An NK3 receptor antagonist
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SB-218795

Item No. 42373

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
aR-[[(2-phenyl-4-quinolinyl)carbonyl]amino]-benzeneacetic acid, methyl ester
CAS Number
174635-53-1
Molecular Formula
C25H20N2O3
Formula Weight
396.4
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Sparingly Soluble: 1-10 mg/ml
SMILES
O=C(C1=CC(C2=CC=CC=C2)=NC3=C1C=CC=C3)N[C@@H](C(OC)=O)C4=CC=CC=C4
InChi Code
InChI=1S/C25H20N2O3/c1-30-25(29)23(18-12-6-3-7-13-18)27-24(28)20-16-22(17-10-4-2-5-11-17)26-21-15-9-8-14-19(20)21/h2-16,23H,1H3,(H,27,28)/t23-/m1/s1
InChi Key
IUMQXQJZIHWLIN-HSZRJFAPSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    5 mg

    $98

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    10 mg

    $186

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    25 mg

    $416

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    Product Description

    SB-218795 is a neurokinin-3 (NK3) receptor antagonist (Ki = 0.013 µM).1 It is selective for NK3 over NK1 and NK2 receptors (Kis = >100 and 1.221 µM, respectively). SB-218795 inhibits senktide-induced contractions in isolated rabbit iris sphincter muscle preparations (Kb = 43 nM). It also inhibits substance P-induced contraction of longitudinal and circular smooth muscles isolated from rabbit duodenum, jejunum, or ileum when used at a concentration of 1 µM.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Giardina, G.A., Sarau, H.M., Farina, C., et al. Discovery of a novel class of selective non-peptide antagonists for the human neurokinin-3 receptor. 1. Identification of the 4-quinolinecarboxamide framework. J. Med. Chem. 40(12), 1794-1807 (1997).

    2. Valero, M.S., Fagundes, D.S., Grasa, L., et al. Contractile effect of tachykinins on rabbit small intestine. Acta Pharmacol. Sin. 32(4), 487-494 (2011).