貨號	規(guī)格	價格	上海	北京	武漢	南京
S81468-5mg	99.4%	￥125.00 S81468-5mg ￥125.00 現(xiàn)貨	3 3	-	-	-
S81468-10mg	99.4%	￥238.00 S81468-10mg ￥238.00 現(xiàn)貨	7 7	-	-	-
S81468-25mg	99.4%	￥430.00 S81468-25mg ￥430.00 現(xiàn)貨	9 9	-	-	-
S81468-50mg	99.4%	￥731.00 S81468-50mg ￥731.00 現(xiàn)貨	6 6	-	-	-
S81468-100mg	≥99%	￥1020.00 S81468-100mg ￥1020.00 2-3天	0 貨期：2-3天	-	-	-
S81468-200mg	≥99%	￥1955.00 S81468-200mg ￥1955.00 2-3天	0 貨期：2-3天	-	-	-

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產(chǎn)品介紹

Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.

產(chǎn)品描述：

Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.

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(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：

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。

參考文獻

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