877636-42-5 Usage
Description
ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 μM). It is selective for APJ over the angiotensin II type 1 (AT1) receptor (IC50 = >78 μM). ML-221 antagonizes apelin 13-induced activation of APJ in cAMP and β-arrestin recruitment assays (IC50s = 0.7 and 1.75 μM, respectively). It inhibits proliferation and angiogenesis in Mz-ChA-1 cholangiocarcinoma cells when used at concentrations ranging from 5 to 15 μM. In vivo, ML-221 (150 μg/kg) reduces tumor growth in a Mz-ChA-1 mouse xenograft model. Intrathecal injection of ML-221 (10 μg per animal) reduces mechanical allodynia and heat hyperalgesia induced by chronic constriction injury (CCI) of the sciatic nerve in rats. ML-221 also inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy.
Uses
ML 221 is a functional antagonist of the apelin (APJ) receptor which is shown to treat or mediate the homeostasis of the cardiovascular system.
Check Digit Verification of cas no
The CAS Registry Mumber 877636-42-5 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 8,7,7,6,3 and 6 respectively; the second part has 2 digits, 4 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 877636-42:
(8*8)+(7*7)+(6*7)+(5*6)+(4*3)+(3*6)+(2*4)+(1*2)=225
225 % 10 = 5
So 877636-42-5 is a valid CAS Registry Number.
877636-42-5Relevant articles and documents
SMALL MOLECULE ANTAGONISTS OF THE APELIN RECEPTOR FOR THE TREATMENT OF DISEASE
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, (2014/02/15)
The present disclosure relates to compounds and methods for treating a disease mediated by apelin.