306974-70-9
GW-1100
CAS: 306974-70-9
Molecular Formula: C27H25FN4O4S
306974-70-9 - Names and Identifiers
306974-70-9 - Physico-chemical Properties
| Molecular Formula | C27H25FN4O4S |
| Molar Mass | 520.58 |
| Density | 1.29±0.1 g/cm3(Predicted) |
| Melting Point | 208-210℃ |
| Boling Point | 690.2±65.0 °C(Predicted) |
| Solubility | Soluble in DMSO (up to 2 mg/ml) or in DMF (up to 5 mg/ml). |
| Appearance | White powder |
| Color | White |
| pKa | 1.20±0.22(Predicted) |
| Storage Condition | +2C to +8C |
| Stability | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or DMF may be stored at -20° for up to 3 months. Dilutions into aqueous media are not stable and should be used within one workin |
| In vitro study | GW-1100 (GW1100) dose dependently inhibits GPR40-mediated Ca 2+ elevations stimulated by GW9508 and linoleic acid (pIC 50 values of 5.99±0.03 and 5.99±0.06, respectively). GW-1100 at a concentration of 1 μM produces a significant rightward shift in the concentration-response curve to GW9508 (pEC 50 =7.17±0.08 in the absence and pEC 50 =6.79±0.09 in the presence of 1 μM GW-1100; P<0.05; n=3). At concentrations of GW-1100 of 3 μM and higher a significant decrease in the maximal response is observed with a continuing rightward shift in the pEC 50 response. GW-1100 (GW1100) reduces FFAR1 ligand-induced intracellular calcium in CHO-K1/bFFAR1 cells and neutrophils. CHO-K1/bFFAR1 cells are incubated for 15 min with 10 μM GW1100 or vehicle (0.1% DMSO) and then stimulated with vehicle, oleic acid, linoleic acid or GW9508. GW-1100 significantly reduces the increase in intracellular calcium induced by 300 μM oleic acid (AUC (60-150 s) , p<0.05), 100 μM linoleic acid (AUC (60-150 s) , p<0.05) and 10 μM GW9508 (AUC (60-150 s) , p<0.05). |
| In vivo study | The intracerebroventricular injection of DHA (50 µg) and GW9508 (1.0 µg), a GPR40-selective agonist, significantly reduces mechanical allodynia and thermal hyperalgesia at day 7, but not at day 1, after CFA injection. These effects are inhibited by intracerebroventricular pretreatment with GW-1100 (10 µg), a GPR40 antagonist. |
306974-70-9 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 1.921 ml | 9.604 ml | 19.209 ml |
| 5 mM | 0.384 ml | 1.921 ml | 3.842 ml |
| 10 mM | 0.192 ml | 0.96 ml | 1.921 ml |
| 5 mM | 0.038 ml | 0.192 ml | 0.384 ml |
Last Update：2024-01-02 23:10:35
306974-70-9 - Reference Information
| biological activity | GW-1100 is a selective GPR40 antagonist, pIC50 is 6.9. |
| target | pIC50: 6.9 (GPR40) |
| in vitro study | GW-1100 (GW1100) dose dependently inhibits GPR40-mediated Ca 2 + elevations stimulated by GW9508 and linoleic acid (pIC 50 values of 5.99±0.03 and 5.99±0.06, respectively). GW-1100 at a concentration of 1 μM produces a significant rightward shift in the concentration-response curve to GW9508 (pEC 50=7.17±0.08 in the absence and pEC 50=6.79±0.09 in the presence of 1 μM GW-1100; P<0.05; N = 3). At concentrations of GW-1100 of 3 μM and higher a significant decrease in the maximal response is observed with a continuing rightward shift in the pEC 50 response. GW-1100 (GW1100) reduces FFAR1 ligand-induced intracellular calcium in CHO-K1/bFFAR1 cells and neutrophils. CHO-K1/bFFAR1 cells are incubated for 15 min with 10 μM GW1100 or vehicle (0.1% DMSO) and then stimulated with vehicle, oleic acid, linoleic acid or GW9508. GW-1100 significantly reduces the increase in intracellular calcium induced by 300 μ m oleic acid (AUC (60-150 s) , p<0.05), 100 μ m linoleic acid (AUC (60-150 s) , p<0.05) and 10 μ m GW9508 (AUC (60-150 s), P<0.05). |
| in vivo studies | The intracerebroventricular injection of DHA (50g) and GW9508 (1.0g), a GPR40-selective agonist, significantly reduces mechanical allodynia and thermal hyperalgesia at day 7, but not at day 1, after CFA injection. These effects are inhibited by intracerebroventricular pretreatment with GW-1100 (10g), a GPR40 antagonist. |
Last Update：2024-04-09 15:16:38
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Product Name: GW-1100 Visit Supplier Webpage Request for quotation
CAS: 306974-70-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
CAS: 306974-70-9
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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