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西他列汀,Sitagliptin;≥98% (HPLC)

别名:西他列丁;磷酸西他列汀;(3R)-3-氨基-1-[3-(三氟甲基)-5,6,7,8-四氢-1,2,4-三唑并[4,3-a]吡嗪-7-基]-4-(2,4,5-三氟苯基)丁-1-酮;(2R)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophenyl)butan-2-amine, (3R)-3-Amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a ]pyrazin-7(8H )-yl]-4-(2,4,5-trifluorophenyl)-1-butanone,, MK 0431 free base, MK 431 free base, MK-0431 free base, MK-431 free base, MK0431 free base, MK431 free base

Empirical Formula (Hill Notation): C16H15F6N5O CAS号: 486460-32-6 分子量: 407.31 MDL编号: MFCD09838015
制造商品牌: 西格玛 Sigma-Aldrich
货号(SKU): SML3205
CAS号: 486460-32-6
MDL号: MFCD09838015
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¥1,576.00

说明

西他列汀是一种口服活性,有效和选择性的二肽基肽酶IV(DPP4;DPP-IV)抑制剂(IC50=18 nM),具有优于其他脯氨酸选择性肽酶的选择性(IC50=48μM/DPP8,>100μM/DPP9&QPP)。西他列汀改善瘦小鼠的葡萄糖耐量(在葡萄糖激发前60分钟用0.1或3mg西他列汀/kg口服5g右旋糖/kg后血糖降低23%和55%)和DIO小鼠(68%和90由于DPP-IV抑制和体内血液中GLP-1水平上调,2g右旋糖/kg后血糖降低%,0.3或3mg西他列汀/kg口服)。

生化/生理作用

Sitagliptin is an orally active, potent and selective dipeptidyl peptidase IV (DPP4; DPP-IV) inhibitor (IC50 = 18 nM) with excellent selectivity over other proline-selective peptidases (IC50 = 48 μM/DPP8, >100 μM/DPP9 & QPP). Sitagliptin improves glucose tolerance in lean mice (23% and 55% reduction of blood glucose post 5 g dextrose/kg with 0.1 or 3 mg Sitagliptin/kg p.o. 60 min prior to dextrose challenge) and in DIO mice (68% and 90% reduction of blood glucose post 2 g dextrose/kg with 0.3 or 3 mg Sitagliptin/kg p.o.) as a result of DPP-IV inhibition and upregulated GLP-1 level in blood in vivo.
 
 

属性

质量水平

100

测定

≥98% (HPLC)

形式

powder

旋光性

[α]/D -17 to -23°, c = 0.5 in chloroform-d

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

−20°C

 

安全信息

象形图

Exclamation markHealth hazard

警示用语:

Warning

危险声明

危险分类

Eye Irrit. 2 - STOT RE 2

靶器官

Liver

储存分类代码

11 - Combustible Solids

WGK

WGK 3

商品规格
属性名称属性值
储存温度 Storage temp.-20°C低温冷冻
全球实时库存 Availability √美国St. Louis ≥ 99 | 欧洲Eur. ≥ 10 | 東京Tokyo ≥ 22 | 香港与北京 ≥ 32
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