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首页-小分子抑制剂&激动剂-GPCR-Formyl peptide receptor (FPR)-FPR agonist Compound 17b
FPR agonist Compound 17b

Chemical Structure : FPR agonist Compound 17b

CAS No.: 1184304-45-7

FPR agonist Compound 17b (FPR agonist Cmpd17b, Compound 17b)

货号: PC-72085Not For Human Use, Lab Use Only.

FPR agonist Compound 17b is a small-molecule FPR1/FPR2 agonist withEC50 of 3.2 uM (hFPR1 Ca2+ mobilization), lack of functional responses at FPR3.

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

    生物&药学活性

    FPR agonist Compound 17b is a small-molecule FPR1/FPR2 agonist withEC50 of 3.2 uM (hFPR1 Ca2+ mobilization), lack of functional responses at FPR3.
    FPR agonist Compound 17b is a biased agonist at FPR2, ∼30-fold biased away from Cai2+ at both FPR1 and FPR2.
    FPR agonist Compound 17b stimulated a concentration-dependent phosphorylation of key cardiomyocyte survival pathways ERK1/2, Akt1/2/3(Thr308) and Akt1/2/3(Ser474), and an increase in Cai2+, inhibited forskolin-stimulated cAMP accumulation in hFPR1-CHO and hFPR2-CHO cells, consistent with FPR1/2 coupling to Gi/o proteins and inhibiting adenylate cyclase.
    FPR agonist Compound 17b demonstrated protective actions against cardiomyocyte injury responses in vitro.
    FPR agonist Cmpd17b reduces cardiac necrosis 24h post I–R injury in vivo, reduces systemic inflammation, and limits cardiac remodelling and dysfunction in vivo.

    物理化学性质&存储条件

    分子量 456.34
    分子式 C22H22BrN3O3
    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

    N-(4-Bromophenyl)-2-[5-(3-methoxybenzyl)-3-methyl-6-oxo-6H-pyridazin-1-yl]-propionamide

    参考文献

    1. Cheng Xue Qin, et al. Nat Commun. 2017 Feb 7;8:14232.

    2. Agostino Cilibrizzi, et al. J Med Chem. 2009 Aug 27;52(16):5044-57.

    3. Sarah A Marshall, et al. Int J Mol Sci. 2020 Feb 18;21(4):1384.

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