram-negative pathogen Pseudomonas aeruginosa uses N-acylated-L-homoserine lactones (AHLs) in quorum sensing to modulate transcriptional activators, including LasR, and regulate the expression of virulence factors. The same AHLs suppress the host immune system. CAY10654 is a synthetic analog of natural AHLs that suppresses host immunity without inducing LasR.{19410} It inhibits the proliferation of mouse peripheral blood leukocytes by concanavalin A (EC50 = 9.3 μM) without concurrent cytotoxicity.{19410} LasR is not induced by 100 μM CAY10654, although LasR is potently induced by natural AHL (5 μM) in positive control experiments.{19410}
Brand:CaymanSKU:10857 - 5 mgAvailable on backorder
The NF-κB/Rel family of transcription factors induce and coordinate the expression of pro-inflammatory genes including cytokines, chemokines, interferons, MHC proteins, growth factors, and cell adhesion molecules. Under resting conditions NF-κB dimers are retained in the cytoplasm by a member of the IκB family of inhibitory proteins. Upon activation by cytokines or other stimuli, IKK phosphorylates IκB, initiating a signaling cascade to activate gene transcription.{7136,8494,18544} CAY10657 is a thiophenecarboximide derivative proposed to inhibit IKK2.{20631} Currently, there are no published reports of its biological activity. However, inhibition of NF-κB activation is likely to be of broad utility in the treatment of inflammatory diseases and cancer.{17345,17344}
Brand:CaymanSKU:11140 - 1 mgAvailable on backorder
The NF-κB/Rel family of transcription factors induce and coordinate the expression of pro-inflammatory genes including cytokines, chemokines, interferons, MHC proteins, growth factors, and cell adhesion molecules. Under resting conditions NF-κB dimers are retained in the cytoplasm by a member of the IκB family of inhibitory proteins. Upon activation by cytokines or other stimuli, IKK phosphorylates IκB, initiating a signaling cascade to activate gene transcription.{7136,8494,18544} CAY10657 is a thiophenecarboximide derivative proposed to inhibit IKK2.{20631} Currently, there are no published reports of its biological activity. However, inhibition of NF-κB activation is likely to be of broad utility in the treatment of inflammatory diseases and cancer.{17345,17344}
Brand:CaymanSKU:11140 - 10 mgAvailable on backorder
The NF-κB/Rel family of transcription factors induce and coordinate the expression of pro-inflammatory genes including cytokines, chemokines, interferons, MHC proteins, growth factors, and cell adhesion molecules. Under resting conditions NF-κB dimers are retained in the cytoplasm by a member of the IκB family of inhibitory proteins. Upon activation by cytokines or other stimuli, IKK phosphorylates IκB, initiating a signaling cascade to activate gene transcription.{7136,8494,18544} CAY10657 is a thiophenecarboximide derivative proposed to inhibit IKK2.{20631} Currently, there are no published reports of its biological activity. However, inhibition of NF-κB activation is likely to be of broad utility in the treatment of inflammatory diseases and cancer.{17345,17344}
Brand:CaymanSKU:11140 - 5 mgAvailable on backorder
17(R),18(S)-Epoxyeicosatetraenoic acid (17(R),18(S)-EpETE), a natural cytochrome P450 epoxygenase metabolite of eicosapentaenoic acid, is known to reduce the contraction rate of spontaneously beating heart cells and to protect neonatal rat cardiomyocytes against arrhythmias induced by β-adrenergic agonists (EC50 = ~ 1-2 nM).{19905} CAY10662 is a 1,3 disubstituted urea derivative of 17(R),18(S)-EpETE that is more metabolically robust and reduces the contractility of cardiomyocytes with improved potency (EC50 fold higher than required for the effect on cardiomyocytes, 1-5 μM CAY10662 exerts weak dose-dependent soluble epoxide hydrolase inhibition.{19905}
Brand:CaymanSKU:11042 - 100 µgAvailable on backorder
17(R),18(S)-Epoxyeicosatetraenoic acid (17(R),18(S)-EpETE), a natural cytochrome P450 epoxygenase metabolite of eicosapentaenoic acid, is known to reduce the contraction rate of spontaneously beating heart cells and to protect neonatal rat cardiomyocytes against arrhythmias induced by β-adrenergic agonists (EC50 = ~ 1-2 nM).{19905} CAY10662 is a 1,3 disubstituted urea derivative of 17(R),18(S)-EpETE that is more metabolically robust and reduces the contractility of cardiomyocytes with improved potency (EC50 fold higher than required for the effect on cardiomyocytes, 1-5 μM CAY10662 exerts weak dose-dependent soluble epoxide hydrolase inhibition.{19905}
