ML-221

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ML-221

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Cat No: 27313

Biochemicals - Receptor Pharmacology

ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 μM).{48358} 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-ar...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

5-[(4-nitrobenzoyl)oxy]-2-[(2-pyrimidinylthio)methyl]-4H-pyran-4-one

Correlated keywords:

ML221 AT 1 MzCHA1 ChA1

Product Overview:
ML-221 is an antagonist of the G protein-coupled receptor (GPCR) APJ (IC50 = 4.8 μM).{48358} 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.{48359} 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.{48360} ML-221 also inhibits pathological angiogenesis and enhances normal vessel recovery in retinal ischemic regions in a mouse model of oxygen-induced retinopathy.{48361}

Size	5 mg
Shipping	dry ice
CAS Number	877636-42-5
Molecular Formula	C₁₇H₁₁N₃O₆S
SMILES	O=C1C(OC(C2=CC=C([N+]([O-])=O)C=C2)=O)=COC(CSC3=NC=CC=N3)=C1
Molecular Weight	385,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2933.59
UNSPSC code	12352100

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MSDS

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Cayman Chemical's mission is to help make research possible by supplying scientists worldwide with the basic research tools necessary for advancing human and animal health. Our utmost commitment to healthcare researchers is to offer the highest quality products with an affordable pricing policy.

Our scientists are experts in the synthesis, purification, and characterization of biochemicals ranging from small drug-like heterocycles to complex biolipids, fatty acids, and many others. We are also highly skilled in all aspects of assay and antibody development, protein expression, crystallization, and structure determination.

Over the past thirty years, Cayman developed a deep knowledge base in lipid biochemistry, including research involving the arachidonic acid cascade, inositol phosphates, and cannabinoids. This knowledge enabled the production of reagents of exceptional quality for cancer, oxidative injury, epigenetics, neuroscience, inflammation, metabolism, and many additional lines of research.

Our organic and analytical chemists specialize in the rapid development of manufacturing processes and analytical methods to carry out clinical and commercial GMP-API production. Pre-clinical drug discovery efforts are currently underway in the areas of bone restoration and repair, muscular dystrophy, oncology, and inflammation. A separate group of Ph.D.-level scientists are dedicated to offering Hit-to-Lead Discovery and Profiling Services for epigenetic targets. Our knowledgeable chemists can be contracted to perform complete sample analysis for analytes measured by the majority of our assays. We also offer a wide range of analytical services using LC-MS/MS, HPLC, GC, and many other techniques.

Accreditations
ISO/IEC 17025:2005
ISO Guide 34:2009

Cayman is a leader in the field of emerging drugs of abuse, providing high-purity Schedule I-V Controlled Substances to federally-licensed laboratories and qualified academic research institutions for forensic analyses. We are certified by ACLASS Accreditation Services with dual accreditation to ISO/IEC 17025:2005 and ISO Guide 34:2009.