| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
Protein-tyrosine phosphatase 1B (PTP1B); a negative regulator of insulin and leptin signaling pathways.
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|---|---|
| ln Vitro |
DPM-1001 trihydrochloride suppresses PTP1B's short form reversibly, while PTP1B(1-405) stayed dormant for a long time. Without any pre-incubation, DPM-1001 is effective against PTP1B (1–405); the IC50 value for PTP1B (1–405) is 600 nM. Nevertheless, the potency is increased to 100 nM following a 30-min pre-incubation. On the other hand, the IC50 value for PTP1B(1-321) does not appear to vary with time [1].
DPM-1001 trihydrochloride inhibits PTP1B with an IC50 of 100 nM; it inhibits the short form of PTP1B reversibly, while PTP1B(1-405) remained inactive over an extended period. |
| ln Vivo |
DPM-1001 trihydrochloride (oral or intraperitoneal administration; 5 mg/kg; once daily; 50 days) prevents mice from becoming obese due to food by enhancing insulin and leptin signaling. After five days of therapy, mice fed a high-fat diet and treated with DPM-1001 trihydrochloride begin to lose weight. There is no more observed drop in body weight after the initial three weeks of weight loss[1].
Oral or intraperitoneal administration at 5 mg/kg once daily for 50 days prevents mice from becoming obese due to high-fat diet by enhancing insulin and leptin signaling; promotes weight loss and improves glucose homeostasis. |
| Enzyme Assay |
DPM-1001 trihydrochloride is an analog of MSI-1436; enzyme inhibition assays use recombinant PTP1B protein and a fluorescent substrate such as DiFMUP; IC50 determined by measuring dephosphorylation inhibition.
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| Cell Assay |
3T3-L1 adipocytes or hepatocytes are treated with DPM-1001 (0.1-10 microM) for 24 h; insulin-stimulated Akt phosphorylation is measured by Western blot; glucose uptake assessed by 2-deoxyglucose uptake assay.
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| Animal Protocol |
Animal/Disease Models: 18 weeks of age, high-fat diet (HFD)-fed obese male mice (C57bl6/J)
Doses: 5 mg/kg Route of Administration: Oral or intraperitoneal (ip)administration; 5 mg/kg; one time/day; 50 day Experimental Results: Led to an 5% decrease in body weight. Improved glucose tolerance and insulin sensitivity in glucose tolerance and insulin tolerance in vivo. Male C57BL/6J mice on high-fat diet are administered DPM-1001 trihydrochloride (5 mg/kg, oral or IP, once daily, for up to 50 days); body weight, food intake, glucose tolerance, and insulin sensitivity are monitored. |
| ADME/Pharmacokinetics |
As an orally active small molecule with favorable bioavailability; pharmacokinetic parameters not detailed; IP administration yields rapid absorption; oral formulation available as suspension in 0.5% CMC Na.
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| Toxicity/Toxicokinetics |
No dedicated toxicity data available; PTP1B inhibition is generally well-tolerated; standard safety pharmacology studies would be required for clinical development.
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| References | |
| Additional Infomation |
DPM-1001 trihydrochloride is an investigational anti-diabetic compound; not FDA/EMA approved for clinical use; for research use only in diabetes and obesity studies.
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| Molecular Formula |
C35H60CL3N3O3
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|---|---|
| Molecular Weight |
677.23
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| Related CAS # |
DPM-1001;1471172-27-6
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| Appearance |
Off-white to light yellow solid powder
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~80 mg/mL (~118.13 mM)
H2O :~33.33 mg/mL (~49.22 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (7.38 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (7.38 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. 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. View More
Solubility in Formulation 3: ≥ 5 mg/mL (7.38 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4766 mL | 7.3830 mL | 14.7660 mL | |
| 5 mM | 0.2953 mL | 1.4766 mL | 2.9532 mL | |
| 10 mM | 0.1477 mL | 0.7383 mL | 1.4766 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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