Brand:CaymanSKU:11042 - 25 µgAvailable on backorder
17(R),18(S)-Epoxyeicosatetraenoic acid (17(R),18(S)-EpETE), a natural cytochrome P450 epoxygenase metabolite of eicosapentaenoic acid, is known to reduce the contraction rate of spontaneously beating heart cells and to protect neonatal rat cardiomyocytes against arrhythmias induced by β-adrenergic agonists (EC50 = ~ 1-2 nM).{19905} CAY10662 is a 1,3 disubstituted urea derivative of 17(R),18(S)-EpETE that is more metabolically robust and reduces the contractility of cardiomyocytes with improved potency (EC50 fold higher than required for the effect on cardiomyocytes, 1-5 μM CAY10662 exerts weak dose-dependent soluble epoxide hydrolase inhibition.{19905}
Brand:CaymanSKU:11042 - 50 µgAvailable on backorder
17(R),18(S)-Epoxyeicosatetraenoic acid (17(R),18(S)-EpETE), a natural cytochrome P450 epoxygenase metabolite of eicosapentaenoic acid, is known to reduce the contraction rate of spontaneously beating heart cells and to protect neonatal rat cardiomyocytes against arrhythmias induced by β-adrenergic agonists (EC50 = ~ 1-2 nM).{19905} CAY10662 is a 1,3 disubstituted urea derivative of 17(R),18(S)-EpETE that is more metabolically robust and reduces the contractility of cardiomyocytes with improved potency (EC50 fold higher than required for the effect on cardiomyocytes, 1-5 μM CAY10662 exerts weak dose-dependent soluble epoxide hydrolase inhibition.{19905}
Brand:CaymanSKU:11042 - 500 µgAvailable on backorder
Isolated neonatal rat cardiomyocytes, which spontaneously beat in culture, are used to evaluate the antiarrhythmic effects of polyunsaturated fatty acids (PUFA).{21675} In this model, the ω-3 PUFA eicosapentaenoic acid (EPA, 3-10 μM) reduces the contraction rate of cells, indicating a positive antiarrhythmic effect.{21675} Cytochrome P450 metabolites of EPA are more potent, with 17,18-epoxyeicosatetraenoic acid (17,18-EET) reducing contractions at 30 nM.{18672} CAY10665 is a bioisostere of 17,18-EET which is approximately 50% more effective at reducing arrhythmic contraction frequency, without affecting amplitude, when tested at 30 nM.{19905} This disubstituted oxamide represents a stable analog of 17,18-EET which may be used to study the mechanism of regulation of cardiomyocyte contractility by EPA metabolites.
Brand:CaymanSKU:11044 - 100 µgAvailable on backorder
Isolated neonatal rat cardiomyocytes, which spontaneously beat in culture, are used to evaluate the antiarrhythmic effects of polyunsaturated fatty acids (PUFA).{21675} In this model, the ω-3 PUFA eicosapentaenoic acid (EPA, 3-10 μM) reduces the contraction rate of cells, indicating a positive antiarrhythmic effect.{21675} Cytochrome P450 metabolites of EPA are more potent, with 17,18-epoxyeicosatetraenoic acid (17,18-EET) reducing contractions at 30 nM.{18672} CAY10665 is a bioisostere of 17,18-EET which is approximately 50% more effective at reducing arrhythmic contraction frequency, without affecting amplitude, when tested at 30 nM.{19905} This disubstituted oxamide represents a stable analog of 17,18-EET which may be used to study the mechanism of regulation of cardiomyocyte contractility by EPA metabolites.
Brand:CaymanSKU:11044 - 25 µgAvailable on backorder
Isolated neonatal rat cardiomyocytes, which spontaneously beat in culture, are used to evaluate the antiarrhythmic effects of polyunsaturated fatty acids (PUFA).{21675} In this model, the ω-3 PUFA eicosapentaenoic acid (EPA, 3-10 μM) reduces the contraction rate of cells, indicating a positive antiarrhythmic effect.{21675} Cytochrome P450 metabolites of EPA are more potent, with 17,18-epoxyeicosatetraenoic acid (17,18-EET) reducing contractions at 30 nM.{18672} CAY10665 is a bioisostere of 17,18-EET which is approximately 50% more effective at reducing arrhythmic contraction frequency, without affecting amplitude, when tested at 30 nM.{19905} This disubstituted oxamide represents a stable analog of 17,18-EET which may be used to study the mechanism of regulation of cardiomyocyte contractility by EPA metabolites.
