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KRH-3955 hydrochloride

CAS No. : 2253744-59-9

MCE 站：KRH-3955 hydrochloride

产品活性：KRH-3955 hydrochloride 是一种具有口服活性的 CXCR4 拮抗剂。KRH-3955 hydrochloride 抑制 SDF-1α 与 CXCR4 的结合，IC₅₀ 为0.61 nM。KRH-3955 hydrochloride 也是高效的、选择性的 X4 HIV-1 抑制剂，EC₅₀ 为 0.3 至 1.0 nM。

研究领域：GPCR/G Protein  |  Immunology/Inflammation  |  Anti-infection

作用靶点：CXCR  |  HIV

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.
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.
KRH-3955 (10-100 nM) inhibits the SDF-1α-induced increase in the intracellular Ca²⁺ concentration in a dose-dependent manner.
KRH-3955 (0.1-1000 nM) binding sites are located in a region composed of all three extracellular loops (ECLs) of CXCR4.
KRH-3955 (10 nM) has a strong binding affinity for CXCR4 and a slow dissociation rate.
KRH-3955 inhibits MAb 12G5 binding to CXCR4 mutants, with the IC₅₀ ranging from 0.5 to 14.1 nM.

In Vivo: KRH-3955 (10 mg/kg; a single p.o.) efficiently suppresses X4 HIV-1 infection in hu-PBL-SCID mice.
KRH-3955 (10 mg/kg; a single p.o.) exhibits moderate oral bioavailability (25.6%) and C_max (86.3 ng/mL).
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).

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