1259389-38-2
1259389-38-2 結(jié)構(gòu)式
常見問題列表
pIC50: 8.13 (FFA1)
AMG 837 (1 nM-10 μM) stimulates insulin secretion in a glucose-dependent manner with an EC
50
of 142±20 nM on islets isolated from mice.
AMG 837 stimulates Ca
2+
flux with the
EC
50
s of 13.5, 22.6 and 31.7 nM for human, mouse and rat receptors in CHO cells, respectively.
AMG 837 (0.03-0.3 mg/kg; p.o. once daily for 21 days) reduces glucose levels and increases insulin levels following glucose challenge in vivo.
AMG 837 (0.03-0.3 mg/kg; a single p.o.) improves glucose tolerance and enhances insulin secretion in Sprague-Dawley rats.
AMG 837 (0.5 mg/kg; p.o.) displays excellent oral bioavailability (F?=?84%) and a total plasma C
max
of 1.4 μM.
| Animal Model: | 8-week old Zucker Fatty Rats |
| Dosage: | 0.03, 0.1, 0.3 mg/kg |
| Administration: | Oral gavage once daily for 21 days |
| Result: |
Decreased glucose AUC values during the glucose tolerance test (GTT) to 7%, 15%, and 25% at 0.03, 0.1 and 0.3 mg/kg, respectively.
Increased insulin levels in the mid- and high-dose groups. Not affected body weights during the 21-day treatment. |
| Animal Model: | 8-week old Sprague-Dawley rats |
| Dosage: | 0.03, 0.1, 0.3 mg/kg |
| Administration: | A single p.o. administration |
| Result: | Reduced the post-prandial glucose with the half-maximal dose of 0.05 mg/kg. |