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Gemigliptin tartrate Sale

(Synonyms: 吉格列汀酒石酸盐,LC15-0444 tartrate) 目录号 : GC60871

A DPP-4 inhibitor

Gemigliptin tartrate Chemical Structure

Cas No.:1374639-74-3

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥1,089.00
现货
10mg
¥990.00
现货
50mg
¥2,970.00
现货
100mg
¥4,680.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

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)

化学性质

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。
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。

溶解性数据

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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
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