S81435 |
1400 W Dihydrochloride |
源葉(MedMol) | 98% |
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- 產(chǎn)品描述: 1400W dihydrochloride is a potent and selective inhibitor of human inducible NO synthase with Ki values of 7 nM.
- 靶點: Ki: 7 nM (iNOS), 2 μM (nNOS), 50 μM (eNOS);NOS;?NOSynthase
- 體外研究:
1400W is a slow, tight binding inhibitor of human inducible nitric- oxide synthase (iNOS). The slow onset of inhibition by 1400W shows saturation kinetics with a maximal rate constant of 0.028 s-1 and a binding constant of 2.0 μM. Inhibition is dependent on the cofactor NADPH. 1400W is at least 5000-fold selective for iNOS versus eNOS. In contrast, inhibition of human neuronal NOS and endothelial NOS (eNOS) is relatively weaker, rapidly reversible, and competitive with L-arginine, with Ki values of 2 μM and 50 μM, respectively. 1400W treatment inhibits iNOS expression without affecting nNOS or eNOS. 1400W also reduces NO, 3-NT and MDA production, and prevents neuronal cell apoptosis in cerebral cortex.
- 體內(nèi)研究:
1400W potently (ED50=0.3 mg/kg) reduces the delayed vascular injury in rats attributable to LPS-induced iNOS but fails to exacerbate acute vascular leakage when given concurrently with LPS. Administration of 1400W lowers NOx levels in all the experimental groups. In addition, lipid peroxidation, the percentage of apoptotic cells, and nitrated protein expression fall in the late post-hypoxia period (48 h and 5 days).
- 參考文獻:
1. Garvey EP, et al. 1400W is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase in vitro and in vivo. J Biol Chem. 1997 Feb 21;272(8):4959-63. 2. Shi Q, et al. 1400W ameliorates acute hypobaric hypoxia/reoxygenation-induced cognitive deficits by suppressing the induction of inducible nitric oxide synthase in rat cerebral cortex microglia. Behav Brain Res. 2017 Feb 15;319:188-199. 3. Rus A, et al. Inducible NOS inhibitor 1400W reduces hypoxia/re-oxygenation injury in rat lung. Redox Rep. 2010;15(4):169-78.
- 溶解性: Soluble in DMSO、H2O
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 3.997 ml 19.986 ml 39.973 ml 5 mM 0.799 ml 3.997 ml 7.995 ml 10 mM 0.4 ml 1.999 ml 3.997 ml 50 mM 0.08 ml 0.4 ml 0.799 ml
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輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)