UAMC00039 dihydrochloride

Name: UAMC00039 dihydrochloride
Brand: MedChemExpress
SKU: HY-101769
Rating: 4.5 (1 reviews)

Cat. No.: HY-101769 Purity: 99.81%: FAQs
Data Sheet SDS COA Handling Instructions

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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

CAS No. : 697797-51-6

Size	Price	Stock	Quantity
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 111	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 111	In-stock	Estimated Time of Arrival: December 31
Solid
2 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 132	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 880	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1540	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

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.

697797-51-6

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
10 mM	0.2613 mL	1.3063 mL	2.6126 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.

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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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)

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

Purity: 99.81%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (246 KB) LCMS (87 KB)

Handling Instructions (2659 KB)

References

[1]. Maes MB, et al. In vivo effects of a potent, selective DPPII inhibitor: UAMC00039 is a possible tool for the elucidation of the physiological function of DPPII. Adv Exp Med Biol. 2006;575:73-85. [Content Brief]

[2]. Maes MB, et al. Dipeptidyl peptidase II and leukocyte cell death. Biochem Pharmacol. 2006 Jun 28;72(1):70-9. [Content Brief]

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	[1]. Maes MB, et al. In vivo effects of a potent, selective DPPII inhibitor: UAMC00039 is a possible tool for the elucidation of the physiological function of DPPII. Adv Exp Med Biol. 2006;575:73-85. [Content Brief] [2]. Maes MB, et al. Dipeptidyl peptidase II and leukocyte cell death. Biochem Pharmacol. 2006 Jun 28;72(1):70-9. [Content Brief]

Complete Stock Solution Preparation Table

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.