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首页-小分子抑制剂&激动剂-GPCR-Chemokine Receptor (CCR and CXCR)-KRH-3955
KRH-3955

Chemical Structure : KRH-3955

CAS No.: 1097732-62-1

KRH-3955 (KRH 3955;KRH3955)

货号: PC-61294Not For Human Use, Lab Use Only.

KRH-3955 is a potent, selective, orally bioavailable inhibitor of CXCR4 that efficiently inhibits SDF-1α binding to CXCR4 with IC50 of 0.61 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

KRH-3955 is a potent, selective, orally bioavailable inhibitor of CXCR4 that efficiently inhibits SDF-1α binding to CXCR4 with IC50 of 0.61 nM.
KRH-3955 inhibits the replication of both X4 and R5X4 HIV-1 in activated PBMCs with EC50 of 0.3 to 1.0 nM but does not affect R5 HIV-1 replication.
KRH-3955 also inhibits the replication of clinical isolates of X4 HIV-1 (92HT599) and R5X4 HIV-1 (92HT593) (EC50=4.0-4.2 nM) in activated PBMCs.
KRH-3955 exhibits inhibition of Ca2+ signaling through CXCR4, blocks X4 HIV-1 replication in human PBL/SCID mice.

物理化学性质&存储条件

分子量 929.975
分子式 C40H63N7O18
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

N1-(4-((((1H-imidazol-2-yl)methyl)((1-methyl-1H-imidazol-2-yl)methyl)amino)methyl)benzyl)-N1-methyl-N4,N4-dipropylbutane-1,4-diamine, (2R,3R)-2,3-dihydroxybutanedioate (1:3)

参考文献

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

2. Iwasaki Y, et al. Cancer Sci. 2009 Apr;100(4):778-81.

3. Nakasone T, et al. Med Microbiol Immunol. 2013 Apr;202(2):175-82.

4. Hikichi Y, et al. J Gen Virol. 2016 Sep;97(9):2427-40.

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