Aprepitant

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Aprepitant

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Cat No: 14867

Biochemicals - Receptor Pharmacology

Aprepitant an antiemetic and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3 nM; IC50 = 0.09 nM for the human receptor).{24162,24160} It is selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3).{24162} In vivo, aprepitant (1 mg/kg) ...

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Territorial Availability: Available through Bertin Technologies only in France

Synonyms:

5-[[(2R,3S)-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)-4-morpholinyl]methyl]-1,2-dihydro-3H-1,2,4-triazol-3-one

Correlated keywords:

221350-96-5 MK 0869 MK0869 ONO7436 MK-0869 emesis antiemetic antagonists NK1 receptors stress responses chemotherapy-induced nausea vomiting vomit CINV substances P neurokinins neurokinin-1 GPCRs 1 one substance-P antiemetic anti-emetic anti emetic antiemetic antagonizes humans NKs hNKs in vivo clinical use prevents chemotherapy-induced chemotherapy induced L754030 L-754030 L 754030 L-754,030 L754,030 754,030 754,030 MK869 MKs 869 MK-869 ONOs 7436 ONO-7436 ONO7436 reflex NK1 inositol phosphates signals transduction pathway cancers neuroscience

Product Overview:
Aprepitant an antiemetic and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3 nM; IC50 = 0.09 nM for the human receptor).{24162,24160} It is selective for NK1 over NK3 receptors (Ki = 454.1 nM for human NK3).{24162} In vivo, aprepitant (1 mg/kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P (Item No. 24035).{24161} It also reduces NK1-agonist-induced foot tapping in gerbils. Formulations containing aprepitant have been used to prevent chemotherapy-induced nausea and vomiting.

Size	1 mg
Shipping	dry ice
CAS Number	170729-80-3
Molecular Formula	C₂₃H₂₁F₇N₄O₃
SMILES	C[C@@H](O[C@@H]1[C@H](C2=CC=C(F)C=C2)N(CC(NN3)=NC3=O)CCO1)C4=CC(C(F)(F)F)=CC(C(F)(F)F)=C4
Molecular Weight	534,4
Formulation	A crystalline solid
Purity	≥98%
Custom Code	2903.99
UNSPSC code	12352100

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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.