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BAY 1316957)

Product Name
BAY 1316957)
CAS No.
1613264-40-6
Chemical 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-
CBNumber
CB54844522
Molecular Formula
C27H27N3O3
Formula Weight
441.52
MOL File
1613264-40-6.mol
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BAY 1316957) Property

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
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

ChemScene
Product number
CS-0087003
Product name
BAY-1316957
Packaging
5mg
Price
$150
Updated
2021/12/16
ChemScene
Product number
CS-0087003
Product name
BAY-1316957
Packaging
10mg
Price
$250
Updated
2021/12/16
ChemScene
Product number
CS-0087003
Product name
BAY-1316957
Packaging
25mg
Price
$550
Updated
2021/12/16
ChemScene
Product number
CS-0087003
Product name
BAY-1316957
Packaging
50mg
Price
$950
Updated
2021/12/16
ChemScene
Product number
CS-0087003
Product name
BAY-1316957
Packaging
100mg
Price
$1550
Updated
2021/12/16
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BAY 1316957) Chemical Properties,Usage,Production

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.

BAY 1316957) Preparation Products And Raw materials

Raw materials

Preparation Products

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BAY 1316957) Suppliers

China 16 United States 4 Global 20
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sales@chemhifuture.com
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  • BAY 1316957)
  • BAY-1316957 (BAY1316957
  • 1H-Benzimidazole-5-carboxylic acid, 2-(9-ethyl-6-methyl-9H-carbazol-3-yl)-1-(2-methoxyethyl)-4-methyl-
  • 1613264-40-6