Brand:CaymanSKU:11044 - 50 µgAvailable on backorder
Isolated neonatal rat cardiomyocytes, which spontaneously beat in culture, are used to evaluate the antiarrhythmic effects of polyunsaturated fatty acids (PUFA).{21675} In this model, the ω-3 PUFA eicosapentaenoic acid (EPA, 3-10 μM) reduces the contraction rate of cells, indicating a positive antiarrhythmic effect.{21675} Cytochrome P450 metabolites of EPA are more potent, with 17,18-epoxyeicosatetraenoic acid (17,18-EET) reducing contractions at 30 nM.{18672} CAY10665 is a bioisostere of 17,18-EET which is approximately 50% more effective at reducing arrhythmic contraction frequency, without affecting amplitude, when tested at 30 nM.{19905} This disubstituted oxamide represents a stable analog of 17,18-EET which may be used to study the mechanism of regulation of cardiomyocyte contractility by EPA metabolites.
Brand:CaymanSKU:11044 - 500 µgAvailable on backorder
CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid (Item No. 13144).{19657} At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro.{19657}
Brand:CaymanSKU:10974 - 1 mgAvailable on backorder
CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid (Item No. 13144).{19657} At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro.{19657}
Brand:CaymanSKU:10974 - 10 mgAvailable on backorder
CAY10669 is an inhibitor of the histone acetyltransferase PCAF (p300/CREB-binding protein-associated factor; IC50 = 662 μM), displaying a 2-fold improvement in inhibitory potency over anacardic acid (Item No. 13144).{19657} At 30-60 μM, CAY10669 can dose-dependently inhibit histone H4 acetylation in HepG2 cells in vitro.{19657}
Brand:CaymanSKU:10974 - 5 mgAvailable on backorder
Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Isoprenylcysteine carboxyl methyltransferase (Icmt) catalyzes the methylation of C-terminal prenylcysteine residues, the last step in this process. CAY10677 is an analog of the Icmt inhibitor cysmethynil (Item No. 14745) that was developed for improved solubility and cell permeability.{23335} CAY10677 inhibits Icmt with an IC50 value of 0.86 μM and demonstrates nearly 10-fold more potent antiproliferative activity than cysmethynil on human breast cancer MDA-MB-231 cells (IC50s = 2.63 versus 27.4 μM, respectively) and human prostate cancer PC3 cells (IC50s = 2.55 versus 25.2 μM, respectively).{23335}
Brand:CaymanSKU:- Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Isoprenylcysteine carboxyl methyltransferase (Icmt) catalyzes the methylation of C-terminal prenylcysteine residues, the last step in this process. CAY10677 is an analog of the Icmt inhibitor cysmethynil (Item No. 14745) that was developed for improved solubility and cell permeability.{23335} CAY10677 inhibits Icmt with an IC50 value of 0.86 μM and demonstrates nearly 10-fold more potent antiproliferative activity than cysmethynil on human breast cancer MDA-MB-231 cells (IC50s = 2.63 versus 27.4 μM, respectively) and human prostate cancer PC3 cells (IC50s = 2.55 versus 25.2 μM, respectively).{23335}
Brand:CaymanSKU:- Post-translational protein prenylation is a 3-step process that occurs at the C-terminus of a number of proteins involved in cell growth control and oncogenesis. Isoprenylcysteine carboxyl methyltransferase (Icmt) catalyzes the methylation of C-terminal prenylcysteine residues, the last step in this process. CAY10677 is an analog of the Icmt inhibitor cysmethynil (Item No. 14745) that was developed for improved solubility and cell permeability.{23335} CAY10677 inhibits Icmt with an IC50 value of 0.86 μM and demonstrates nearly 10-fold more potent antiproliferative activity than cysmethynil on human breast cancer MDA-MB-231 cells (IC50s = 2.63 versus 27.4 μM, respectively) and human prostate cancer PC3 cells (IC50s = 2.55 versus 25.2 μM, respectively).{23335}
Brand:CaymanSKU:-
Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively).{23940} It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration.{23940} CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β.{23940} It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.{23940}
Brand:CaymanSKU:- Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively).{23940} It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration.{23940} CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β.{23940} It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.{23940}
