Description
BAY-1316957 is a potent, selective and orally active prostaglandin E2 receptor subtype 4 (EP4-R) antagonist with an IC50 of 15.3 nM for human EP4-R. BAY-1316957 has excellent drug metabolism and pharmacokinetics properties, and can be used for endometriosis research.
Product information
CAS Number: 1613264-40-6
Molecular Weight: 441.52
Formula: C27H27N3O3
Chemical Name: 2-(9-ethyl-6-methyl-9H-carbazol-3-yl)-1-(2-methoxyethyl)-4-methyl-1H-1,3-benzodiazole-5-carboxylic acid
Smiles: CCN1C2=CC=C(C=C2C2=CC(C)=CC=C12)C1=NC2=C(C=CC(C(O)=O)=C2C)N1CCOC
InChiKey: FHXIZAPGGULPIK-UHFFFAOYSA-N
InChi: InChI=1S/C27H27N3O3/c1-5-29-22-9-6-16(2)14-20(22)21-15-18(7-10-23(21)29)26-28-25-17(3)19(27(31)32)8-11-24(25)30(26)12-13-33-4/h6-11,14-15H,5,12-13H2,1-4H3,(H,31,32)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (226.49 mM; Need ultrasonic).
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
How to use
In Vitro:
BAY-1316957 (Compound 32) shows high solubility and permeability using the Caco-2 cellular assay.
In Vivo:
BAY-1316957 (Compound 32; 0.2-5 mg/kg; oral administration; once) treatment significantly reduces mechanical allodynia in dmPGE2 pain model. The pharmacokinetic parameters of BAY-1316957 (Compound 32) shows a low clearance, long half-life, and high bioavailability (F%=90%) in Wistar rats. Investigation of the metabolic pathways of BAY-1316957 (Compound 32) in human, rat, mouse, dog, and monkey hepatocytes revealed that the formation of the acyl glucuronide was also the common and predominant route of biotransformation, mainly catalyzed by UGT1A1 and to a lesser extent by UGT1A3.
Products are for research use only. Not for human use.
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