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网站主页 KRH-3955 HYDROCHLORIDE KRH-3955 hydrochloride
  • KRH-3955 hydrochloride|T39787|TargetMol

KRH-3955 hydrochloride|T39787|TargetMol

KRH-3955 hydrochloride
2253744-59-9
询价 1removed 起订
上海 更新日期：2026-05-08

TargetMol中国（陶术生物）

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联系人：邵小姐
手机：15002134094 拨打
邮箱：marketing@targetmol.cn

产品详情:

中文名称：
KRH-3955 hydrochloride
英文名称：
KRH-3955 hydrochloride
CAS号：
2253744-59-9
品牌：
TargetMol
产地：
美国
保存条件：
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
产品类别：
抑制剂
货号：
T39787

Product Introduction

Bioactivity

名称KRH-3955 hydrochloride
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.
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.
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year
关键字KRH-3955 Hydrochloride | KRH3955 hydrochloride | KRH 3955 Hydrochloride
相关产品Tenofovir | Valproic Acid | Chloroquine phosphate | (-)-Epigallocatechin Gallate | Emtricitabine | Dolutegravir intermediate-1 | Dextran sulfate sodium salt (MW 5000) | Lamivudine | 5-Fluorouracil | Decanedioic acid | Stavudine | Dimethyl fumarate
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KRH-3955 hydrochloride|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期 (14年)
注册资本 589.8595万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,工厂,试剂,定制,服务
主营行业 中间体,天然产物,生物化工,化学试剂,生物技术服务

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