SSTR5 antagonist 1

小分子

SSTR5 拮抗剂 1

SSTR5 antagonist 1

S655649-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 ( SSTR5 ) antagonist with IC 50 s of 9.6 and 57 nM for hSSTR5 and mSSTR5 , respectively In Vitro 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 In Vivo 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) Route Dose (mg/kg) CL total (mL/h/kg) V ss (mL/kg) MRT (h) iv 0.1 1761 3052 1.7 / Route Dose (mg/kg) C max (ng/mL) T max (h) AUC 0-8 h (ng·h/mL) F (%) po 1 74.8 2.0 332 58 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 and comparable to that of 30 mg/kg Alogliptin . Augmented insulin secretion in a glucose-dependent manner and displayed a blood glucose-lowering effect, indicating its anti-diabetic efficacy in vivo. IC50& Target:IC50: 9.6 nM (hSSTR5), 57 nM (mSSTR5)

SSTR5 拮抗剂 1（化合物 25a）是一种选择性口服体生长抑素受体亚型 5（SSTR5）拮抗剂，对 hSSTR5 和 mSSTR5 的 IC 50 s 分别为 9.6 和 57 nM。

1628741-91-2(DMSO)

C28H34FN3O5

511.59 g/mol

CCOC1=CC(=CC(=C1C2=CC=C(C=C2)F)OCC)CN3CC4(C3)CC(=NO4)N5CCC(CC5)C(=O)O