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

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

For research use only. We do not sell to patients.

UAMC00039 dihydrochloride Chemical Structure

UAMC00039 dihydrochloride Chemical Structure

CAS No. : 697797-51-6

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 111 In-stock
Solution
10 mM * 1 mL in DMSO USD 111 In-stock
Solid
2 mg USD 66 In-stock
5 mg USD 133 In-stock
10 mg USD 200 In-stock
25 mg USD 400 In-stock
50 mg USD 600 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE UAMC00039 dihydrochloride

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

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]

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].

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

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].

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

Molecular Weight

382.76

Formula

C16H26Cl3N3O

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N1CCCCC1)[C@@H](N)CCNCC2=CC=C(Cl)C=C2.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
In Vitro: 

DMSO : ≥ 150 mg/mL (391.89 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 100 mg/mL (261.26 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 100 mg/mL (261.26 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation
References
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.

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    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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Product Name:
UAMC00039 dihydrochloride
Cat. No.:
HY-101769
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