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。
| 生物活性 | SSTR5antagonist 1 (compound 25a) is a selective and orally availablesomatostatin receptorsubtype 5 (SSTR5) antagonist withIC50s of 9.6 and 57 nM forhSSTR5andmSSTR5, respectively[1]. |
| IC50& Target | IC50: 9.6 nM (hSSTR5), 57 nM (mSSTR5)[1] |
体外研究
(In Vitro) | 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 μlminkg (hlm) and 19 (mlm),respectively[1].
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体内研究
(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) | 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 |
| 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/kgGlibenclamide(HY-15206) and comparable to that of 30 mg/kgAlogliptin(HY-A0023A).
Augmented insulin secretion in a glucose-dependent manner and displayed a blood glucose-lowering effect, indicating its anti-diabetic efficacy in vivo. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 90 mg/mL(175.92 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.9547 mL | 9.7735 mL | 19.5469 mL | | 5 mM | 0.3909 mL | 1.9547 mL | 3.9094 mL | | 10 mM | 0.1955 mL | 0.9773 mL | 1.9547 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 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: ≥ 2.25 mg/mL (4.40 mM); Clear solution
此方案可获得 ≥ 2.25 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 22.5 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: ≥ 2.25 mg/mL (4.40 mM); Clear solution
此方案可获得 ≥ 2.25 mg/mL (4.40 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 22.5 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.25 mg/mL (4.40 mM); Clear solution
此方案可获得 ≥ 2.25 mg/mL (4.40 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例，取 100 μL 22.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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