BAY 1316957)
BAY 1316957) Basic information
- Product Name:
- BAY 1316957)
- Synonyms:
-
- BAY 1316957)
- BAY-1316957 (BAY1316957
- 1H-Benzimidazole-5-carboxylic acid, 2-(9-ethyl-6-methyl-9H-carbazol-3-yl)-1-(2-methoxyethyl)-4-methyl-
- CAS:
- 1613264-40-6
- MF:
- C27H27N3O3
- MW:
- 441.52
- Mol File:
- 1613264-40-6.mol
BAY 1316957) Chemical Properties
- Boiling point:
- 646.3±65.0 °C(Predicted)
- Density
- 1.26±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO : 100 mg/mL (226.49 mM; Need ultrasonic)
- form
- Solid
- pka
- 2.10±0.30(Predicted)
- color
- White to off-white
BAY 1316957) Usage And Synthesis
Uses
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 agent metabolism and pharmacokinetics properties, and can be used for endometriosis research[1].
Biological Activity
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]. BAY-1316957 (Compound 32) shows high solubility and permeability using the Caco-2 cellular assay[1]. 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].
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].
| 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. |
IC 50
human EP4-R: 15.3 nM (IC50)
References
[1]. B?urle S, et al. Identification of a Benzimidazolecarboxylic Acid Derivative (BAY 1316957) as a Potent and Selective Human Prostaglandin E2 Receptor Subtype 4 (hEP4-R) Antagonist for the Treatment of Endometriosis. J Med Chem. 2019 Mar 14;62(5):2541-2563.
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