Brand:CaymanSKU:- Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2.{7229} Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1β, and TNF-α.{11537} CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively).{23940} It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 μM but reduces lipocalin-type PGDS activity by 60% at this concentration.{23940} CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1β.{23940} It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.{23940}
Brand:CaymanSKU:-
CAY10679 is an anionic oligopeptide-based bola-amphiphile that contains a hexane moiety flanked by a glycylglycine group at each end, which creates distinct hydrophilic and hydrophobic regions.{24677} The microtube self-assembling properties of this amphiphilic peptide have been studied in aqueous acidic solution.{24606} Bola-amphiphiles are of interest in the construction of nanotubes, nanovesicles, nanowires, nanocarriers for drug delivery, and other applications of bionanotechnology.{24677}
Brand:CaymanSKU:9001475 - 10 mgAvailable on backorder
CAY10679 is an anionic oligopeptide-based bola-amphiphile that contains a hexane moiety flanked by a glycylglycine group at each end, which creates distinct hydrophilic and hydrophobic regions.{24677} The microtube self-assembling properties of this amphiphilic peptide have been studied in aqueous acidic solution.{24606} Bola-amphiphiles are of interest in the construction of nanotubes, nanovesicles, nanowires, nanocarriers for drug delivery, and other applications of bionanotechnology.{24677}
Brand:CaymanSKU:9001475 - 100 mgAvailable on backorder
CAY10679 is an anionic oligopeptide-based bola-amphiphile that contains a hexane moiety flanked by a glycylglycine group at each end, which creates distinct hydrophilic and hydrophobic regions.{24677} The microtube self-assembling properties of this amphiphilic peptide have been studied in aqueous acidic solution.{24606} Bola-amphiphiles are of interest in the construction of nanotubes, nanovesicles, nanowires, nanocarriers for drug delivery, and other applications of bionanotechnology.{24677}
Brand:CaymanSKU:9001475 - 25 mgAvailable on backorder
CAY10679 is an anionic oligopeptide-based bola-amphiphile that contains a hexane moiety flanked by a glycylglycine group at each end, which creates distinct hydrophilic and hydrophobic regions.{24677} The microtube self-assembling properties of this amphiphilic peptide have been studied in aqueous acidic solution.{24606} Bola-amphiphiles are of interest in the construction of nanotubes, nanovesicles, nanowires, nanocarriers for drug delivery, and other applications of bionanotechnology.{24677}
Brand:CaymanSKU:9001475 - 50 mgAvailable on backorder
CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human).{25432} It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 µM) and MAO-A (IC50 ≥ 10 µM).{25432} At 1-20 µM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors.{25432} In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson’s disease. An additional strategy in the treatment of Parkinson’s disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.
Brand:CaymanSKU:- CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human).{25432} It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 µM) and MAO-A (IC50 ≥ 10 µM).{25432} At 1-20 µM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors.{25432} In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson’s disease. An additional strategy in the treatment of Parkinson’s disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.
Brand:CaymanSKU:- CAY10680 is a dopamine-sparing, benzothiazinone compound that selectively inhibits both MAO-B activity (IC50 = 34.9 nM in human) and adenosine A2A receptors (Ki = 39.5 nM in human).{25432} It demonstrates significantly less potent inhibitory values for other adenosine receptor subtypes (Kis > 1 µM) and MAO-A (IC50 ≥ 10 µM).{25432} At 1-20 µM, CAY10680 has been shown to abolish cAMP accumulation in CHO cells transfected with adenosine A2A receptors.{25432} In the central nervous system adenosine A2A receptor expression is localized to dopamine-innervated areas where heteromeric complexes are formed with dopamine D2 receptors. Because inhibition of adenosine A2A receptors has been shown to enhance D2 receptor function, the blockade of adenosine A2A receptors has emerged as a potential treatment for Parkinson’s disease. An additional strategy in the treatment of Parkinson’s disease has been to block the activity of monoamine oxidase B (MAO-B), the enzyme involved in dopamine catabolism.
Brand:CaymanSKU:-