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Evogliptin tartrate

    级别和纯度:
  • ≥99%
有货

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货号 (SKU) 包装规格 是否现货 价格 数量
E646233-5mg
5mg 期货 Stock Image
E646233-10mg
10mg 期货 Stock Image
E646233-25mg
25mg 期货 Stock Image
E646233-50mg
50mg 期货 Stock Image
E646233-100mg
100mg 期货 Stock Image

基本描述

别名 酒石酸依沃列汀
英文别名 (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-[(2-methylpropan-2-yl)oxymethyl]piperazin-2-one;(2R,3R)-2,3-dihydroxybutanedioic acid | DA-1229 (tartrate) | Evogliptin tartrate [WHO-DD] | R14RT6A3LK | Evogliptin (tartrate) | 1222102-51-3 | 2-Pip
规格或纯度 ≥99%
英文名称 Evogliptin tartrate
生化机理 酒石酸埃沃格列汀(DA-1229)是一种口服活性 DPP4 抑制剂,在小鼠模型中具有显著和持续的降血糖作用。酒石酸埃沃格列汀还能通过诱导肝细胞自噬,抑制肝细胞中炎症和纤维化信号的产生。
储存温度 2-8°C储存,干燥
运输条件 冰袋运输
作用类型 抑制剂
产品介绍


Evogliptin (DA-1229) tartrate is an orally active DPP4 inhibitor with significant and sustained hypoglycaemic effects in mouse models. Evogliptin tartrate also inhibits the production of inflammatory and fibrotic signals in hepatocytes by inducing autophagy . Evogliptin tartrate can be used in studies of type 2 diabetes, osteoporosis, renal impairment and chronic liver inflammation

In Vitro

Evogliptin tartrate (2.49 mM; 12 h) efficiently inhibits mDPP4 (membrane DPP4) enzymatic activity in PWM-induced H9 Th1 cells. Evogliptin tartrate prevents inflammatory and fibrotic signaling through autophagy induction in primary hepatocytes of ATG7 f/f -Cre + mice. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Viability AssayCell Line: H9 Th1 cells (pokeweed mitogen (PWM)-induced) Concentration: 2.49 mM (1 µg/mL) Incubation Time: 12 h Result: Potently inhibited mDPP4 (membrane DPP4) activity in a dose-dependent manner but did not affect either the cytokine profile or cell viability in PWM-activated CD4 + CD26 + H9 Th1 cells.

In Vivo

Evogliptin tartrate (100, 300 mg/kg; in animal feedings; single daily for 10 weeks) exhibits antidiabetic effects on HFD/STZ mice and improves glucose intolerance and insulin resistance. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male ICR mice (four-week-old; HFD/STZ mice model). Dosage: 100, 300 mg/kg Administration: In animal feedings; single daily for 10 weeks Result: Decreased the blood glucose level from the second weekand persisted through the 10-week treatment, when at 300 mg/kg. Significantly reduced HbA1c level when dosage at 300 mg/kg. Significantly decreased 6 h-fasted blood glucose levels in a dose-dependent manner.

Form:Solid

IC50& Target:DPP-4

纯度 ≥99%

名称和识别符

IIUPAC Name (3R)-4-[(3R)-3-amino-4-(2,4,5-trifluorophenyl)butanoyl]-3-[(2-methylpropan-2-yl)oxymethyl]piperazin-2-one;(2R,3R)-2,3-dihydroxybutanedioic acid
INCHI 1S/C19H26F3N3O3.C4H6O6/c1-19(2,3)28-10-16-18(27)24-4-5-25(16)17(26)8-12(23)6-11-7-14(21)15(22)9-13(11)20;5-1(3(7)8)2(6)4(9)10/h7,9,12,16H,4-6,8,10,23H2,1-3H3,(H,24,27);1-2,5-6H,(H,7,8)(H,9,10)/t12-,16-;1-,2-/m11/s1
InChi Key RBBXDAJRSNHIJZ-DLDKMZOSSA-N
Smiles CC(C)(C)OCC1C(=O)NCCN1C(=O)CC(CC2=CC(=C(C=C2F)F)F)N.C(C(C(=O)O)O)(C(=O)O)O
Isomeric SMILES CC(C)(C)OC[C@@H]1C(=O)NCCN1C(=O)C[C@@H](CC2=CC(=C(C=C2F)F)F)N.[C@@H]([C@H](C(=O)O)O)(C(=O)O)O
PubChem CID 135395528
分子量 401.4215009

化学和物理性质

溶解性 DMSO : 100 mg/mL (181.32 mM; Need ultrasonic)

质检证书(CoA,COO,BSE/TSE 和分析图谱)

C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:

溶液计算器