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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-KSI-6666
KSI-6666

Chemical Structure : KSI-6666

CAS No.: 1807873-14-8

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KSI-6666 ((RS)-KSI-6666, KSI 6666)

货号: PC-22735Not For Human Use, Lab Use Only.

KSI-6666 is a potent and selective competitive antagonist of sphingosine 1-phosphate receptor 1 (S1PR1, S1P1 receptor) with IC50 of 6.4 nM in GTP binding assay, and IC50 of 2.64 nM in in Ca2+ mobilization assays.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    KSI-6666 is a potent and selective competitive antagonist of sphingosine 1-phosphate receptor 1 (S1PR1, S1P1 receptor) with IC50 of 6.4 nM in GTP binding assay, and IC50 of 2.64 nM in in Ca2+ mobilization assays.
    KSI-6666 competitively inhibits the agonist-dependent Ca2+ mobilization of S1PR1, but not for other S1PRs. KSI-6666 inhibited mouse and rat S1PR1 with similar inhibitory activity as human S1PR1, demonstrating its cross-species efficacy.
    KSI-6666 functions as a potent competitive inhibitor of S1PR1 with less effect on cardiac and pulmonary functions.
    KSI-6666 is a potent anti-inflammatory agent in the mouse EAE model.
    KSI-6666 is an insurmountable antagonist with pseudoirreversible inhibitory activity, which is consistent with the hindered dissociation of KSI-6666 predicted by MetaD simulation, shows persistent efficacy.
    Residue Met124 of S1PR1 is critical for the pseudoirreversible inhibition by KSI-6666.

    物理化学性质&存储条件

    分子量 454.92
    分子式 C23H26ClF3N2O2
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO
    Chemical Name/SMILES

    1-(5-(1-((4-chloro-3-(trifluoromethyl)phenyl)(ethyl)amino)ethyl)-2-methylbenzyl)azetidine-3-carboxylic acid

    参考文献

    1. Maruyama Y, et al. Nat Commun. 2024 Jul 19;15(1):5743.

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