Brinzolamide-d5 is intended for use as an internal standard for the quantification of brinzolamide (Item No. 11660) by GC- or LC-MS. Brinzolamide is a potent inhibitor of carbonic anhydrase II (CAII) and CAIV (IC50s = 3.19 and 45.3 nM, respectively).{53202} It is selective for CAII and CAIV over CAI (IC50 = ~1,365 nM). Brinzolamide (30 mg/kg) reduces intestinal charcoal meal progression by 44% and prolongs pentobarbital sodium-induced sleep time by 35% in mice. Topical administration of brinzolamide (0.25, 0.5, and 1 mg/eye) reduces intraocular pressure in a rabbit model of spontaneous ocular hypertension. It also reduces intraocular pressure in a cynomolgus monkey model of argon laser trabeculoplasty-induced ocular hypertension. Formulations containing brinzolamide have been used in the treatment of glaucoma and ocular hypertension.
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An internal standard for the quantification of brinzolamide by GC- or LC-MS
Formal name: (4R)-4-(ethyl-1,1,2,2,2-d5-amino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide, 1,1-dioxide
Synonyms:
Molecular weight: 388.5
CAS: 1217651-02-9
Purity: ≥99% deuterated forms (d1-d5)
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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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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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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