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  • Maraviroc

    • 马拉维若;马拉韦罗, UK-427857
    货号: abs810489
    CAS号: 376348-65-1
    分子式: C29H41F2N5O
    分子量: 513.67
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    货号-规格 货期 价格 数量
    abs810489-5mg 现货 ¥560.00
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    abs810489-10mg 现货 ¥1043.00
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    abs810489-50mg 现货 ¥3277.00
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    abs810489-100mg 现货 ¥6400.00
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    大包装询价
    产品描述
    描述

    Maraviroc (Selzentry, UK-427857, Celsentri) 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.

    纯度
    >98%
    储存/保存方法
    Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.
    基本信息
    别名
    马拉维若;马拉韦罗; UK-427857
    外观
    White powder
    可溶性/溶解性
    DMSO : 50 mg/mL (97.34 mM; Need ultrasonic)
    Ethanol : 6.5 mg/mL (12.65 mM; Need ultrasonic)
    生物活性
    靶点
    CCR5;MIP-1α;RANTES;MIP-1β
    In vitro(体外研究)
    Maraviroc inhibits MIP-1β-stimulated γ-S-GTP binding to HEK-293 cell membranes, indicating its ability to inhibit chemokine-dependent stimulation of GDP-GTP exchange at the CCR5/G protein complex. Maraviroc also 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. In the same experiments, Maraviroc does not trigger release of intracellular calcium at concentrations up to 10 μM, indicating that it is devoid of CCR5 agonist activity. Consistent with this, Maraviroc fails to induce CCR5 internalization. Maraviroc is active at low nanomolar concentrations against HIV-1 Ba-L. Maraviroc inhibits all 200 pseudotyped viruses with a geometric mean IC90 of 13.7 nM. At concentrations >1000 times the 50% inhibitory concentration, maraviroc did not inhibit other chemokine receptors (CCR1, 2, 3, 4, 7, and 8; CXCR1 and 2) to a clinically relevant degree.
    In vivo(体内研究)
    The half-life values of Maraviroc are 0.9 hour in the rat and 2.3 hours in the dog. Following oral administration (2 mg/kg) to the dog, the Cmax (256 ng/ml) occurred 1.5 hours post-dose, and the bioavailability is 40%. For the rat, approximately 30% of the administered dose is absorbed from the intestinal tract. Female RAG-hu mice are challenged vaginally with HIV-1 an hour after intravaginal application of the Maraviroc gel. Maraviroc gel treated mice are fully protected against vaginal HIV-1 challenge in contrast to placebo gel treated mice which all became infected. Vaginal administration of Maraviroc fully protects mice against HIV-1 vaginal challenge. While there is a clear pattern of CD4 T cell decline in placebo-gel treated and viral challenged mice, their levels are stable in mice receiving Maraviroc gel.
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    • 实验方法 实验条件
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