Physicochemical Properties
| Molecular Formula | C22H40N4O6S2 |
| Molecular Weight | 520.704 |
| Exact Mass | 520.238 |
| CAS # | 251572-86-8 |
| Related CAS # | P32/98;136259-20-6 |
| Appearance | Typically exists as solid at room temperature |
| SMILES | C(/C(=O)O)=C\C(=O)O.C(N1CSCC1)(=O)[C@@H](N)[C@@H](C)CC |
| Chemical Name | (2S,3S)-2-amino-3-methyl-1-(thiazolidin-3-yl)pentan-1-one hemifumarate |
| Synonyms | P-3298 hemi-fumarateP3298 P32/98 P-3298 P 3298 |
| HS Tariff Code | 2934.99.9001 |
| Storage |
Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| ln Vitro | GLP-1's primary renal catabolic route is DPPIV, and it serves to both promote satiety and glucose-dependent insulin secretion in the body [2]. In pig proximal tubular cells, P32/98 hemifumarate and 200 pM GLP-1 (10 μM; 3 hours) do not significantly decrease salt reabsorption [2]. The mRNA expression of GLP-1R, DPPIV, Na+/H+ exchanger 3 (NHE3), and sodium-dependent glucose transporters slc5a1, slc5a2 (SGLT1, 2) is unaffected by P32/98 hemifumarate (10 μM; 96 hours). |
| ln Vivo | Zucker diabetic obese rats (IGT; impaired glucose tolerance model) can greatly increase their glucose tolerance with long-term treatment with P32/98 hemifumarate (25 mg/kg; i.e., once daily) [3]. |
| Cell Assay |
Cytotoxicity assay[2] Cell Types: Porcine proximal tubular cells Tested Concentrations: 10 μM Incubation Duration: 96 hrs (hours) Experimental Results: No toxicity. |
| Animal Protocol |
Animal/Disease Models: Zucker diabetic fat rats [3] Doses: 25 mg/kg Route of Administration: po (oral gavage); one time/day Experimental Results: Dramatically improved glucose tolerance in Zucker diabetic fat rats. |
| References |
[1]. Efficacy of the dipeptidyl peptidase IV inhibitor isoleucine thiazolidide (P32/98) in fatty Zucker rats with incipient and manifest impaired glucose tolerance. Diabetes Obes Metab. 2008;10(10):850-861. [2]. Glucagon-like peptide 1 receptor expression in primary porcine proximal tubular cells. Regul Pept. 2007 Jun 7;141(1-3):120-8. [3]. Improvement of glucose tolerance in Zucker diabetic fatty rats by long-term treatment with the dipeptidyl peptidase inhibitor P32/98: comparison with and combination with rosiglitazone. Diabetes Obes Metab. 2005;7(2):170-181. |
Solubility Data
| Solubility (In Vitro) | May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples |
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples. Injection Formulations (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9205 mL | 9.6025 mL | 19.2049 mL | |
| 5 mM | 0.3841 mL | 1.9205 mL | 3.8410 mL | |
| 10 mM | 0.1920 mL | 0.9602 mL | 1.9205 mL |