An NK1 receptor antagonist
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Befetupitant

Item No. 43004

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N,α,α-trimethyl-N-[4-(2-methylphenyl)-6-(4-morpholinyl)-3-pyridinyl]-3,5-bis(trifluoromethyl)-benzeneacetamide
CAS Number
290296-68-3
Synonyms
  • Ro 67-5930
Molecular Formula
C29H29F6N3O2
Formula Weight
565.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CC(C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)(C(N(C(C(C2=C(C=CC=C2)C)=C3)=CN=C3N4CCOCC4)C)=O)C
InChi Code
InChI=1S/C29H29F6N3O2/c1-18-7-5-6-8-22(18)23-16-25(38-9-11-40-12-10-38)36-17-24(23)37(4)26(39)27(2,3)19-13-20(28(30,31)32)15-21(14-19)29(33,34)35/h5-8,13-17H,9-12H2,1-4H3
InChi Key
ZGNPLCMMVKCTHM-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $523

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    1 mg

    $994

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    5 mg

    $2,090

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    Product Description

    Befetupitant is a neurokinin-1 (NK1) receptor antagonist (Ki = 1 nM).1 It inhibits GR73632-induced foot tapping in gerbils (ID50 = 0.2 mg/kg). Topical administration of befetupitant (0.4 or 1.6 mg/ml for four days) decreases hemangiogenesis and lymphangiogenesis but induces corneal opacity, stromal leukocyte infiltration, and corneal toxicity in a mouse model of corneal alkali burn.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hoffmann, T., Bös, M., Stadler, H., et al. Design and synthesis of a novel, achiral class of highly potent and selective, orally active neurokinin-1 receptor antagonists. Bioorg. Med. Chem. Lett. 16(5), 1362-1365 (2006).

    2. Bignami, F., Giacomini, C., Lorusso, A., et al. NK1 receptor antagonists as a new treatment for corneal neovascularization. Invest. Ophthalmol. Vis. Sci. 55(10), 6783-6794 (2014).