A nonpeptide NK1 receptor antagonist
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CP 99,994 (hydrochloride)

Item No. 27669

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2S,3S)-N-[(2-methoxyphenyl)methyl]-2-phenyl-3-piperidinamine, dihydrochloride
CAS Number
145148-39-6
Molecular Formula
C19H24N2O • 2HCl
Formula Weight
369.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: 50 mMMethanol: SolubleWater: 100 mM
SMILES
COC1=C(C=CC=C1)CN[C@H]2CCCN[C@H]2C3=CC=CC=C3.Cl.Cl
InChi Code
InChI=1S/C19H24N2O.2ClH/c1-22-18-12-6-5-10-16(18)14-21-17-11-7-13-20-19(17)15-8-3-2-4-9-15;;/h2-6,8-10,12,17,19-21H,7,11,13-14H2,1H3;2*1H/t17-,19-;;/m0../s1
InChi Key
WNHRFWPLRATIDT-FFUVTKDNSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $268

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    Product Description

    CP 99,994 is a nonpeptide neurokinin-1 (NK1) receptor antagonist (Ki = 0.25 nM in a radioligand binding assay).1 It is selective for NK1 over NK2 and NK3 receptors (Kis = >10 μM for both) as well as dopamine D1 and D2, α1-, α2- and β-adrenergic, serotonin, histamine H1, muscarinic and nicotinic acetylcholine, μ-opioid, glutamate, benzodiazepine, and γ-aminobutyric acid (GABA) receptors (IC50s = >1 μM for all). In vitro, CP 99,994 inhibits excitation of guinea pig locus coeruleus cells induced by substance P (Item No. 24035; IC50 = 25 nM). It inhibits increases in horizontal locomotor activity induced by the NK1 agonist [Sar9,Met(O2)11]-substance P in guinea pigs (ID50 = 0.59 mg/kg). CP 99,994 inhibits aerosolized capsaicin-induced plasma extravasation in guinea pig lung (ID50 = 4 mg/kg). It exhibits anti-emetic effects in ferret models of emesis induced by copper sulfate, loperamide, or cisplatin (Item No. 13119) when administered at doses of 0.3 and 1 mg/kg.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. McLean, S., Ganong, A., Seymour, P.A., et al. Pharmacology of CP-99,994; a nonpeptide antagonist of the tachykinin neurokinin-1 receptor. J. Pharmacol. Exp. Ther. 267(1), 472-479 (1993).

    2. Watson, J.W., Gonsalves, S.F., Fossa, A.A., et al. The anti-emetic effects of CP-99,994 in the ferret and the dog: Role of the NK1 receptor. Br. J. Pharmacol. 115(1), 84-94 (1995).