Evogliptin (DA-1229) tartrat 是一种口服有效的DPP4抑制剂，在小鼠模型中具有显著而持久的降糖效果。Evogliptin tartrat 还可通过诱导自噬来抑制肝细胞的炎症和纤维化信号的产生。Evogliptin tartrat 可用于 2 型糖尿病、骨质疏松症，肾功能损害以及慢性肝脏炎症的研究。
| 生物活性 | Evogliptin (DA-1229) tartrate is an orally activeDPP4inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin tartrate also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducingautophagy. Evogliptin tartrate can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation[1][2][3][4]. |
| IC50& Target | |
体外研究
(In Vitro) | Evogliptin tartrate (2.49 mM; 12 h) efficiently inhibits mDPP4 (membrane DPP4) enzymatic activity in PWM-induced H9 Th1 cells[1].
Evogliptin tartrate prevents inflammatory and fibrotic signaling through autophagy induction in primary hepatocytes of ATG7f/f-Cre+mice[2].
Cell Viability Assay[1] | Cell Line: | H9 Th1 cells (pokeweed mitogen (PWM)-induced) | | Concentration: | 2.49 mM (1 μg/mL) | | Incubation Time: | 12 h | | Result: | Potently inhibited mDPP4 (membrane DPP4) activity in a dose-dependent manner but did not affect either the cytokine profile or cell viability in PWM-activated CD4+CD26+H9 Th1 cells. |
|
体内研究
(In Vivo) | Evogliptin tartrate (100, 300 mg/kg; in animal feedings; single daily for 10 weeks) exhibits antidiabetic effects on HFD/STZ mice and improves glucose intolerance and insulin resistance[3].
| Animal Model: | Male ICR mice (four-week-old; HFD/STZ mice model)[3]. | | Dosage: | 100, 300 mg/kg | | Administration: | In animal feedings; single daily for 10 weeks | | Result: | Decreased the blood glucose level from the second weekand persisted through the 10-week treatment, when at 300 mg/kg.
Significantly reduced HbA1c level when dosage at 300 mg/kg.
Significantly decreased 6 h-fasted blood glucose levels in a dose-dependent manner. |
|
| Clinical Trial | |
| 分子量 | |
| 性状 | |
| Formula | |
| CAS 号 | |
| 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: DMSO : 100 mg/mL(181.32 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.8132 mL | 9.0660 mL | 18.1320 mL | | 5 mM | 0.3626 mL | 1.8132 mL | 3.6264 mL | | 10 mM | 0.1813 mL | 0.9066 mL | 1.8132 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： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.53 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 (4.53 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.53 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。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (4.53 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (4.53 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 25.0 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。
|
m.cnreagent.com