Description
ONO-8130 is an orally bioavailable and selective antagonist of the prostaglandin E2 (PGE2) receptor EP1 with Ki value of 1.9 nM . Prostaglandins contribute to the sensitization of peripheral and central nociceptive neurons during peripheral inflammation. Prostaglandin E2 (PGE2) is considered a dominant pronociceptive prostanoid. PGE2 receptors are G protein-coupled receptors and classified into 4 general subtypes (EP1, EP2, EP3, and EP4) that are located unevenly in different tissues. EP1 receptors play a major role in processing of pain . In cystitis-related bladder pain mice, Oral preadministration of ONO-8130 at 0.3-30 mg/kg strongly prevented both the bladder pain-like behavior and referred hyperalgesia in a dose-dependent way. ONO-8130 at 30 mg/kg also reversed the established cystitis-related bladder pain. ONO-8130 also blocked prostaglandin E2 caused prompt phosphorylation of ERK in the L6 spinal cord . In the guinea pig trachea (GPT), ONO-8130 inhibited the initial contraction mediated by PGE2. ONO-8130 also eliminated the spontaneous tone .
Product information
CAS Number: 459841-96-4
Molecular Weight: 500.63
Formula: C25H28N2O5S2
Chemical Name: 4-[({6-[N-(2-methylpropyl)4-methyl-1,3-thiazole-2-sulfonamido]-2,3-dihydro-1H-inden-5-yl}oxy)methyl]benzoic acid
Smiles: CC1=CSC(=N1)S(=O)(=O)N(CC(C)C)C1=CC2CCCC=2C=C1OCC1C=CC(=CC=1)C(O)=O
InChiKey: IOXMDBQCUCDLAF-UHFFFAOYSA-N
InChi: InChI=1S/C25H28N2O5S2/c1-16(2)13-27(34(30,31)25-26-17(3)15-33-25)22-11-20-5-4-6-21(20)12-23(22)32-14-18-7-9-19(10-8-18)24(28)29/h7-12,15-16H,4-6,13-14H2,1-3H3,(H,28,29)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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