Vigabatrin is an irreversible GABA transaminase (GABA-T) inhibitor.{55297} It inhibits rat brain GABA-T when used at a concentration of 0.1 mM. Vigabatrin is selective for rat brain GABA-T over P. fluorescens GABA-T at 10 mM and is 100-fold selective over rat brain glutamic acid decarboxylase (GAD). Vigabatrin (1,500 mg/kg) decreases brain GABA-T activity without affecting GAD activity in mice.{55298} It reduces the incidence of myoclonus in a mouse model of audiogenic seizures.{55299} Vigabatrin also increases the electroconvulsive threshold in mouse model of maximal electroshock-induced seizures and reduces the number of clonic convulsions induced by pentylenetetrazol (PTZ; Item No. 18682) in mice.{55300} Formulations containing vigabatrin have been used in the treatment of seizures and infantile spasms.
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A structural analog of the inhibitory neurotransmitter GABA that irreversibly inhibits its catabolism by GABA transaminase; produces a dose-dependent increase in extracellular GABA, and has been shown to result in increasing seizure suppression
Formal name: 4-amino-5-hexenoic acid
Synonyms: γ-Vinyl GABA
Molecular weight: 129.2
CAS: 68506-86-5
Purity: ≥95%
Formulation: A crystalline 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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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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