Gemigliptin tartrate
(Synonyms: 吉格列汀酒石酸盐,LC15-0444 tartrate) 目录号 : GC60871A DPP-4 inhibitor
Cas No.:1374639-74-3
Sample solution is provided at 25 µL, 10mM.
Gemigliptin is an inhibitor of dipeptidyl peptidase 4 (DPP-4; IC50 = 0.01 ?M).1 It is selective for DPP-4 over DPP-8, DPP-9, and fibroblast activation protein-α (FAP-α; IC50s = 277.28, 233.72, 418.43 ?M, respectively). Gemigliptin inhibits DPP-4 activity in isolated human, rat, dog, and monkey plasma (IC50s = 11.5, 14.5, 14.5, and 14 nM, respectively). It scavenges methylglyoxal in vitro and inhibits advanced glycation end product (AGE) formation between BSA and methylglyoxal and cross-linking of AGE-BSA with rat tail tendon collagen (IC50s = 1.15, 11.69, and 1.39 mM, respectively).2 Gemigliptin (100 mg/kg) reduces the levels of circulating AGE and red blood cell IgG content in a db/db mouse model of diabetes when administered for 12 weeks. It decreases blood glucose and hemoglobin A1c (HbA1c) levels and reduces pancreatic β-cell damage in a dose-dependent manner in a mouse model of diabetes induced by a high-fat diet and streptozotocin .1 Gemigliptin also induces cytotoxicity in SW1736 and TPC-1 human thyroid cancer cells.3,4 Formulations containing gemigliptin have been used in the treatment of type 2 diabetes.
1.Kim, S.-H., Jung, E., Yoon, M.K., et al.Pharmacological profiles of gemigliptin (LC15-0444), a novel dipeptidyl peptidase-4 inhibitor, in vitro and in vivoEur. J. Pharmacol.78854-64(2016) 2.Jung, E., Kim, J., Kim, S.H., et al.Gemigliptin, a novel dipeptidyl peptidase-4 inhibitor, exhibits potent anti-glycation properties in vitro and in vivoEur. J. Pharmacol.74498-102(2014) 3.Kim, S.H., Kang, J.G., Kim, C.S., et al.Gemigliptin, a novel dipeptidyl peptidase-IV inhibitor, exerts a synergistic cytotoxicity with the histone deacetylase inhibitor PXD101 in thyroid carcinoma cellsJ. Endocrinol. Invest.41(6)677-689(2018) 4.Kim, S.H., Kang, J.G., Kim, C.S., et al.Synergistic cytotoxicity of the dipeptidyl peptidase-IV inhibitor gemigliptin with metformin in thyroid carcinoma cellsEndocrine59(2)383-394(2018)
Cas No. | 1374639-74-3 | SDF | |
别名 | 吉格列汀酒石酸盐,LC15-0444 tartrate | ||
Canonical SMILES | O=C(O)[C@H](O)[C@@H](O)C(O)=O.O=C1N(C[C@@H](N)CC(N2CCC3=C(C(F)(F)F)N=C(C(F)(F)F)N=C3C2)=O)CC(F)(F)CC1 | ||
分子式 | C22H25F8N5O8 | 分子量 | 639.45 |
溶解度 | DMSO: 100 mg/mL (156.38 mM) | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet