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Merck
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文件

SML3205

Sigma-Aldrich

Sitagliptin

≥98% (HPLC)

别名:

(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

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About This Item

经验公式（希尔记法）:
C16H15F6N5O
CAS号:
486460-32-6
分子量:
407.31
MDL號碼:
MFCD09838015
分類程式碼代碼:
51111800
NACRES:
NA.77

品質等級

100

化驗

≥98% (HPLC)

形狀

powder

光學活性

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

顏色

white to beige

溶解度

DMSO: 2 mg/mL, clear

儲存溫度

−20°C

InChI

1S/C16H15F6N5O/c17-10-6-12(19)11(18)4-8(10)3-9(23)5-14(28)26-1-2-27-13(7-26)24-25-15(27)16(20,21)22/h4,6,9H,1-3,5,7,23H2/t9-/m1/s1

InChI 密鑰

MFFMDFFZMYYVKS-SECBINFHSA-N

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.

象形圖

Health hazardExclamation mark
GHS08,GHS07

訊號詞

Warning

危險聲明

H319,H373

危險分類

Eye Irrit. 2 - STOT RE 2

標靶器官

Liver

儲存類別代碼

11 - Combustible Solids

水污染物質分類（WGK）

WGK 3

閃點（°F）

Not applicable

閃點（°C）

Not applicable

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Heba A Habib et al.
Life sciences, 278, 119624-119624 (2021-05-19)
Diabetic nephropathy, a major threat to diabetic patients, is considered as the main reason for end-stage renal disease. Fortunately, incretin-based therapy has been aroused as considerable source to attenuate diabetic renal damage. This study aimed to investigate whether superior protective
Shuhei Kamada et al.
Oncogene, 40(22), 3899-3913 (2021-05-12)
Tyrosine kinase inhibitors (TKIs) are used as targeted drugs for advanced renal cell carcinoma (RCC), although most cases eventually progress by acquiring resistance. Cancer stemness plays critical roles in tumor aggressiveness and therapeutic resistance, and dipeptidyl peptidase IV (DPP4) has
Mohamed Abouelkheir
Current molecular pharmacology (2021-06-03)
We previously tested two angiotensin-converting enzyme (ACE) inhibitors and two dipeptidyl peptidase-4 (DPP-4) inhibitors for dual enzyme inhibitory effect. Only two DPP-4 inhibitors, linagliptin and sitagliptin, were able to inhibit ACE. In the present study, we investigated if other inhibitors
Rui Li et al.
Frontiers in oncology, 11, 679816-679816 (2021-06-15)
Cancer has been as one of common comorbidities of diabetes. Long-term antidiabetic treatment may potentially exert uncertain impacts on diabetic patients with cancer including breast cancer (BC). Dipeptidyl peptidase-4 inhibitors (DPP-4i) are currently recommended by the AACE as first-line hypoglycemic
Soraya Mehrdoost et al.
Iranian journal of basic medical sciences, 24(4), 451-459 (2021-06-08)
Fatty liver disease (FLD) is a disorder related to accumulation of excess fat within the hepatocytes. In this study, the effects of Berberine, a natural compound, and Sitagliptin as a DPP-4 inhibitor, were observed in a rat model of FLD.
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