1. GPCR/G Protein
  2. Prostaglandin Receptor
  3. BAY-1316957

BAY-1316957 

Cat. No.: HY-111539
Handling Instructions

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.

For research use only. We do not sell to patients.

BAY-1316957 Chemical Structure

BAY-1316957 Chemical Structure

CAS No. : 1613264-40-6

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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[1].

IC50 & Target[1]

h-EP4

15.3 nM (IC50)

In Vitro

BAY-1316957 (Compound 32) shows high solubility and permeability using the Caco-2 cellular assay[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

BAY-1316957 (Compound 32; 0.2-5 mg/kg; oral administration; once) treatment significantly reduces mechanical allodynia in dmPGE2 pain model[1].
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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male adult Sprague Dawley rats (220-265 g) injected with 16,16-dimethyl prostaglandin E2 (dmPGE2)[1]
Dosage: 0.2 mg/kg, 1 mg/kg, 5 mg/kg
Administration: Oral administration; once
Result: Significantly reduced paw withdrawal thresholds in dmPGE2 pain model.
Molecular Weight

441.52

Formula

C₂₇H₂₇N₃O₃

CAS No.

1613264-40-6

SMILES

COCCN(C(C1=CC2=C(N(CC)C3=C2C=C(C)C=C3)C=C1)=N4)C5=C4C(C)=C(C(O)=O)C=C5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

BAY-1316957BAY1316957BAY 1316957Prostaglandin ReceptorEP4-Rendometriosisanti-inflammatoryantinociceptiveUGT1A1Inhibitorinhibitorinhibit

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BAY-1316957
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