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NVP DPP 728 dihydrochloride

DPP-IV inhibitor CAS# 247016-69-9

NVP DPP 728 dihydrochloride

Catalog No. BCC2365----Order now to get a substantial discount!

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NVP DPP 728 dihydrochloride: 5mg $104 In Stock
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Quality Control of NVP DPP 728 dihydrochloride

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Chemical structure

NVP DPP 728 dihydrochloride

3D structure

Chemical Properties of NVP DPP 728 dihydrochloride

Cas No. 247016-69-9 SDF Download SDF
PubChem ID 22318679 Appearance Powder
Formula C15H20Cl2N6O M.Wt 371.27
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO > 10 mM
Chemical Name 6-[2-[[2-(2-cyanopyrrolidin-1-yl)-2-oxoethyl]amino]ethylamino]pyridine-3-carbonitrile;dihydrochloride
SMILES C1CC(N(C1)C(=O)CNCCNC2=NC=C(C=C2)C#N)C#N.Cl.Cl
Standard InChIKey VNACOBVZDCLAEV-UHFFFAOYSA-N
Standard InChI InChI=1S/C15H18N6O.2ClH/c16-8-12-3-4-14(20-10-12)19-6-5-18-11-15(22)21-7-1-2-13(21)9-17;;/h3-4,10,13,18H,1-2,5-7,11H2,(H,19,20);2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of NVP DPP 728 dihydrochloride

DescriptionNVP DPP 728 dihydrochloride is a potent and orally active inhibitor of dipeptidyl peptidase (DPP)-IV with Ki and IC50 values of 11 nM and 14 nM, respectively.
TargetsDPP-IV    
IC5014 nM (Ki = 11 nM)     

NVP DPP 728 dihydrochloride Dilution Calculator

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NVP DPP 728 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of NVP DPP 728 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6935 mL 13.4673 mL 26.9346 mL 53.8692 mL 67.3364 mL
5 mM 0.5387 mL 2.6935 mL 5.3869 mL 10.7738 mL 13.4673 mL
10 mM 0.2693 mL 1.3467 mL 2.6935 mL 5.3869 mL 6.7336 mL
50 mM 0.0539 mL 0.2693 mL 0.5387 mL 1.0774 mL 1.3467 mL
100 mM 0.0269 mL 0.1347 mL 0.2693 mL 0.5387 mL 0.6734 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on NVP DPP 728 dihydrochloride

NVP DPP 728 dihydrochloride
Description:
Ki: Inhibit human DPP-IV amidolytic activity with a Ki of 11 nM [1]
Inhibitors of dipeptidyl peptidase 4, also known as DPP-4 inhibitors or gliptins, are a class of oral hypoglycemics that can be used to treat diabetes mellitus type 2. NVP DPP 728 dihydrochloride is a potent and orally active inhibitor of dipeptidyl peptidase (DPP)-IV.
In vitro: NVP-DPP728 was found to inhibit human DPP-IV amidolytic activity with a Ki of 11 nM, a kon value of 1.3 x 105 M-1 s-1, and a koff of 1.3 x 10-3 s-1. NVP-DPP728 inhibited DPP-IV in a manner consistent with a two-step inhibition mechanism. Taken together, these data suggest that NVP-DPP728 inhibits DPP-IV through formation of a novel, reversible, nitrile-dependent complex with transition state characteristics [1].
In vivo: Aging caused a decrease in early insulin response after an oral glucose challenge in aged Wistar or DPP-IV(+) F344 rats, but not in aged DPP-IV(-) F344 rats, compared with young control groups. Glucose tolerance after an oral glucose challenge in aged DPP-IV(-) F344 rats was better than in aged DPP-IV(+) F344 and Wistar rats associated with the preservation of the early insulin response. NVP-DPP728 improved the glucose tolerance after an oral glucose challenge by potentiating the early insulin response throughout the inhibition of plasma DPP-IV activity in aged DPP-IV(+) Wistar andF34 4 rats. In contrast, NVP-DPP728 did not affect the glucose tolerance after an oral glucose challenge in aged DPP-IV(-) F344 rats. These results indicate that treatment with NVP-DPP728 ameliorated glucose tolerance in aged rats by the direct inhibition of plasma DPP-IV activity and presumably the subsequent increase in endogenous incretin action [2].
Clinical trial: NVP-DPP728 is currently in the preclinical development and no clinical trial is ongoing.
Reference:
[1] Hughes TE, Mone MD, Russell ME, Weldon SC, Villhauer EB. NVP-DPP728 (1-[[[2-[(5-cyanopyridin-2-yl)amino]ethyl]amino]acetyl]-2-cyano-(S)-pyrrolidine), a slow-binding inhibitor of dipeptidyl peptidase IV. Biochemistry. 1999;38(36):11597-603.
[2] Mitani H, Takimoto M, Kimura M. Dipeptidyl peptidase IV inhibitor NVP-DPP728 ameliorates early insulin response and glucose tolerance in aged rats but not in aged Fischer 344 rats lacking its enzyme activity. Jpn J Pharmacol. 2002;88(4):451-8.

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