| Aprepitant |
| 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 |
| (CAS 170729-80-3) |
 |
| Description： |
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. 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. |
| Product No. |
KT00560 |
| Product Name |
Aprepitant |
| Synonyms |
MK-0869; MK-869; L-754030; Emend |
| Formal Name |
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 |
| CAS Number |
170729-80-3 |
| Molecular Formula |
C23H21F7N4O3 |
| Formula Weight |
534.4 |
| Formulation |
A crystalline solid |
| Purity |
98%min |
| Stability |
2 years |
| Storage |
-20°C |
| Shipping |
USD45 for Europe and USA. No shipping charge once amount reach USD500 |
| Quality Control |
HNMR,CNMR,LCMS,HPLC,IR,etc. |
| Price & Availability |
In Stock. Price Negotiated. |
|
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