1. GPCR/G Protein
    Immunology/Inflammation
    Anti-infection
  2. CXCR
    HIV
  3. KRH-3955 hydrochloride

KRH-3955 hydrochloride 

Cat. No.: HY-122058A
Handling Instructions

KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM.

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KRH-3955 hydrochloride Chemical Structure

KRH-3955 hydrochloride Chemical Structure

CAS No. : 2253744-59-9

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Description

KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM[1].

IC50 & Target[1]

SDF-1α-CXCR4

0.61 nM (IC50)

X4 HIV-1NL4-3

0.3-1.0 nM (EC50)

In Vitro

KRH-3955 inhibits the replication of NL4-3 in activated peripheral blood mononuclear cells (PBMCs) from eight different donors with the EC50 ranging from 0.23 to 1.3 nM[1].
KRH-3955 inhibits the infection of CD4/CXCR4 cells by these recombinant drug-resistant viruses, including viruses resistant to PIs, NRTIs, or NNRTIs, multidrug-resistant viruses and T20-resistant viruses, with the IC50 ranging from 0.4 to 0.8 nM[1].
KRH-3955 (10-100 nM) inhibits the SDF-1α-induced increase in the intracellular Ca2+ concentration in a dose-dependent manner[1].
KRH-3955 (0.1-1000 nM) binding sites are located in a region composed of all three extracellular loops (ECLs) of CXCR4[1].
KRH-3955 (10 nM) has a strong binding affinity for CXCR4 and a slow dissociation rate[1].
KRH-3955 inhibits MAb 12G5 binding to CXCR4 mutants, with the IC50 ranging from 0.5 to 14.1 nM[1].

In Vivo

KRH-3955 (10 mg/kg; a single p.o.) efficiently suppresses X4 HIV-1 infection in hu-PBL-SCID mice[1].
KRH-3955 (10 mg/kg; a single p.o.) exhibits moderate oral bioavailability (25.6%) and Cmax (86.3 ng/mL)[1].
KRH-3955 (10 mg/kg; a single i.v.) exhibits terminal elimination half-lives (99 h) due to high plasma clearance (3.9 liters/h/kg) combined with large volumes of distribution (374 liters/kg)[1].

Animal Model: C.B-17 SCID mice engrafted with human PBMCs and injected with infectious X4 HIV-1 (NL4-3)[1]
Dosage: 10 mg/kg
Administration: A single p.o. administration
Result: Four of five mock-treated mice were infected whereas only one of five mice treated with KRH-3955 was infected.
Animal Model: Male Sprague-Dawley rats[1]
Dosage: 10 mg/kg (Pharmacokinetic Analysis)
Administration: A single p.o. or i.v. administration
Result: Well absorbed and the absolute oral bioavailability in rats was calculated to be 25.6%.
The half time (T1/2) of 99.0±13.1 h.
Stable in human hepatic microsomes, and no significant inhibition of CYP450 liver enzymes by this compound was observed.
Molecular Weight

589.09

Formula

C₂₈H₄₈Cl₃N₇

CAS No.

2253744-59-9

SMILES

CCCN(CCC)CCCCN(CC1=CC=C(CN(CC2=NC=CN2)CC3=NC=CN3C)C=C1)C.[H]Cl.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

KRH-3955KRH3955KRH 3955CXCRHIVCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virusCXCR4X4HIV-1orallybioavailableInhibitorinhibitorinhibit

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