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  • ML221
    • ML 221;ML-221
    货号: abs814586
    CAS号: 877636-42-5
    分子式: C17H11N3O6S
    分子量: 385.35
    产品说明书
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    货号-规格 货期 价格 数量
    abs814586-10mg 1-2周 ¥882.00
    - +
    abs814586-50mg 1-2周 ¥3308.00
    - +
    大包装询价
    产品描述
    描述

    ML221 is a potent apelin receptor (APJ) functional antagonist in cell-based assays that is >37-fold selective over the closely related angiotensin II type 1 (AT1) receptor. The IC50 values of ML221 are 0.70 and 1.75 μM in a cAMP assay and β-arrestin assay, respectively. 

    纯度
    >98%
    储存/保存方法
    Store at -20°C
    基本信息
    别名
    ML 221;ML-221
    外观
    powder
    可溶性/溶解性
    DMSO :9 mg/mL (23.36 mM)
    生物活性
    靶点
    apelin receptor
    In vitro(体外研究)
    In a PAMPA permeability assay, ML221 exhibits moderate permeability. ML221 displays moderate plasma and poor microsomal stability, as it is rapidly metabolized in both human and mouse liver homogenates (4.2% and 4.9% remaining at 60 min). It shows no toxicity (>50 μM) toward human hepatocytes. ML221 displays limited cross reactivity against a range of GPCRs. ML221 inhibits endothelial cell proliferation by blocking apelin-APJ signaling without affecting the expression of VEGF and VEGFR2.
    In vivo(体内研究)
    Intraperitoneal administration of ML221 inhibits pathological angiogenesis but enhances the recovery of normal vessels into the ischemic regions in the retina of the OIR model mice. A single application of ML221 alleviates mechanical allodynia and heat hyperalgesia 7 days following chronic constriction injury (CCI), in a dose‑dependent manner. Intraspinal delivery of ML221, at the onset of and in fully‑established neuropathic pain, persistently attenuates CCI‑induced pain hypersensitivity, indicating that the apelin‑APJ system is involved in initiating and maintaining pain. Intrathecal ML221 downregulates phosphorylated extracellular signal‑related kinase (ERK) in the rat spinal cord dorsal horn, suggesting that the effect of apelin on neuropathic pain may be mediated via ERK signaling.
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