Diazoxide-d3 is intended for use as an internal standard for the quantification of diazoxide (Item No. 14576) by GC- or LC-MS. Diazoxide is an activator of sulfonylurea receptor 1 (SUR1) linked to ATP-sensitive potassium channel Kir6.2 (EC50 = 14.1 µM in a FLIPR assay using HEK293 cells).{36318} It also activates SUR2A/Kir6.2 and SUR2B/Kir6.2 channels in HEK293T cells in a patch-clamp assay when used at concentrations of 30 and 300 µM.{48765} Diazoxide inhibits glucose-induced insulin release from isolated rat pancreatic β cells and induces relaxation of isolated rat aortic rings precontracted with potassium chloride (IC50s = 22.6 and 22.4 µM, respectively).{48766} It reduces mean arterial pressure and cerebral blood flow in spontaneously hypertensive rats when administered intravenously as a 5 mg/kg bolus dose.{48767} Diazoxide (50 mg/kg, i.p.) increases blood glucose levels in mice.{48768} Formulations containing diazoxide have been used in the treatment of hypoglycemia.
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An internal standard for the quantification of diazoxide by GC- or LC-MS
Formal name: 7-chloro-3-(methyl-d3)-4H-benzo[e][1,2,4]thiadiazine 1,1-dioxide
Synonyms:
Molecular weight: 233.7
CAS: 1432063-51-8
Purity: ≥99% deuterated forms (d1-d3)
Formulation: A solid
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}
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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}
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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}
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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.
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