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CAS No. : 1628741-91-2
MCE 国际站:SSTR5 antagonist 1
产品活性: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。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:Somatostatin Receptor
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 <10 μL/min/kg (HLM) and 19 μL/min/kg (MLM), respectively.
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) | CLtotal (mL/h/kg) | Vss (mL/kg) | MRT (h) | |
iv | 0.1 | 1761 | 3052 | 1.7 | / |
Route | Dose (mg/kg) | Cmax (ng/mL) | Tmax (h) | AUC0-8 h (ng·h/mL) | F (%) |
po | 1 | 74.8 | 2.0 | 332 | 58 |
相关产品:Bioactive Compound Library Plus | GPCR/G Protein Compound Library | Neuronal Signaling Compound Library | Anti-diabetic Compound Library | Endocrinology Compound Library | Orally Active Compound Library | Targeted Diversity Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | MK-4256 | Somatostatin-28 (sheep) | BIM-23190 | sst2 Receptor agonist-1 | Cortistatin 14, human, rat | Pasireotide (diaspartate) | Octreotide pamoate | PRL 2915 | CYN 154806 | BIM-23056 TFA | MAT2A-IN-1 | L-797591 | TT-232 | DOTA-NOC | SSTR4 agonist 3 | SSTR5 antagonist 2 | Cortistatin-14 TFA | J-2156 TFA | Cyclosomatostatin TFA | L-803087 | Veldoreotide | Angiopeptin TFA | [Nle8] Somatostatin (1-28) | MAT2A-IN-3 | Somatostatin-28 (1-14)
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