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L-798,106 (CAS 244101-02-8) LS-H75

EP3 receptor antagonist
LS-H75-1 / 1 mg / $185
LS-H75-5 / 5 mg / $225
LS-H75-10 / 10 mg / $255
LS-H75-50 / 50 mg / $635
USA Shipment Only
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Description: Prostaglandin E2 exerts its effects through four separate G-protein coupled receptors (EP1, EP2, EP3, and EP4). 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. At 0.2 µM, it blocks the EP3 agonist activity of sulprostone on guinea pig vas deferens and trachea. H75_ChemicalStructureImage.png
(2E)-N-[(5-bromo-2-methoxyphenyl)sulfonyl]-3-[2-(2-naphthalenylmethyl)phenyl]-2-propenamide
CM9
GW671021
biochemical, chemical, antagonist
LS-H75
244101-02-8
C27H22BrNO4
≥95%
A crystalline solid
 
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=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+
ODTKFNUPVBULRJ-NTCAYCPXSA-N
Shipped at 4°C, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: PTGER3 / EP3 related products

Usage Information

L-798,106 is supplied as a crystalline solid. A stock solution may be made by dissolving the L-798,106 in the solvent of choice. L-798,106 is soluble in organic solvents such as DMSO and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of L-798,106 in these solvents is approximately 10 and 20 mg/ml, respectively. L-798,106 is sparingly soluble in aqueous solutions. To enhance aqueous solubility, dilute the organic solvent solution into aqueous buffers or isotonic saline. If performing biological experiments, ensure the residual amount of organic solvent is insignificant, since organic solvents may have physiological effects at low concentrations. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Coleman, R.A., Smith, W.L., and Narumiya, S. Classification of prostanoid receptors: Properties, distribution, and structure of the receptors and their subtypes. Pharmacol. Rev. 46, 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, 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).

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