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產品描述： Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV. |
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靶點：
MIP-1α-CCR5:3.3 nM (IC50, in HEK-293 cell membrane);MIP-1β-CCR5:7.2 nM (IC50, in HEK-293 cell membrane);RANTES-CCR5:5.2 nM (IC50, in HEK-293 cell membrane);HIV-1 (Ba-L):1.1 nM (IC50, in PM-1 cells);HIVProtease;?CCR |
體內研究：
Clearance values are moderate to high in both rat and dog species following i.v. administration (74 and 21 mL/min/kg, respectively). Maraviroc also has a moderate volume of distribution in both species (4.3 to 6.5 liters/kg). The half-life values of maraviroc are 0.9 h in the rat and 2.3 h in the dog. Following oral administration (2 mg/kg) to the dog, the Cmax(256 ng/mL) occurs 1.5 h. post-dose, and the bioavailability is 40%. For the rat, investigation of the concentrations obtain in the portal vein following oral administration indicated that approximately 30% of the administered dose is absorbed from the intestinal tract. In the DSS/TNBS colitis and in the transfer model, Maraviroc attenuates development of intestinal inflammation by selectively reducing the recruitment of CCR5 bearing leukocytes |
參考文獻：
1. Dorr P, et al. Maraviroc (UK-427,857), a potent, orally bioavailable, and selective small-molecule inhibitor of chemokine receptor CCR5 with broad-spectrum anti-human immunodeficiency virus type 1 activity. Antimicrob Agents Chemother. 2005 Nov;49(11):472 2. Mencarelli A, et al. Highly specific blockade of CCR5 inhibits leukocyte trafficking and reduces mucosal inflammation in murine colitis. Sci Rep. 2016 Aug 5;6:30802. 3. Romero-Sánchez MC, et al. Effect of maraviroc on HIV-disease progression-related biomarkers. Antimicrob Agents Chemother. 2012 Nov;56(11):5858-64. 4. Huilin Mou, et al. NRSF and CCR5 Established Neuron-glia Communication during Acute and Chronic Stresses. Journal of Drug Metabolism & Toxicology. January 10, 2016. |
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溶解性：
DMSO : 50 mg/mL (97.34 mM; Need ultrasonic) Ethanol : 6.5 mg/mL (12.65 mM; Need ultrasonic) |
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保存條件：
-20℃ |
配置溶液濃度參考：
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1mg |
5mg |
10mg |
| 1 mM |
1.947 ml |
9.734 ml |
19.468 ml |
| 5 mM |
0.389 ml |
1.947 ml |
3.894 ml |
| 10 mM |
0.195 ml |
0.973 ml |
1.947 ml |
| 50 mM |
0.039 ml |
0.195 ml |
0.389 ml |
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| 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