GPR40 agonist 6 (Compound 7a) is a potent and selective free fatty acid receptor 1 ( FFAR1 or GPR40 ) agonist with an EC 50 of 0.058 μM In Vitro GPR40 agonist 6 (Compound 7a) shows a very favorable ADME profile, and shows no significant inhibition of the principal cytochrome P450 isoforms (1A2, 2C9, 2C19, 2D6 and 3A4) at 5 µM. ADME profile for GPR40 agonist 6 (Compound 7a)GPR40 agonist 6 (Compound 7a) Plasma protein binding (human) a 98.6% Aqueous solubility (PBS, pH 7.4) b 404 µM Microsomal stability (mouse, t1/2) c 434 min A-B permeability (Caco-2, cm•s -1 ) d 15.2 • 10 -6 a Each value is an average of n = 4, measured at c = 1 µM. b Each value is an average of n = 2. c Each value is an average of n = 5, measured at c = 2 µM. d Each value is an average of n = 2, measured at c = 10 µM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:EC 50 : 0.058 μM (GPR40)
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GPR40 agonist 6
CAS number:1798751-25-3(DMSO) molecular formula:C20H19NO4
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| Chinese alias | GPR40 激动剂 6 | ||
| English alias | - | ||
| CAS number | 1798751-25-3(DMSO) | molecular formula | C20H19NO4 |
| molecular weight | 337.37 g/mol | Exact mass | 10mM in DMSO |
| PSA | - | logp | - |
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