Maraviroc

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Maraviroc 是 MIP-1α、MIP-1β 和 RANTES 的 CCR5 拮抗剂，IC50 分别为 3.3 nM、7.2 nM 和 5.2 nM。

Maraviroc is a CCR5 antagonist for MIP-1α, MIP-1β and RANTES with IC50 of 3.3 nM, 7.2 nM and 5.2 nM, respectively.(In Vitro):Maraviroc (UK-427857) is a selective CCR5 antagonist with potent anti-human immunodeficiency virus type 1 (HIV-1) activity. Maraviroc inhibits the downstream event of chemokine-induced intracellular calcium redistribution, with IC50s ranging from 7 to 30 nM obtained against MIP-1β, MIP-1α and RANTES.Maraviroc (UK-427857) is active (IC90) at low nanomolar concentrations against HIV-1 Ba-L (a lab-adapted R5 strain) when measured in a 5-day antiviral assay using either isolated multiple (pooled) donor PBMC (IC90, 3.1 nM), single-donor PBMC (IC90, 1.8 nM) or PM-1 cells (IC90, 1.1 nM)(In Vivo):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.

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Celsentri | Selzentry | UK 427857

Autophagy

CCR

MIP-1α| MIP-1β| RANTES

Inflammation/Immunology

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376348-65-1

513.67

C29H41F2N5O

>98% (HPLC)

Ethanol: 100 mg/mL (194.67 mM); DMSO: 100 mg/mL (194.67 mM)

CC1=NN=C(N1C2CC3CCC(C2)N3CCC(C4=CC=CC=C4)NC(=O)C5CCC(CC5)(F)F)C(C)C

4,4-difluoro-N-[(1S)-3-[(1S,5R)-3-(3-methyl-5-propan-2-yl-1,2,4-triazol-4-yl)-8-azabicyclo[3.2.1]octan-8-yl]-1-phenylpropyl]cyclohexane-1-carboxamide

(-20℃)

With Ice Pack

≥ 2 years