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

BAY-1316957 

Cat. No.: HY-111539 Purity: 98.94%
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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Free Sample (0.5-1 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 165 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
10 mg USD 250 In-stock
Estimated Time of Arrival: December 31
25 mg USD 550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 950 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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.
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (226.49 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2649 mL 11.3245 mL 22.6490 mL
5 mM 0.4530 mL 2.2649 mL 4.5298 mL
10 mM 0.2265 mL 1.1325 mL 2.2649 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (11.32 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Product Name:
BAY-1316957
Cat. No.:
HY-111539
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