Gemigliptin LC15-0444|cas:911637-19-9|西域试剂

Gemigliptin LC15-0444

产品编号：Bellancom-14892| CAS NO：911637-19-9| 分子式：C₁₈H₁₉F₈N₅O₂| 分子量：489.36

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货号	价格	库存与货期
Bellancom-14892	￥1100.00	杭州北京（现货）
Bellancom-14892	￥3300.00	杭州北京（现货）
Bellancom-14892	￥5200.00	杭州北京（现货）

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Gemigliptin LC15-0444

产品介绍

Gemigliptin (LC15-0444) 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 具有很强的抗糖基化特性。Gemigliptin 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 (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC₅₀ of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications.

体外研究

Gemigliptin dose-dependently inhibits the formation of AGE-BSA with IC₅₀ of 11.69 mM.
Gemigliptin dose-dependently suppressed the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC₅₀ of 1.39 mM.
Gemigliptin is a competitive inhibitor with a K_i of 7.25 nM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

Gemigliptin (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo.
Gemigliptin dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/KsJ-db/db mice (7 weeks old)
Dosage:	100 mg/kg
Administration:	Oral gavage, daily, for 12 weeks
Result:	Significantly reduced circulating AGE levels by 44.5% in serum.

体内研究

Gemigliptin (100 mg/kg; i.g.; daily; for 12 weeks) inhibits AGEs formation and AGE cross-links in vivo.
Gemigliptin dose-dependently inhibits plasma DPP-4 activity in rats, dogs, and monkeys.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male C57BL/KsJ-db/db mice (7 weeks old)
Dosage:	100 mg/kg
Administration:	Oral gavage, daily, for 12 weeks
Result:	Significantly reduced circulating AGE levels by 44.5% in serum.

性状

溶解性数据

In Vitro:

DMSO : 50 mg/mL (102.17 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0435 mL	10.2174 mL	20.4349 mL
5 mM	0.4087 mL	2.0435 mL	4.0870 mL
10 mM	0.2043 mL	1.0217 mL	2.0435 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 (5.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.11 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。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.11 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.11 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明