ChemicalBook CAS DataBase List 1628741-91-2

1628741-91-2

Name	SSTR5 antagonist 1
CAS	1628741-91-2
Molecular Formula	C28H34FN3O5
Molecular Weight	511.59
MOL File	1628741-91-2.mol

Chemical Properties

Boiling point	614.2±65.0 °C(Predicted)
density	1.32±0.1 g/cm3(Predicted)
storage temp.	Store at -20°C
solubility	DMSO : 90 mg/mL (175.92 mM; Need ultrasonic)
form	Solid
pka	4.48±0.20(Predicted)
color	White to off-white

Hazard Information

Uses

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].

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	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

Animal Model:	High-fat diet fed C57BL/6J mice^[1]
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.

References

[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. DOI:10.1016/j.bmc.2017.06.007

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