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• 產(chǎn)品描述： Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.

• 靶點(diǎn)： 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(nèi)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(xiàn)：
  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)

• 保存條件： -20℃

• 配置溶液濃度參考：
  

  	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

• 注意：部分產(chǎn)品我司僅能提供部分信息，我司不保證所提供信息的權(quán)威性，僅供客戶參考交流研究之用。

輸入產(chǎn)品批號(hào)：

本計(jì)算器可幫助您計(jì)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(guān)系，公式為：

質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *