SSTR5 antagonist 1 (compound 25a) 是一种选择性，口服有效的生长抑素受体亚型 5 (SSTR5) 拮抗剂，对 hSSTR5 和 mSSTR5 的 IC₅₀ 分别为 9.6 和 57 nM。

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.

Solid

IC50: 9.6 nM (hSSTR5), 57 nM (mSSTR5)

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 <10 μL/min/kg (HLM) and 19 μL/min/kg (MLM), respectively.
has not independently confirmed the accuracy of these methods. They are for reference only.

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)

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Hirose H, et al. Discovery of novel 5-oxa-2,6-diazaspiro[3.4]oct-6-ene derivatives as potent, selective, and orally available somatostatin receptor subtype 5 (SSTR5) antagonists for treatment of type 2 diabetes mellitus. Bioorg Med Chem. 2017 Aug 1;25(15):4175-4193.

In Vitro: DMSO : 90 mg/mL (175.92 mM; Need ultrasonic)配制储备液