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首页-小分子抑制剂&激动剂-GPCR-Lysophospholipid Receptor-ASP1126
ASP1126

Chemical Structure : ASP1126

CAS No.: 1228580-11-7

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ASP1126 (ASP-1126)

货号: PC-49026Not For Human Use, Lab Use Only.

ASP1126 is a potent, selective and orally active sphingosine-1-phosphate (S1P) agonist with EC50 of 7.12 and 517 nM for hS1P1 and hS1P3 in GTPgS-binding assays, respectively.

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

    生物&药学活性

    ASP1126 is a potent, selective and orally active sphingosine-1-phosphate (S1P) agonist with EC50 of 7.12 and 517 nM for hS1P1 and hS1P3 in GTPgS-binding assays, respectively.
    ASP1126 selectively stimulated hS1P1 (EC50=13.4 uM) over hS1P3 (EC50=1760 nM) in Ca2+ influx assays.
    ASP1126 has similar selectivity and agonistic activity for rat S1P1.
    ASP1126 and tacrolimus synergistically prolong allograft survival in rats and monkeys.
    ASP1126 decreased the number of peripheral lymphocytes, repeated dosing showed a cumulative effect on lymphopenia in both rats and monkeys.
    ASP1126 reduced not only the number of naive T cells and central memory T cells but also effector memory T cells in the peripheral blood, and prolonged allograft survival in combination with tacrolimus in nonhuman primate (NHP) renal transplantation.

    物理化学性质&存储条件

    分子量 581.93
    分子式 C26H26ClF6NO5
    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

    4-Piperidinecarboxylic acid, 1-[[7-[[4-(2,2,2-trifluoroethoxy)-3-(trifluoromethyl)phenyl]methoxy]-2H-1-benzopyran-3-yl]methyl]-, hydrochloride (1:1)

    参考文献

    1. Akira Okimoto, et al. Transplant Proc. Jul-Aug 2019;51(6):2081-2098.

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