S81468 |
Maraviroc |
| MedMol | 99% |
- 提示：详情请下载说明书。
- 产品描述： Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.
- 靶点： 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)
- 体内研究： 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
- 参考文献：
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.
- 溶解性： DMSO : 50 mg/mL (97.34 mM; Need ultrasonic) Ethanol : 6.5 mg/mL (12.65 mM; Need ultrasonic)
- 保存条件： -20℃
- 配置溶液浓度参考：
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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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
