Chemical Structure : KRH-3955
CAS No.:
1097732-62-1
KRH-3955
(KRH 3955;KRH3955)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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929.975
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Formula
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C40H63N7O18
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20 °C 12 Months; 4°C 6 Months
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- In Solvent
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-80 °C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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)
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References
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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