| Bioactivity | 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[1]. | ||||||||||||
| Target | IC50: 9.6 nM (hSSTR5), 57 nM (mSSTR5) | ||||||||||||
| Invitro | SSTR5 antagonist 1 (compound 25a) (30 μM) inhibits hERG activity by 5.6%[1].SSTR5 antagonist 1 (10 μM) shows highly selective inhibitory effect on SSTR5 over SSTR1-4, with inhibition rates of 11%, 8%, 14%, 10%[1].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[1]. | ||||||||||||
| 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)[1].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[1].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[1].Pharmacokinetic profiles in male ICR mouse (8-week-old)[1]Route | ||||||||||||
| Name | SSTR5 antagonist 1 | ||||||||||||
| CAS | 1628741-91-2 | ||||||||||||
| Formula | C28H34FN3O5 | ||||||||||||
| Molar Mass | 511.59 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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. |
SSTR5 antagonist 1
CAS: 1628741-91-2 F: C28H34FN3O5 W: 511.59
SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 (SSTR5) antagonist
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