GPR40 agonist 6
Based on 1 Customer Validation
GPR40 agonist 6 (Compound 7a) is a potent and selective free fatty acid receptor 1 (FFAR1 or GPR40) agonist with an EC50 of 0.058 μM.
For research use only. We do not sell to patients.
- Purity: 98.81%
- CAS No.: 1798751-25-3
- Formula: C20H19NO4
- Molecular Weight:337.37
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
EC50: 0.058 μM (GPR40)[1]
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
>10 μM
Compound: 7a
|
Agonist activity at GPR120 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
Agonist activity at GPR120 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
|
[PMID: 26096679] |
| CHO | EC50 |
>10 μM
Compound: 7a
|
Agonist activity at GPR41 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
Agonist activity at GPR41 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
|
[PMID: 26096679] |
| CHO | EC50 |
>10 μM
Compound: 7a
|
Agonist activity at GPR43 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
Agonist activity at GPR43 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
|
[PMID: 26096679] |
| CHO | EC50 |
0.058 μM
Compound: 7a
|
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
Agonist activity at GPR40 (unknown origin) expressed in CHO cells by FLIPR calcium flux assay in presence of 0.1% bovine serum albumin
|
[PMID: 26096679] |
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[1].
ADME profile for GPR40 agonist 6 (Compound 7a)[1]
| 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 |
aEach value is an average of n = 4, measured at c = 1 µM.
bEach value is an average of n = 2.
cEach value is an average of n = 5, measured at c = 2 µM.
dEach value is an average of n = 2, measured at c = 10 µM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1798751-25-3
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Appearance Solid
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Molecular Weight 337.37
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Formula C20H19NO4
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Color White to off-white
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SMILES
CC1=C(COC2=CC=C(CCC(O)=O)C=C2)N=C(C3=CC=CC=C3)O1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 125 mg/mL (370.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (270 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9641 mL | 14.8205 mL | 29.6410 mL | 74.1026 mL |
| 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL | 14.8205 mL | |
| 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL | 7.4103 mL | |
| 15 mM | 0.1976 mL | 0.9880 mL | 1.9761 mL | 4.9402 mL | |
| 20 mM | 0.1482 mL | 0.7410 mL | 1.4821 mL | 3.7051 mL | |
| 25 mM | 0.1186 mL | 0.5928 mL | 1.1856 mL | 2.9641 mL | |
| 30 mM | 0.0988 mL | 0.4940 mL | 0.9880 mL | 2.4701 mL | |
| 40 mM | 0.0741 mL | 0.3705 mL | 0.7410 mL | 1.8526 mL | |
| 50 mM | 0.0593 mL | 0.2964 mL | 0.5928 mL | 1.4821 mL | |
| 60 mM | 0.0494 mL | 0.2470 mL | 0.4940 mL | 1.2350 mL | |
| 80 mM | 0.0371 mL | 0.1853 mL | 0.3705 mL | 0.9263 mL | |
| 100 mM | 0.0296 mL | 0.1482 mL | 0.2964 mL | 0.7410 mL |