SSTR5 antagonist 2 (compound 10) 是强效的、具有口服活性的生长激素抑制激素(受体)亚型 5 (SSTR5) 的选择性拮抗剂,有潜力用于 2 型糖尿病的研究。
生物活性 | SSTR5antagonist 2 (compound 10) is a highly potent, oral active andselective somatostatin (receptor) subtype 5 (SSTR5)antagonist and has potential for the research of treat type 2 diabetes mellitus (T2DM)[1]. |
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体内研究 (In Vivo) | SSTR5 antagonist 2 (10 mg/kg, orally) increases both total and active circulating incretin hormone GLP1 levels in mice at a dose of 10 mg/kg[1]. SSTR5 antagonist 2 increases pancreatic insulin secretion as well as total and active GLP1 release, and demonstrates synergistic effects in combination with DPP4 inhibitors[1].
Animal Model: | Rodent diabetic model without risk of hypoglycemia[1]. | Dosage: | 10 mg/kg. | Administration: | Orally. | Result: | Increased both total and active circulating incretin hormone GLP1 levels. |
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运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
溶解性数据 | In Vitro: DMSO : 25 mg/mL(45.73 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 1.8294 mL | 9.1470 mL | 18.2939 mL | 5 mM | 0.3659 mL | 1.8294 mL | 3.6588 mL | 10 mM | 0.1829 mL | 0.9147 mL | 1.8294 mL |
In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶 1. 请依序添加每种溶剂: 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.57 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂: 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (4.57 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.57 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。 *以上所有助溶剂都可在本网站选购。
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