An NK1 receptor antagonist
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Orvepitant (maleate)

Item No. 43077

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2R,4S)-N-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethyl]-2-(4-fluoro-2-methylphenyl)-4-[(8aS)-hexahydro-6-oxopyrrolo[1,2-a]pyrazin-2(1H)-yl]-N-methyl-1-piperidinecarboxamide, (2Z)-2-butenedioate
CAS Number
579475-24-4
Synonyms
  • GW 823296B
Molecular Formula
C31H35F7N4O2 • C4H4O4
Formula Weight
744.7
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlChloroform: Slightly Soluble: 0.1-1 mg/ml
SMILES
O=C(O)/C=C\C(O)=O.C[C@H](C1=CC(C(F)(F)F)=CC(C(F)(F)F)=C1)N(C)C(N2[C@@H](C3=C(C=C(C=C3)F)C)C[C@@H](N4C[C@@]5([H])N(C(CC5)=O)CC4)CC2)=O
InChi Code
InChI=1S/C31H35F7N4O2.C4H4O4/c1-18-12-23(32)4-6-26(18)27-16-24(40-10-11-41-25(17-40)5-7-28(41)43)8-9-42(27)29(44)39(3)19(2)20-13-21(30(33,34)35)15-22(14-20)31(36,37)38;5-3(6)1-2-4(7)8/h4,6,12-15,19,24-25,27H,5,7-11,16-17H2,1-3H3;1-2H,(H,5,6)(H,7,8)/b;2-1-/t19-,24+,25+,27-;/m1./s1
InChi Key
IPACOHTZCSBGBV-WUXDIRCFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

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    1 mg

    $72

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    5 mg

    $323

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    10 mg

    $466

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    Product Description

    Orvepitant is a neurokinin-1 (NK1) receptor antagonist (Ki = 0.06 nM for the human receptor).1 It is selective for the NK1 receptor over a panel of 67 transporters, ion channels, and enzymes at 10 µM. Orvepitant inhibits substance P-induced calcium release in CHO cells expressing the recombinant human NK1 receptor (apparent pKB = 10.3). It inhibits GR73632-induced foot tapping in gerbils with half-maximal inhibitory dose (ID50) values of 0.11, 0.09, 0.09, and 3.36 mg/kg when administered 1, 4, 8, or 24 hours prior to GR73632, respectively. Orvepitant also inhibits GR73632-induced hindlimb scratching in gerbils.2 It reduces the number of territorial postures in the human threat test in marmosets, indicating anxiolytic-like activity, when administered at doses of 1, 3, and 10 mg/kg.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Di Fabio, R., Alvaro, G., Braggio, S., et al. Identification, biological characterization and pharmacophoric analysis of a new potent and selective NK1 receptor antagonist clinical candidate. Bioorg. Med. Chem. 21(21), 6264-6273 (2013).

    2. Trower, M.K., Fisher, A., Upton, N., et al. Neurokinin-1 receptor antagonist orvepitant is an effective inhibitor of itch-associated response in a Mongolian gerbil model of scratching behaviour. Exp. Dermatol. 23(11), 858-860 (2014).