1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase
  3. UAMC00039 dihydrochloride

UAMC00039 dihydrochloride 

目录号: HY-101769 纯度: 99.81%
COA 产品使用指南

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

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UAMC00039 dihydrochloride Chemical Structure

UAMC00039 dihydrochloride Chemical Structure

CAS No. : 697797-51-6

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     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1010
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2 mg ¥800
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5 mg ¥1200
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10 mg ¥1800
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25 mg ¥4000
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50 mg ¥7200
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200 mg   询价  

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查看 Dipeptidyl Peptidase 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.

IC50 & Target

IC50: 0.48 nM (DPPII)[1]; Ki: 0.082 nM (DPPII)[2]

体外研究
(In Vitro)

UAMC00039 has an IC50 of 0.48±0.04 nM and a high selectivity for DPPII compared to DPPIV (IC50=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[1]. 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%[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

382.76

Formula

C16H26Cl3N3O

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 150 mg/mL (391.89 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : 100 mg/mL (261.26 mM; 超声助溶)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6126 mL 13.0630 mL 26.1260 mL
5 mM 0.5225 mL 2.6126 mL 5.2252 mL
查看完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

以下溶解方案,请直接配置工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: PBS

    Solubility: 100 mg/mL (261.26 mM); 澄清溶液; 超声助溶

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献
Kinase Assay
[2]

Stability of UAMC00039 in RPMI medium or assay buffer (50 mM cacodylate buffer pH5.5) is monitored at 37 °C. The inhibitors’ capacity (IC50) to inhibit DPPII is measured at different time points (up to 48 h). U937 cells are incubated with various concentrations of UAMC00039 for 15 min at 37 °C in RPMI. Cells are then ished with PBS, lysed and assayed for DPPII activity. Concentration–response and time–response curves are generated from incubations of PBMC with UAMC00039 (0.01 nM–1 μM) in RPMI at 37 °C for 1, 5, 15, 30 and 60 min. Ished cells are lysed overnight at 4 °C using 100 mM HEPES buffer pH 7.4, 10 mM EDTA, 70 μg/mL aprotinin and 1% octylglucoside[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Rats: UAMC00039 is administered orally at 2 mg/kg (-5 µmol/kg in a vehicle of 2% tween 80, 10 mL/kg) on a blind basis in all in vivo assays. For each assay, a reference compound and vehicle control is analyzed concurrently. For the in vivo studies 3 to 5 animals per condition are tested[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

UAMC00039 dihydrochloride 相关分类

完整储备液配制表

* 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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.6126 mL 13.0630 mL 26.1260 mL 65.3151 mL
5 mM 0.5225 mL 2.6126 mL 5.2252 mL 13.0630 mL
10 mM 0.2613 mL 1.3063 mL 2.6126 mL 6.5315 mL
15 mM 0.1742 mL 0.8709 mL 1.7417 mL 4.3543 mL
20 mM 0.1306 mL 0.6532 mL 1.3063 mL 3.2658 mL
25 mM 0.1045 mL 0.5225 mL 1.0450 mL 2.6126 mL
30 mM 0.0871 mL 0.4354 mL 0.8709 mL 2.1772 mL
40 mM 0.0653 mL 0.3266 mL 0.6532 mL 1.6329 mL
50 mM 0.0523 mL 0.2613 mL 0.5225 mL 1.3063 mL
60 mM 0.0435 mL 0.2177 mL 0.4354 mL 1.0886 mL
80 mM 0.0327 mL 0.1633 mL 0.3266 mL 0.8164 mL
100 mM 0.0261 mL 0.1306 mL 0.2613 mL 0.6532 mL

* 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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产品名称:
UAMC00039 dihydrochloride
目录号:
HY-101769
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