产品
编 号：F195680
分子式：C28H34FN3O5
分子量：511.59
分子式：C28H34FN3O5
分子量：511.59
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
询价
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10mg
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询价
25mg
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询价
结构图
CAS No: 1628741-91-2
产品详情
生物活性：
SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively.
体内研究：
SSTR5 antagonist 1 (compound 25a) (1 mg/kg; p.o.; single dose) is orally available with acceptable plasma exposure in mice in pharmacokinetic screening and exhibits excellent solubility (260 μg/mL, pH=6.8).SSTR5 antagonist 1 (100 mg/kg; p.o.; single dose; measured at 0-120 min) augments insulin secretion in a glucose-dependent manner and lowers blood glucose concentration in high-fat diet fed C57BL/6J mice.SSTR5 antagonist 1 (1, 3, 10, and 30 mg/kg; p.o.; single dose) shows dose-dependent effect on glucose excursion measured during the oral glucose tolerance test in HFD fed C57BL/6J mice.Pharmacokinetic profiles in male ICR mouse (8-week-old)RouteDose (mg/kg)CLtotal (mL/h/kg)Vss (mL/kg)MRT (h)
iv0.1176130521.7/
RouteDose (mg/kg)Cmax (ng/mL)Tmax (h)AUC0-8 h (ng·h/mL)F (%)
po174.82.033258
Animal Model:High-fat diet fed C57BL/6J mice
Dosage:100 mg/kg
Administration:Oral gavage; single dose; monitored over 2 h
Result:Showed the maximum efficacy superior to that of 10 mg/kg Glibenclamide (HY-15206) and comparable to that of 30 mg/kg Alogliptin (HY-A0023A).Augmented insulin secretion in a glucose-dependent manner and displayed a blood glucose-lowering effect, indicating its anti-diabetic efficacy in vivo.
体外研究：
SSTR5 antagonist 1 (compound 25a) (30 μM) inhibits hERG activity by 5.6%.SSTR5 antagonist 1 (10 μM) shows highly selective inhibitory effect on SSTR5 over SSTR1-4, with inhibition rates of 11%, 8%, 14%, 10%.SSTR5 antagonist 1 (1 μM; 15 min and 30 min) exhibits good metabolic stability toward both human and mouse microsomes with in vitro CLint value of SSTR5 antagonist 1 相关抗体:
SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 (SSTR5) antagonist with IC50s of 9.6 and 57 nM for hSSTR5 and mSSTR5, respectively.
体内研究：
SSTR5 antagonist 1 (compound 25a) (1 mg/kg; p.o.; single dose) is orally available with acceptable plasma exposure in mice in pharmacokinetic screening and exhibits excellent solubility (260 μg/mL, pH=6.8).SSTR5 antagonist 1 (100 mg/kg; p.o.; single dose; measured at 0-120 min) augments insulin secretion in a glucose-dependent manner and lowers blood glucose concentration in high-fat diet fed C57BL/6J mice.SSTR5 antagonist 1 (1, 3, 10, and 30 mg/kg; p.o.; single dose) shows dose-dependent effect on glucose excursion measured during the oral glucose tolerance test in HFD fed C57BL/6J mice.Pharmacokinetic profiles in male ICR mouse (8-week-old)RouteDose (mg/kg)CLtotal (mL/h/kg)Vss (mL/kg)MRT (h)
iv0.1176130521.7/
RouteDose (mg/kg)Cmax (ng/mL)Tmax (h)AUC0-8 h (ng·h/mL)F (%)
po174.82.033258
Animal Model:High-fat diet fed C57BL/6J mice
Dosage:100 mg/kg
Administration:Oral gavage; single dose; monitored over 2 h
Result:Showed the maximum efficacy superior to that of 10 mg/kg Glibenclamide (HY-15206) and comparable to that of 30 mg/kg Alogliptin (HY-A0023A).Augmented insulin secretion in a glucose-dependent manner and displayed a blood glucose-lowering effect, indicating its anti-diabetic efficacy in vivo.
体外研究：
SSTR5 antagonist 1 (compound 25a) (30 μM) inhibits hERG activity by 5.6%.SSTR5 antagonist 1 (10 μM) shows highly selective inhibitory effect on SSTR5 over SSTR1-4, with inhibition rates of 11%, 8%, 14%, 10%.SSTR5 antagonist 1 (1 μM; 15 min and 30 min) exhibits good metabolic stability toward both human and mouse microsomes with in vitro CLint value of SSTR5 antagonist 1 相关抗体:
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