GPR
阻害剤の選択性比較
| カタログ番号 | 製品カタログ | 溶解度(25°C) | ||
|---|---|---|---|---|
| 水 | DMSO | アルコール | ||
| S7263 | AZD1981 | <1 mg/mL | 11 mg/mL | <1 mg/mL |
| S2822 | OC000459 | <1 mg/mL | 4 mg/mL | <1 mg/mL |
| S2637 | Fasiglifam (TAK-875) | <1 mg/mL | 100 mg/mL | <1 mg/mL |
| S2149 | GSK1292263 | <1 mg/mL | 34 mg/mL | <1 mg/mL |
| S8014 | GW9508 | <1 mg/mL | 69 mg/mL | 69 mg/mL |
| S6746 | APD668 | <1 mg/mL | 96 mg/mL | 2 mg/mL |
GPR製品
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S7263 |
AZD1981AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2. |
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| S2822 |
OC000459OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2. |
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| S2637 |
Fasiglifam (TAK-875)Fasiglifam (TAK-875) is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid. |
INS-1 cells were incubated with 50 uM palmitate or BSA in the presence or absence of 5 uM TAK 875 for 30 min, followed by stimulation with 16.6 mm [U-13C]glucose for 30 min. Under these conditions, the following were measured: fructose bisphosphate (FBP) (I), NADH/NAD+ ratio (J). Error bars represent mean ?S.E. n = 3-4.
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| S2149 |
GSK1292263GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2. |
(B) WB403 at 10, 20 μmol/l had no significant stimulation effect on hGPR119 dependent cAMP accumulation. GSK1292263 (1 μmol/l) was used as positive agonist of GPR119.
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| S8014 |
GW9508GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. |
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| S6746新 |
APD668APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively. |
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| S6759新 |
GPR39-C3 (TC-G-1008)GPR39-C3 is a potent and orally bioavailable agonist of GPR39 with EC50 of 0.4nM and 0.8nM for rat and human receptor, respectively. |
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| S4709 |
LatanoprostLatanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S7263 |
AZD1981AZD1981 is a potent, selective CRTh2 (DP2) receptor antagonist with IC50 of 4 nM, showing >1000-fold selectivity over more than 340 other enzymes and receptors, including DP1. Phase 2. |
2019, 18(11):2097-2110 |
|
| S2822 |
OC000459OC000459 is a potent and selective D prostanoid receptor 2 (DP2) antagonist with IC50 of 13 nM. Phase 2. |
| 製品コード | 製品説明 | 文献中Selleckの製品使用例 | お客様のフィードバック |
|---|---|---|---|
| S2637 |
Fasiglifam (TAK-875)Fasiglifam (TAK-875) is a selective GPR40 agonist with EC50 of 14 nM in human GPR40 expressing CHO cell line, 400-fold more potent than oleic acid. |
2018, 159(8):2939-2952 2017, 7(1):4657 2016, 22(4):439-45 |
INS-1 cells were incubated with 50 uM palmitate or BSA in the presence or absence of 5 uM TAK 875 for 30 min, followed by stimulation with 16.6 mm [U-13C]glucose for 30 min. Under these conditions, the following were measured: fructose bisphosphate (FBP) (I), NADH/NAD+ ratio (J). Error bars represent mean ?S.E. n = 3-4.
|
| S2149 |
GSK1292263GSK1292263 is a novel GPR119 agonist, showing potential for the treatment of type 2 diabetes. Phase 2. |
2015, 10(7):e0134051 |
(B) WB403 at 10, 20 μmol/l had no significant stimulation effect on hGPR119 dependent cAMP accumulation. GSK1292263 (1 μmol/l) was used as positive agonist of GPR119.
|
| S8014 |
GW9508GW9508 is a potent and selective agonist for FFA1 (GPR40) with pEC50 of 7.32, 100-fold selective against GPR120, stimulates insulin secretion in a glucose-sensitive manner. |
2019, 170:176-186 2018, 4(10):eaau2357 2018, 32(7):3924-3935 |
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| S6746新 |
APD668APD668 is a potent GPR119 agonist with EC50s of 2.7 and 33 nM for human and rat forms, respectively. |
||
| S6759新 |
GPR39-C3 (TC-G-1008)GPR39-C3 is a potent and orally bioavailable agonist of GPR39 with EC50 of 0.4nM and 0.8nM for rat and human receptor, respectively. |
||
| S4709 |
LatanoprostLatanoprost is a prostaglandin F2alpha analogue and a prostanoid selective FP receptor agonist with an ocular hypertensive effect. Latanoprost increases uveoscleral outflow and thereby reduces intraocular pressure. |
