A selective EP3 receptor antagonist
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L-798,106

Item No. 11129

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(2E)-N-[(5-bromo-2-methoxyphenyl)sulfonyl]-3-[2-(2-naphthalenylmethyl)phenyl]-2-propenamide
CAS Number
244101-02-8
Synonyms
  • CM 9
  • GW 671021
Molecular Formula
C27H22BrNO4S
Formula Weight
536.4
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: 1 mg/mlDMF: 20 mg/mlDMSO: 10 mg/ml
λmax
221, 285 nm
SMILES
O=C(NS(C1=C(OC)C=CC(Br)=C1)(=O)=O)/C=C/C2=CC=CC=C2CC3=CC4=C(C=C3)C=CC=C4
InChi Code
InChI=1S/C27H22BrNO4S/c1-33-25-14-13-24(28)18-26(25)34(31,32)29-27(30)15-12-21-7-3-5-9-23(21)17-19-10-11-20-6-2-4-8-22(20)16-19/h2-16,18H,17H2,1H3,(H,29,30)/b15-12+
InChi Key
ODTKFNUPVBULRJ-NTCAYCPXSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    Prostaglandin E2 (Item No. 14010) exerts its effects through four separate G-protein coupled receptors (EP1, EP2, EP3, and EP4).1 L-798,106 is a highly selective EP3 receptor antagonist with Ki values of 0.3, 916, >5,000, and >5,000 nM at EP3, EP4, EP1, and EP2, respectively.2 At 0.2 µM, it blocks the EP3 agonist activity of sulprostone (Item No. 14765) on guinea pig vas deferens and trachea.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Coleman, R.A., Smith, W.L., and Narumiya, S. International Union of Pharmacology classification of prostanoid receptors: Properties, distribution, and structure of the receptors and their subtypes. Pharmacol. Rev. 46(2), 205-229 (1994).

    2. Juteau, H., Gareau, Y., Labelle, M., et al. Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor. Bioorg. Med. Chem. 9(8), 1977-1984 (2001).

    3. Jones, R.L., Giembycz, M.A., and Woodward, D.F. Prostanoid receptor antagonists: Development strategies and therapeutic applications. Br. J. Pharmacol. 158(1), 104-145 (2009).