ML221|>98%|abs814586-爱必信(上海)生物科技有限公司

ML221

参考价：¥840

供货周期：

一周

品牌：

爱必信

规格：

>98%

货号：

abs814586

CAS号：

877636-42-5

产品详情

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抑制剂描述：

产品名称：ML221

产品别名：见爱必信官网

英文别名：ML221

靶点：Apelin Receptor

CAS：877636-42-5

纯度：>98%

外观：见爱必信官网

保存方法：Store at -20°C

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.

溶解性：DMSO ：9 mg/mL (23.36 mM)

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.

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.

产品信息订购：

产品货号	产品名称	规格	价格	大包装及货期
abs814586	ML221	10mg	840.00	立即咨询
abs814586	ML221	50mg	3150.00	立即咨询

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