| 產品描述： | Ro 61-8048 is an orally active and selective inhibitor of kynurenine 3-hydroxylase, with an IC50 of 37 nM. Ro 61-8048 provokes a significant increase of extracellular kynurenic acid concentrations |
| 靶點： |
Hydroxylase |
| 體內研究： |
Ro 61-8048 (50, 100 and 150 mg/kg i.p.) significantly reduces the severity of dystonia in dtsz hamsters without leading to marked central side effects. Ro 61-8048 (100 mg/kg i.p.) provokes a two- to threefold increase of the endogeneous broad spectrum glutamate receptor antagonist kynurenic acid in the striatum, cerebellum and brainstem of mutant hamsters. |
| 參考文獻： |
1. S R?ver, et al. Synthesis and biochemical evaluation of N-(4-phenylthiazol-2-yl)benzenesulfonamides as high-affinity inhibitors of kynurenine 3-hydroxylase. J Med Chem. 1997 Dec 19;40(26):4378-85. 2. Melanie Hamann, et al. Effects of the kynurenine 3-hydroxylase inhibitor Ro 61-8048 after intrastriatal injections on the severity of dystonia in the dt sz mutant. Eur J Pharmacol. 2008 May 31;586(1-3):156-9. 3. AlbertoChiarugi, et al. Quinolinic acid formation in immune-activated mice: studies with (m-nitrobenzoyl)-alanine (mNBA) and 3,4-dimethoxy-[-N-4-(-3-nitrophenyl) thiazol-2yl]-benzenesulfonamide (Ro 61-8048), two potent and selective inhibitors of kynureni |
| 溶解性： |
DMSO : ≥ 59 mg/mL (139.99 mM) |
| 保存條件： |
2-8℃ |
| 配置溶液濃度參考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.373 ml |
11.864 ml |
23.728 ml |
| 5 mM |
0.475 ml |
2.373 ml |
4.746 ml |
| 10 mM |
0.237 ml |
1.186 ml |
2.373 ml |
| 50 mM |
0.047 ml |
0.237 ml |
0.475 ml |
|
| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
危險品化學品經營許可證（不帶存儲）
營業執照(三證合一)
北京