2-Thiophenecarboxylic acid, 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]-

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2-Thiophenecarboxylic acid, 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]- Basic information
Product Name:2-Thiophenecarboxylic acid, 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]-
Synonyms:2-Thiophenecarboxylic acid, 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]-;P2Y14R antagonist 2
CAS:2989271-65-8
MF:C18H13FN2O4S
MW:372.37
EINECS:
Product Categories:
Mol File:2989271-65-8.mol
2-Thiophenecarboxylic acid, 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]- Structure
2-Thiophenecarboxylic acid, 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]- Chemical Properties
Boiling point 471.2±45.0 °C(predicted)
density 1.462±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted)
pka3.78±0.10(predicted)
Safety Information
MSDS Information
2-Thiophenecarboxylic acid, 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]- Usage And Synthesis
UsesP2Y14R antagonist 2 (compound 39) is a potent, selective and orally active P2Y14R antagonist with an IC50 value of 0.40 nM. P2Y14R antagonist 2 shows anti-inflammatory activity. P2Y14R antagonist 2 has the potential for the research of colitis[1].
in vivo

P2Y14R antagonist 2 (50, 100 μM for 100μL per mice; rectally administered, daily for 7 days) shows anti-inflammatory activity in mice with colitis[1].
Pharmacokinetic Parameters[1].

Parametersdose (mg/kg)Cmax (ng/mL)T1/2 (min)Tmax (min)AUCall (min*ng/mL)CL (mL/min/kg)F (%)
iv1.0-21 ± 8.4-27924 ± 5520133.8 ± 33-
po5.0518.25 ± 196.26177.6 ± 24.61590744 ± 21613232.2 ± 46.265.0
Animal Model:6-8 weeks, 20-22 g, male C57BL/6 mice (colitis) [1]
Dosage:50, 100 μM for 100μL per mice
Administration:Rectally administered, daily for 7 days
Result:Alleviated DSS-induced body weight loss, loose stools, rectal bleeding, colon shortening, and elevated spleen weighted index.
IC 50P2Y14 Receptor: 0.40 nM (IC50)
References[1] Wang YH, et al. Discovery of a Series of 4-Amide-thiophene-2-carboxyl Derivatives as Highly Potent P2Y14 Receptor Antagonists for Inflammatory Bowel Disease Treatment. J Med Chem. 2024 Jul 3. DOI:10.1021/acs.jmedchem.4c00699
2-Thiophenecarboxylic acid, 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]- Preparation Products And Raw materials
Tag:2-Thiophenecarboxylic acid, 5-[(5-fluoro-2-pyridinyl)oxy]-4-[(4-methylbenzoyl)amino]-(2989271-65-8) Related Product Information
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