现货,Vicriviroc Malate ,微生物学(Microbiology), CCR5 , CCR5 抑制剂,selleck,目录号S2004

信号转导通路: 微生物学(Microbiology) >> CCR5 >> CCR5 抑制剂 >> Vicriviroc Malatehttp://www.selleck.cn/vicriviroc-malate-S2004.html

技术数据:

分子量(MW): 667.72

化学式:

C28H38F3N5O2.C4H6O5

 

溶解度: DMSO ≥134mg/mL Water ≥38mg/mL Ethanol ≥134mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 541503-81-5

生物活性

 

 

In order to determine if vicriviroc malate is a receptor agonist or antagonist, three functional assays were employed to measure the ability of the compound to block b-chemokine signaling in CCR5-expressing cells.A chemotaxis assay was first employed to determine the ability of vicriviroc malate to inhibit chemokine-mediated migration of a mouse Ba/F3 cell line stably expressing recombinant human CCR5. In this assay, vicriviroc malate showed equally potent inhibition of the chemotactic response to MIP-1 with IC50 values below 1 nM. The ability of vicriviroc malate to inhibit intracellular calcium release induced by receptor stimulation was also assessed. A assay utilized to demonstrate the ability of vicriviroc malate to inhibit CCR5 receptor signaling was a GTPS exchange assay. GTPS binding induced by RANTES. vicriviroc malate potently inhibited RANTES-induced signaling with mean IC50s of 4.2 nM. [1] Vicriviroc Malate is highly water-soluble and demonstrates oral bioavailability of >89% in rats and monkeys. The compound is modestly human plasma protein-bound (≈84%) and widely distributed in the extra vascular space.Absorption and exposure in humans are linear and doseproportional, with a terminal phase half-life >24 hours supportive of once daily dosing. Variability in absorption is modest (20–40%). [2] Vicriviroc Malate is NOT A p-glycoprotein Substrate In Vitro. [3]

 

 

 

参考文献

Discovery and Characterization of Vicriviroc (SCH 417690), a CCR5 Antagonist with Potent Activity against Human Immunodeficiency Virus Type 1 Julie M. Strizki,Cecile Tremblay,et al. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY Dec. 2005;49:4911–4919

Vicriviroc Is a Novel, Potent CCR5 Inhibitor With Outstanding Pharmaceutic, Pharmacokinetic and PharmaCodynamic (PK/PD) Properties Lisa Dunkle, Anther Keung,et al. Retrovirology 2005;2(Suppl 1):S12

Vicriviroc, A Novel CCR5 Inhibitor, is NOT A p-glycoprotein Substrate In Vitro Cheng Li,Anther Keung,et al. Retrovirology 2005;2(Suppl 1):P158

 

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