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KRH-3955 hydrochloride

KRH-3955 hydrochloride

产品编号 T39787   CAS 2253744-59-9

KRH-3955 hydrochloride is a CXCR4 antagonist with oral bioavailability. It effectively inhibits the binding of SDF-1α to CXCR4, exhibiting an IC 50 of 0.61 nM. Additionally, KRH-3955 hydrochloride displays high potency and selectivity as an inhibitor of X4 HIV-1, with an EC 50 ranging from 0.3 to 1.0 nM.

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KRH-3955 hydrochloride Chemical Structure
KRH-3955 hydrochloride, CAS 2253744-59-9
规格 价格/CNY 货期 数量
25 mg ¥ 10,600 6-8周
其他形式的 KRH-3955 hydrochloride:
产品目录号及名称: KRH-3955 hydrochloride (T39787)
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该分子属于定制产品。陶术拥有优秀的合成团队,经验和能力,可以为您提供高性价比的产品。但由于客观因素,研发中会存在小概率合成不成功的情况,还请理解,如您有任何问题,欢迎咨询,我们将竭诚为您服务。
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 KRH-3955 hydrochloride is a CXCR4 antagonist with oral bioavailability. It effectively inhibits the binding of SDF-1α to CXCR4, exhibiting an IC 50 of 0.61 nM. Additionally, KRH-3955 hydrochloride displays high potency and selectivity as an inhibitor of X4 HIV-1, with an EC 50 ranging from 0.3 to 1.0 nM.
靶点活性 SDF-1α-CXCR4:0.61 nM (IC50), X4 HIV-1 NL4-3:0.3-1.0 nM (EC50)
体外活性 KRH-3955 inhibits the replication of NL4-3 in activated peripheral blood mononuclear cells (PBMCs) from eight different donors with the EC 50 ranging from 0.23 to 1.3 nM[1]. KRH-3955 inhibits the infection of CD4/CXCR4 cells by these recombinant drug-resistant viruses, including viruses resistant to PIs, NRTIs, or NNRTIs, multidrug-resistant viruses and T20-resistant viruses, with the IC 50 ranging from 0.4 to 0.8 nM[1]. KRH-3955 (10-100 nM) inhibits the SDF-1α-induced increase in the intracellular Ca 2+ concentration in a dose-dependent manner[1]. KRH-3955 (0.1-1000 nM) binding sites are located in a region composed of all three extracellular loops (ECLs) of CXCR4[1]. KRH-3955 (10 nM) has a strong binding affinity for CXCR4 and a slow dissociation rate[1]. KRH-3955 inhibits MAb 12G5 binding to CXCR4 mutants, with the IC 50 ranging from 0.5 to 14.1 nM[1].
体内活性 KRH-3955 (10 mg/kg; a single p.o.) efficiently suppresses X4 HIV-1 infection in hu-PBL-SCID mice[1]. KRH-3955 (10 mg/kg; a single p.o.) exhibits moderate oral bioavailability (25.6%) and C max (86.3 ng/mL)[1]. KRH-3955 (10 mg/kg; a single i.v.) exhibits terminal elimination half-lives (99 h) due to high plasma clearance (3.9 liters/h/kg) combined with large volumes of distribution (374 liters/kg)[1]. Animal Model: C.B-17 SCID mice engrafted with human PBMCs and injected with infectious X4 HIV-1 (NL4-3)[1]Dosage: 10 mg/kg Administration: A single p.o. administration Result: Four of five mock-treated mice were infected whereas only one of five mice treated with KRH-3955 was infected. Animal Model: Male Sprague-Dawley rats[1]Dosage: 10 mg/kg (Pharmacokinetic Analysis) Administration: A single p.o. or i.v. administration Result: Well absorbed and the absolute oral bioavailability in rats was calculated to be 25.6%. The half time (T 1/2 ) of 99.0±13.1 h. Stable in human hepatic microsomes, and no significant inhibition of CYP450 liver enzymes by this compound was observed.
分子量 589.09
分子式 C28H48Cl3N7
CAS No. 2253744-59-9

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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参考文献

1. Tsutomu M, et, al. The Novel CXCR4 Antagonist KRH-3955 Is an Orally Bioavailable and Extremely Potent Inhibitor of Human Immunodeficiency Virus Type 1 Infection: Comparative Studies With AMD3100. Antimicrob Agents Chemother. 2009 Jul; 53(7): 2940-8.

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体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

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Keywords

KRH-3955 hydrochloride 2253744-59-9 KRH3955 hydrochloride KRH-3955 Hydrochloride KRH 3955 Hydrochloride KRH 3955 hydrochloride KRH3955 Hydrochloride Inhibitor inhibitor inhibit

 

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