UAMC 00039 DIHYDROCHLORIDE

中文名称:

UAMC 00039 DIHYDROCHLORIDE

中文同义词:

DIPEPTIDYL PEPTIDASE II抑制剂;化合物UAMC 00039 DIHYDROCHLORIDE

英文名称:

UAMC 00039 dihydrochloride

英文同义词:

UAMC 00039 dihydrochloride;UAMC00039 2HCl;UAMC 0039 (hydrochloride);(2S)-2-Amino-4-[[(4-chlorophenyl)methyl]amino]-1-(1-piperidinyl)-1-butanone dihydrochloride;UAMC00039;UAMC 00039;UAMC-00039;UAMC00039 DIHYDROCHLORIDE, >98%;UAMC00039dihydrochloride, >98%

CAS号:

697797-51-6

分子式:

C16H25Cl2N3O

分子量:

346.3

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

697797-51-6.mol

储存条件 

Inert atmosphere,Store in freezer, under -20°C

生物活性

UAMC00039 dihydrochloride是高效，可逆，竞争性的dipeptidyl peptidase II抑制剂，IC50值为0.48 nM。

靶点

IC50: 0.48 nM (DPPII); Ki: 0.082 nM (DPPII)

体外研究

UAMC00039 has an IC 50 of 0.48±0.04 nM and a high selectivity for DPPII compared to DPPIV (IC 50 =165±9 µM) and DPP activity not caused by DPPII or DPPIV. UAMC00039 seems a promising tool to unravel the function of DPPII as well as to validate its potential as a therapeutic target. The efficacy of a DPPII inhibitor in cell culture depends not only on the inhibitors’ potency towards the enzyme but also on its stability in the medium and its ability to enter the cell. UAMC00039 is stable for at least 48 h at 37 °C in culture medium and in DPPII assay buffer. The compound is able to enter PBMC within 1 min resulting in a concentration-dependent inhibition of intracellular DPPII activity without affecting the ‘non-DPPII’ DPP activity. 1 and 100 μM UAMC00039 inhibits DPPII activity of PBMC and U937 cells more than 90%.

体内研究

A dose dependent inhibition of DPPII but not of DPPIV is observed in the peripheral organs of both the rats and the mice (after oral administration) and the rabbits (after IV administration). UAMC00039 tested orally at 2 mg/kg does not cause signs of acute toxicity and does not cause any significant changes in the following functions that are evaluated: general behaviour, body temperature, respiration, bleeding time, blood pressure, urine volume, liver function, fasting glucose and gastrointestinal parameters like acidity, motility and irritation.