KRH-1636

Names

[ Name ]:
KRH-1636

[Synonym ]:
Benzamide, N-[(1S)-4-[(diaminomethylene)amino]-1-[[[(1S)-1-(1-naphthalenyl)ethyl]amino]carbonyl]butyl]-4-[[(2-pyridinylmethyl)amino]methyl]-
N-[(2S)-5-[(Diaminomethylene)amino]-1-{[(1S)-1-(1-naphthyl)ethyl]amino}-1-oxo-2-pentanyl]-4-{[(2-pyridinylmethyl)amino]methyl}benzamide

Biological Activity

[Description]:

A potent, selective inhibitor of CXCR4 with IC50 of 13 nM, has no effect on CXCR1, CCR3, CCR4, or CCR5; 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; selectively blocks CXCR4-mediated Ca2+ signaling, blocks X4 HIV-1 replication in human PBL/SCID mice.

[References]

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. View Related Products by Target Chemokine Receptor (CCR and CXCR)

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Molecular Formula ]:
C₃₂H₃₇N₇O₂

[ Molecular Weight ]:
551.682

[ Exact Mass ]:
551.300903

[ LogP ]:
2.96

[ Index of Refraction ]:
1.643

Related Compounds

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