Gemigliptin tartrate (Synonyms:LC15-0444 tartrate)
目录号 : KM9419 CAS No. : 1374639-74-3 纯度 : 98%

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。

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10mg
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生物活性

Gemigliptin tartrate (LC15-0444 tartrate) 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 tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications.

体外研究

Gemigliptin tartrate dose-dependently inhibits the formation of AGE-BSA with IC50 of 11.69 mM.
Gemigliptin tartrate dose-dependently suppresses the cross-linking of preformed AGE-BSA with rat tail tendon collagen with an IC50 of 1.39 mM.
Gemigliptin tartrate is a competitive DPP-4 inhibitor with a Ki of 7.25 nM.

体内研究

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

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.
分子式
C22H25F8N5O8
分子量
639.45
CAS号
1374639-74-3
中文名称
吉格列汀酒石酸盐
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
溶解性数据
In Vitro: 

DMSO : 100 mg/mL (156.38 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
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°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 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-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

临床试验
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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