Phenoxybenzamine-d5 is intended for use as an internal standard for the quantification of phenoxybenzamine (Item No. 16211) by GC- or LC-MS. Phenoxybenzamine is an antagonist of α-adrenergic receptors (α-ARs).{53203,26625} It inhibits norepinephrine-induced inositol phosphate formation in HEK293 cells expressing α1-ARs (EC50s = 125.9-316.2 nM), as well as radioligand binding to α2A-, α2B-, and α2C-ARs in CHO cell membranes (Kis = 60, 10, and 60 nM, respectively). Phenoxybenzamine (0.5-5 µM) decreases norepinephrine-, histamine-, and calcium-induced contractions in isolated rabbit aortic strips.{53204} It also inhibits proliferation of nine cancer cell lines, including lymphoma, breast, and lung cancer cells, with IC50 values ranging from 29.5 to 99.8 µM.{53205} Phenoxybenzamine (3-1,000 µg/kg) reduces increases in diastolic blood pressure induced by the α-AR agonists cirazoline (Item No. 21791), St-587, Sgd 101/75, and B-HT 920 (Item No. 14177) in pithed rats.{53206} It also decreases the time to find the platform in the Morris water maze, indicating restored spatial memory, in a rat model of fluid percussion-induced traumatic brain injury (TBI).{53207} Formulations containing phenoxybenzamine have been used in the treatment of hypertension and hyperhidrosis associated with pheochromocytomas, an adrenal medullary neuroendocrine tumor.
Available on backorder
An internal standard for the quantification of phenoxybenzamine by GC- or LC-MS
Formal name: N-benzyl-N-(2-chloroethyl)-1-(phenoxy-d5)propan-2-amine, monohydrochloride
Synonyms:
Molecular weight: 345.3
CAS: 1329838-45-0
Purity: ≥98% deuterated forms (d1-d5)
Formulation: A solid
The maintenance of embryonic stem cells in culture typically requires feeder cells and various exogenous factors found in serum. Murine embryonic stem (mES) cells can be maintained in the absence of feeder cells and serum but require the leukemia inhibitor factor (LIF) and bone morphogenic protein (BMP) to prevent differentiation and promote self-renewal. SC-1 is a small molecule activator of stem cell renewal that allows the propagation of OG2 mES cells for at least 10 passages in an undifferentiated state.{14533} The activity of SC-1 is mediated by the combined inhibition of RasGAP and ERK1 with Kd values of 98 and 212 nM, respectively.{14533} Inhibition of RasGAP increases Ras signaling via the PI3-kinase pathway which promotes self-renewal, whereas inhibition of ERK blocks differentiation.
Available on backorder
Cyclin-dependent kinases (CDKs) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. (R)-Roscovitine is a potent inhibitor of Cdk2/cyclin E with an IC50 value of 0.1 µM.{14988} It also inhibits Cdk7/cyclin H, Cdk5/p35, and cell division cycle (cdc)/cyclin B with IC50 values of 0.49, 0.16, and 0.65 µM, respectively.{14987,14988,14991} (R)-Roscovitine inhibits the growth of rapidly proliferating cells with an average IC50 value of 15.2 µM against a panel of 19 human tumor cell lines.{14988} In murine models of polycystic kidney disease, (R)-roscovitine effectively inhibited disease progression at doses of 50-100 mg/kg.{14564}
Available on backorder
1,2-Dipalmitoyl-sn-glycero-3-PC (DPPC) is a zwitterionic glycerophospholipid commonly used in the formation of lipid monolayers, bilayers, and liposomes for use in a variety of applications.{14480,24261,14478,14479} It has been used in the formation of proteoliposomes for implantation of γ-glutamyl transpeptidase into human erythrocyte membranes.{14478} Incorporation of glycosphingolipid antigens into DPPC-containing liposomes increases the immunogenicity of the antigens in mice.{14479}
Available on backorder
The PtdIn phosphates play an important role in the generation and transduction of intracellular signals.{8344,4096,14518} PtdIns-(3,4,5)-P3-biotin is an affinity probe which allows the PIP3 to be detected through an interaction with the biotin ligand. This design allows PtdIns-(3,4,5)-P3-biotin to serve as a general probe for any protein with a high affinity binding interaction with inositol-(3,4,5)-triphosphate phospholipids, such as phosphatidylinositol 3-kinase, PTEN, or PH-domain-containing proteins.
Available on backorder