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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-KRH-1636
KRH-1636

Chemical Structure : KRH-1636

CAS No.: 568526-77-2

KRH-1636 (KRH1636;KRH 1636)

货号: PC-61292Not For Human Use, Lab Use Only.

KRH-1636 (KRH1636) is a potent, selective inhibitor of CXCR4 with IC50 of 13 nM, has no effect on CXCR1, CCR3, CCR4, or CCR5.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

KRH-1636 (KRH1636) is a potent, selective inhibitor of CXCR4 with IC50 of 13 nM, has no effect on CXCR1, CCR3, CCR4, or CCR5.
KRH-1636 completely inhibits X4 HIV-1 (IIIB strain) replication in MT-4 cells with EC50 of 19.3 nM and EC90 of 47.8 nM, without cytotoxic concentration (CC50>400 uM), also has effectivity against HTLV-IIIB and three clinical isolates in PBMCs including YU-6 (EC50=46 nM), but not R5 HIV-1, YU-1, YU-2.
KRH-1636 selectively blocks CXCR4-mediated Ca2+ signaling, blocks X4 HIV-1 replication in human PBL/SCID mice.

物理化学性质&存储条件

分子量 551.695
分子式 C32H37N7O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-((S)-5-guanidino-1-(((S)-1-(naphthalen-1-yl)ethyl)amino)-1-oxopentan-2-yl)-4-(((pyridin-2-ylmethyl)amino)methyl)benzamide

参考文献

1. Ichiyama K, et al. Proc Natl Acad Sci U S A. 2003 Apr 1;100(7):4185-90.

2. Murakami T, et al. Antimicrob Agents Chemother. 2009 Jul;53(7):2940-8.

3. Zachariassen ZG, et al. J Med Chem. 2015 Oct 22;58(20):8141-53.

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