Gemigliptin tartrate (LC15-0444 tartrate) 是一种高度选择性的，可逆的，竞争性的二肽基肽酶 4 (DPP-4) 抑制剂，对人重组 DPP-4 作用的IC50值为 10.3 nM。Gemigliptin tartrate 具有很强的抗糖基化特性。Gemigliptin tartrate 可用于晚期糖基化终产物 (AGE) 相关的糖尿病并发症的研究。
| 生物活性 | Gemigliptin tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with anIC50of 10.3 nM for human recombinantDPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications[1][2]. |
| IC50& Target | IC50: 10.3 nM (human recombinant DPP-4)[2] |
体外研究
(In Vitro) | Gemigliptin tartrate dose-dependently inhibits the formation of AGE-BSA with IC50of 11.69 mM[1].
Gemigliptin tartrate dose-dependently suppresses the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50of 1.39 mM[1].
Gemigliptin tartrate is a competitive DPP-4 inhibitor with a Kiof 7.25 nM[2].
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体内研究
(In Vivo) | Gemigliptin tartrate (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo[1].
Gemigliptin tartrate dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys[2].
| Animal Model: | Male C57BL/KsJ-db/db mice (7 weeks old)[1] | | Dosage: | 100 mg/kg | | Administration: | Oral gavage, daily, for 12 weeks | | Result: | Significantly reduced circulating AGE levels by 44.5% in serum. |
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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: DMSO : 100 mg/mL(156.38 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.5638 mL | 7.8192 mL | 15.6384 mL | | 5 mM | 0.3128 mL | 1.5638 mL | 3.1277 mL | | 10 mM | 0.1564 mL | 0.7819 mL | 1.5638 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 (3.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.91 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 (3.91 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.91 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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