USBio Logo

259675 Aprepitant CAS: 170729-80-3

Specifications
References
CAS Number
170729-80-3
Grade
Highly Purified
Molecular Formula
C23H21F7N4O3
Molecular Weight
534.43
EU Commodity Code
38220090
Shipping Temp
RT
Storage Temp
4°C
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; Emend; L 754030; MK-869; ONO-7436

Aprepitant an antiemetic and antagonist of the neurokinin-1 (NK1) receptor (Ki = 3nM; IC50 = 0.09nM for the human receptor).It is selective for NK1 over NK3 receptors (Ki = 454.1nM for human NK3). In vivo, aprepitant (1mg/Kg) prevents plasma extravasation into the esophagus of guinea pigs induced by substance P. It also reduces NK1-agonist-induced foot tapping in gerbils. Formulations containing aprepitant have been used to prevent chemotherapy-induced nausea and vomiting.

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; Emend; L 754030; MK-869; ONO-7436
CAS Number
170729-80-3
Molecular Formula
C23H21F7N4O3
Molecular Weight
534.43
Appearance
White to off-white powder
Purity
≥98%
Identity (1H NMR)
Conforms to structure
Melting Point
As Reported
Storage and Stability
Store at RT. Stable for 6 months after receipt.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Toxicity and Hazards:  All products should be handled by qualified personnel only, trained in laboratory procedures.
Purity
≥98%
Form
White to off-white powder
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
References
1. Bissantz, C., Bohnert, C., Hoffmann, T., et al. Identification of a crucial amino acid in the helix position 6.51 of human tachykinin neurokinin 1 and 3 receptors contributing to the insurmountable mode of antagonism by dual NK1/NK3 antagonists. J. Med. Chem. 55(11), 5061-5076 (2012). 2. Finke, P.E., Meurer, L.C., Levorse, D.A., et al. Cyclopentane-based human NK1 antagonists. Part 1: Discovery and initial SAR. Bioorg. Med. Chem. Lett. 16(17), 4497-4503 (2006). 3. Meurer, L.C., Finke, P.E., Owens, K.A., et al. Cyclopentane-based human NK1 antagonists. Part 2: Development of potent, orally active, water-soluble derivatives. Bioorg. Med. Chem. Lett. 16(17), 4504-4511 (2006).
USBio References
No references available
Pricing
Order
Proceed to Checkout
Cart Summary
ProductSizeListYour PriceQtyExt Price
Subtotal:Subtotal:
Subtotal:Subtotal:
Total Coupon Savings:Total Coupon Savings:()
Your cart is currently empty.
- Coupon Code
Recently Viewed
  • Contact Us

    Visit our technical library or contact our support staff to answer your questions.

    Telephone:
    1-800-520-3011

    Library | Contact

    Distributors

    For customers outside of the United States, please use one of our many distributors.

    View Distributors

    Payment Methods

    We accept the following payment methods as well as pay-by-invoice.

    MasterCard Visa PayPal
    © 2023-2024 United States Biological - All Rights Reserved