SSTR5 antagonist 1

小分子

SSTR5 拮抗剂 1

SSTR5 antagonist 1

S648964-5mg

5mg

≥99%

-20°C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. Form:Solid 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

C28H34FN3O5

511.59 g/mol

90423921

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

1-[2-[[3,5-diethoxy-4-(4-fluorophenyl)phenyl]methyl]-5-oxa-2,6-diazaspiro[3.4]oct-6-en-7-yl]piperidine-4-carboxylic acid

1S/C28H34FN3O5/c1-3-35-23-13-19(14-24(36-4-2)26(23)20-5-7-22(29)8-6-20)16-31-17-28(18-31)15-25(30-37-28)32-11-9-21(10-12-32)27(33)34/h5-8,13-14,21H,3-4,9-12,15-18H2,1-2H3,(H,33,34)

UQRAIIGEZLINAT-UHFFFAOYSA-N

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

90423921

DMSO : 90 mg/mL (175.92 mM; Need ultrasonic)

1

8

9

511.248 Da

511.248 Da

83.800 Ų

37

0

790.000

0

1

1.100