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Aprepitant

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    Aprepitant
  • Aprepitant
Cat No: 14867
Chemicals - Miscellaneous Chemicals
Cayman
€86.00
Price is excluding VAT and does not include packaging neither shipping

An antiemetic compound that selectively antagonizes the human NK1 receptor (Kis = 3 and 454.1 nM for hNK1 and hNK3, respectively; IC50 = 0.09 nM for hNK1)
Substance P, a neurokinin peptide found in the brain and gastrointestinal tract, is thought to mo...

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Territorial Availability: Available through Bertin Pharma only in Europe
Product Overview:
An antiemetic compound that selectively antagonizes the human NK1 receptor (Kis = 3 and 454.1 nM for hNK1 and hNK3, respectively; IC50 = 0.09 nM for hNK1)
Substance P, a neurokinin peptide found in the brain and gastrointestinal tract, is thought to modulate stress responses, including the emetic reflex. Its actions are mediated through the neurokinin-1 (NK1) receptor, one of three GPCRs that couple neurokinin binding to the inositol phosphate signal transduction pathway. Aprepitant is an anti-emetic compound that selectively antagonizes the human NK1 receptor (Kis = 3 and 454.1 nM for hNK1 and hNK3, respectively; IC50 = 0.09 nM for hNK1). In in vivo assays to measure peripheral (guinea pig SYVAL assay) and central (gerbil foot-tapping stress response assay) inhibition of NK1 receptors, aprepitant demonstrates ED50 values of 0.008 and 0.36 mg/kg, respectively. Through antagonism of NK1 receptor activity, aprepitant has found clinical use to prevent chemotherapy-induced nausea and vomiting.
Size: 1 mg
Shipping: wet ice
Stability: Store at -20 degrees; shelf life 730 days maximum after production
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: 2903990002
UNSPSC code: 12352100

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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.

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