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

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

KRH-3955 hydrochloride Chemical Structure

CAS No. : 2253744-59-9

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Based on 1 publication(s) in Google Scholar

Other Forms of KRH-3955 hydrochloride:

KRH-3955 hydrochloride Related Antibodies

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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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

KRH-3955 hydrochloride Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Appearance

Solid

Color

White to light yellow

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

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation
References
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KRH-3955 hydrochloride Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

KRH-39552253744-59-9KRH3955KRH 3955CXCRHIVCXC chemokine receptorsC-X-C motif chemokine receptorsHuman immunodeficiency virusCXCR4X4HIV-1orallybioavailableInhibitorinhibitorinhibit

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