Powder: -20°C for 3 years | In solvent: -80°C for 1 year
BMS-903452 is a potent and selective GPR119 agonist with EC50 of 14 nM. BMS-903452 is indicated for the treatment of acute and chronic rodent diabetes. GPR119 was mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. GPR119 had no significant inhibitory effect on 9 different cytochrome P450 enzymes (IC50 > 40 μM), did not activate PXR (EC50>50 μM), and was not toxic to liver (HEPG2) cell lines.
パッケージサイズ | 在庫状況 | 単価(税別) |
---|---|---|
1 mg | 在庫あり | ¥ 59,500 |
5 mg | 在庫あり | ¥ 147,500 |
10 mg | 在庫あり | ¥ 209,500 |
25 mg | 在庫あり | ¥ 314,500 |
50 mg | 在庫あり | ¥ 424,500 |
100 mg | 在庫あり | ¥ 574,000 |
500 mg | 在庫あり | ¥ 1,124,500 |
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 173,000 |
説明 | BMS-903452 is a potent and selective GPR119 agonist with EC50 of 14 nM. BMS-903452 is indicated for the treatment of acute and chronic rodent diabetes. GPR119 was mainly expressed in pancreatic b cells and gastrointestinal endocrine cells. GPR119 had no significant inhibitory effect on 9 different cytochrome P450 enzymes (IC50 > 40 μM), did not activate PXR (EC50>50 μM), and was not toxic to liver (HEPG2) cell lines. |
ターゲット&IC50 | GPR119:14nM(EC50) |
In vivo |
An oral glucose tolerance test (OGTT) to measure the acute efficacy of this agonist in C57/BL6 mice. Glucose excursion was 37%-40% lower in mice treated with BMS-903452 (0.1, 0.3, and 1 mg/kg) than in control mice. Treatment of SD rats with 0.3 mg/kg BMS-903452 stimulated GLP-1 production, and co-administration of BMS-903452 with a DPP-4 inhibitor synergistically augmented GLP-1 levels. [1] BMS-903452 (0.03 mg/kg/day) also reduced fasting plasma glucose levels with increased insulin levels in db/db mice. [1] BMS-903452 was safe and tolerable in normal healthy volunteers given a single dose ranging from 0.1 to 120mg, but did not alter plasma GLP-1 within the first 24 h of treatment.[2] |
分子量 | 513.37 |
分子式 | C21H19Cl2FN4O4S |
CAS No. | 1339944-47-6 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mg/mL (19.48 mM)
You can also refer to dose conversion for different animals. 詳細
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BMS-903452 1339944-47-6 Endocrinology/Hormones GPCR/G Protein GPR Inhibitor inhibitor inhibit