P32/98 (hemifumarate) |
| カタログ番号GC14786 |
P32/98 (ヘミフマレート) は、130 nM の Ki 値を持つジペプチジル ペプチダーゼ IV の強力な阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 251572-86-8
Sample solution is provided at 25 µL, 10mM.
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Ki: 126 nM
P32/98 (hemifumarate) is an inhibitor of DPP IV.
Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) are responsible for >50% of nutrient-stimulated insulin secretion. After being released into the circulation, GIP and GLP-1 are quickly inactivated by the circulating enzyme dipeptidyl peptidase IV (DPP IV).
In vitro: P32/98 was found to be able to block adipogenesis dose-dependently, starting at the concentration of 100 μM, and P32/98 could completely block adipogenesis in 3T3-L1 cell line at 500 μM concentration. In addition, the inhibitory effects of P32/98 was further confirmed by detecting the expression of adipocyte markers at the end of differentiation [1].
In vivo: In previou animal study, two groups of fa/fa Zucker rats were orally treated twice daily for three months with P32/98 at 20 mg/kg/day and monthly oral glucose tolerance tests (OGTTs) were conducted after drug washout. Results showed that after 12 weeks of P32/98 treatment, the peak OGTT blood glucose values in the treated rats averaged 8.5 mmol/l less than in the controls. In addition, the concomitant insulin resulted in an increased early-phase insulin response in the treated group. Moreover, in response to an 8.8 mmol/l glucose perfusion, pancreata from controls showed no increase in insulin secretion, while pancreata from P32/98-treated animals had a 3.2-fold rise in insulin secretion [2].
Clinical trial: Up to now, P32/98 is still in the preclinical development stage.
References:
1. Han R, Wang X, Bachovchin W, Zukowska Z, Osborn JW. Inhibition of dipeptidyl peptidase 8/9 impairs preadipocyte differentiation. Sci Rep. 2015 Aug 5;5:12348.
2. J. A. Pospisilik, S. G. Stafford, H. U. Demuth, et al. Long-term treatment with the dipeptidyl peptidase IV inhibitor P32/98 causes sustained improvements in glucose tolerance, insulin sensitivity, hyperinsulinemia, and β-cell glucose responsiveness in VDF (fa/fa) zucker rats. Diabetes 51, 943-950 (2002).
| Cas No. | 251572-86-8 | SDF | |
| Chemical Name | (2S,3S)-2-amino-3-methyl-1-(3-thiazolidinyl)-1-pentanone, (2E)-2-butenedioate | ||
| Canonical SMILES | O=C([C@@H](N)[C@@H](C)CC)N1CCSC1.OC(/C=C/C(O)=O)=O | ||
| Formula | C9H18N2OS • 1/2C4H4O4 | M.Wt | 260.4 |
| 溶解度 | ≤1mg/ml in ethanol;15mg/ml in DMSO;5mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.8402 mL | 19.2012 mL | 38.4025 mL |
| 5 mM | 0.768 mL | 3.8402 mL | 7.6805 mL |
| 10 mM | 0.384 mL | 1.9201 mL | 3.8402 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 7 reference(s) in Google Scholar.)
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