Results for Activators & Inhibitors ( 70880 )
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(+)-Geodin (Legacy Tebubio ref. 282T37232). (+)-Geodin is a fungal metabolite. It increases the fibrinolytic activity of bovine aortic endothelial cells (BAECs) when used at concentrations ranging from 50 to 150 μM. (+)-Geodin (1-100 μg/ml) also increases 2-deoxyglucose uptake by rat adipocytes.
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(±)14(15)-EpEDE (Legacy Tebubio ref. 282T37233). 8,11,14-Eicosatrienoic acid, also known as dihomo-γ-linolenic acid , is a polyunsaturated fatty acid (PUFA) produced from γ-linolenic acid by the action of fatty acid elongases. It can be metabolized by the cyclooxygenase pathway to produce 1-series prostaglandins (PGs) (e.g., PGE1). (±)14(15)-EpEDE is an EpEDE acid formed from 8,11,14-eicosatrienoic acid. This monoepoxide can be generated from the PUFA, in vitro, by the action of a strong oxidizing agent. Alternatively, this compound may be produced, in vivo, by epoxidation of the PUFA by cytochrome P450 epoxygenases. The biological properties of this compound are poorly understood.
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(±)14(15)-EpETE (Legacy Tebubio ref. 282T37234). EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids, produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoic acid have been little studied relative to arachidonate epoxygenase metabolites. (±)14(15)-EpETE is the ω-3 homolog of 14(15)-EpETrE, derived via epoxidation of the 14,15-double bond of EPA. The EDHF activity of (±)14(15)-EpETE has not yet been determined.
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(±)17(18)-DiHETE (Legacy Tebubio ref. 282T37236). Eicosapentaenoic acid is an ω-3 fatty acid abundantly available in marine organisms. (±)17(18)-DiHETE is one of the major metabolites produced when eicosapentaenoic acid (EPA) is incubated with various rat tissue homogenates or cynomolgus monkey seminal vesicles. The route of production of (±)17(18)-DiHETE likely proceeds through cytochrome P450-catalyzed epoxidation at the ω-3 double bond followed by conversion to the vicinal diols by epoxide hydrolase. EPA is also metabolized preferentially by Gaeumannomyces graminis to (±)17(18)-DiHETE.
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(±)19(20)-EpDPA (Legacy Tebubio ref. 282T37238). EDHF (endothelium-derived hyperpolarizing factor) is an unidentified mediator released from vascular endothelial cells in response to acetylcholine and bradykinin which is distinct from the NOS- (nitric oxide) and COX-derived (prostacyclin) vasodilators. Cytochrome P450 (CYP450) metabolism of polyunsaturated fatty acids produces epoxides such as (±)14(15)-EpETrE which are prime candidates for the actual active mediator. However, the CYP450 metabolites of eicosapentaenoic acid and docosahexaenoic acid have been little studied relative to arachidonate epoxygenase metabolites. (±)19(20)-EpDPA is a DHA epoxygenase metabolite, derived via epoxidation of the ω-3 double bond of DHA. The EDHF activity of (±)19(20)-EpDPA has not yet been determined. The epoxygenase metabolites of DHA have also been detected in a mouse inflammation model.
- Ref: T3724Sizes: 1 mg, 5 mg, 25 mg, 100 mg, 50 mg, 10 mg, 200 mg, 1 mL * 10 mM (in DMSO)From: €176.00
Rolapitant hydrochloride (Legacy Tebubio ref. 282T3724). Rolapitant (SCH619734) hydrochloride is a potent, selective, long-acting, and orally active neurokinin 1 (NK1) receptor antagonist with a K_i of 0.66 nM, which does not interact with CYP3A4 and demonstrates potent centrally-mediated anti-emetic activity in both acute and delayed ferret emesis models [1] [2].
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(±)4(5)-DiHDPA lactone (Legacy Tebubio ref. 282T37240). (±)5(6)-DiHET lactone is a 1,5 cyclic ester derived from (±)5(6)-DiHET , which, in turn, is a potential derivative of epoxidation of arachidonic acid at the α-5 double bond. (±)4(5)-DiHDPA lactone is a derivative of docosahexaenoic acid that is analogous to (±)5(6)-DiHET lactone. It is the 1,4 cyclic ester derived from (±)4(5)-DiHDPA, which is produced by epoxidation of DHA at the α-4 double bond. Its biological activity is unknown.