Fezagepras (Setogepram) sodium 是一种具有口服活性的GPR40激动剂和GPR84拮抗剂或反向激动剂。Fezagepras sodium 减轻肾，肝和胰腺纤维化。Fezagepras sodium 具有抗纤维化，抗炎和抗增殖作用。
| 生物活性 | Fezagepras (Setogepram) sodium acts as an orally active agonist forGPR40and as an antagonist or inverse agonist forGPR84[1]. Fezagepras sodium decreases renal, liver and pancreatic fibrosis[1][2]. Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions[2]. |
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体外研究
(In Vitro) | Fezagepras sodium (500 μM; 24 hours) inhibits TGF-β (10 ng/mL)-activated human hepatic stellate cells (HSCs) proliferation[2].
Fezagepras sodium (250 or 500 μM; 24 hours) dose-dependently arrests HSCs at the G0/G1 phase without inducing apoptosis[2].
Cell Proliferation Assay[2] | Cell Line: | HSCs | | Concentration: | 250 or 500 μM | | Incubation Time: | 24 hours | | Result: | Inhibited TGF-β-activated HSC proliferation. TGF-β (10 ng/mL) increased HSC proliferation by 10%. |
Cell Cycle Analysis[2] | Cell Line: | HSCs | | Concentration: | 250 μM, 500 μM | | Incubation Time: | 24 hours | | Result: | Inhibited cell cycle progression. |
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体内研究
(In Vivo) | Fezagepras sodium (100 mg/kg/day; gavage from 8-20 weeks of age) markedly decreases hyperglycemia and markedly improvea glucose tolerance in type 2 diabetes eNOS-/-db/dbmice[1].
| Animal Model: | Type 2 diabetes eNOS-/-db/dbmice[1] | | Dosage: | 100 mg/kg/day | | Administration: | Given via daily gavage from 8-20 weeks | | Result: | Compared with vehicle-treated mice, hyperglycemia was markedly decreased, and glucose tolerance was markedly improved. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: H2O : ≥ 100 mg/mL(438.10 mM) DMSO : ≥ 64 mg/mL(280.38 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 1 mM | 4.3810 mL | 21.9048 mL | 43.8097 mL | | 5 mM | 0.8762 mL | 4.3810 mL | 8.7619 mL | | 10 mM | 0.4381 mL | 2.1905 mL | 4.3810 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 (sealed storage, away from moisture)。-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： PBS Solubility: 120 mg/mL (525.72 mM); Clear solution; Need ultrasonic 2. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.11 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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。 3. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.11 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 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。 4. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.08 mg/mL (9.11 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (9.11 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 20.8 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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