Chemical Structure : KRH-1636
CAS No.:
568526-77-2
KRH-1636
(KRH1636;KRH 1636)
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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551.695
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Formula
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C32H37N7O2
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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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N-((S)-5-guanidino-1-(((S)-1-(naphthalen-1-yl)ethyl)amino)-1-oxopentan-2-yl)-4-(((pyridin-2-ylmethyl)amino)methyl)benzamide
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References
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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