| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
PTP1B[1]
PTP1B (protein tyrosine phosphatase 1B). PTP1B-IN-15 is a potent and selective inhibitor of PTP1B. It blocks the dephosphorylation of the insulin receptor and leptin receptor, enhancing insulin sensitivity and energy metabolism. |
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| ln Vitro |
PTP1B-IN-15 inhibits PTP1B enzymatic activity in vitro, blocking the dephosphorylation of the insulin receptor (IR) and its downstream substrates. By preventing PTP1B-mediated negative regulation of insulin signaling, it enhances insulin receptor phosphorylation and AKT activation. This leads to improved glucose uptake and insulin sensitivity in cell-based assays.
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| ln Vivo |
In vivo, PTP1B-IN-15 has research potential for type II diabetes and obesity. By inhibiting PTP1B in liver, muscle, and adipose tissue, it improves glucose tolerance, reduces blood glucose levels, and enhances insulin sensitivity in animal models. It may also promote energy expenditure and reduce body weight by enhancing leptin signaling. Further in vivo studies are needed to fully characterize its efficacy.
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| Enzyme Assay |
For non-cellular assays, recombinant human PTP1B is incubated with a fluorogenic substrate such as DiFMUP (6,8-difluoro-4-methylumbelliferyl phosphate) in assay buffer (50 mM Tris-HCl, pH 7.5, 1 mM DTT, 1 mM EDTA). PTP1B-IN-15 is added at varying concentrations (0.1-100 uM). Fluorescence is measured (excitation 360 nm, emission 460 nm), and IC50 values are calculated from dose-response curves. Selectivity is assessed against other phosphatases.
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| Cell Assay |
For cell-based assays, hepatocytes (e.g., HepG2) or myotubes are treated with PTP1B-IN-15 (0.5-50 uM) for 2-24 hours, then stimulated with insulin. Insulin receptor (IR) and AKT phosphorylation are measured by Western blot using phospho-specific antibodies. Glucose uptake is assessed using 2-deoxyglucose assays. Cellular PTP1B activity in lysates is measured using fluorogenic substrates. Adipocyte differentiation and lipid accumulation can also be assessed.
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| Animal Protocol |
For animal studies, PTP1B-IN-15 is administered orally or intraperitoneally to mouse models of type 2 diabetes (e.g., db/db mice, ob/ob mice, or diet-induced obesity models). Doses typically range from 10-50 mg/kg once daily. Glucose tolerance tests (GTT) and insulin tolerance tests (ITT) are performed. Blood glucose, insulin, and leptin levels are measured. Body weight and food intake are monitored. Liver and muscle tissues are collected for analysis of insulin signaling markers.
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| ADME/Pharmacokinetics |
PTP1B-IN-15 is orally bioavailable with favorable pharmacokinetic properties. It can be formulated in 0.5% methylcellulose or other oral vehicles for in vivo administration. Detailed PK parameters (half-life, Cmax, AUC) are likely available in the literature from preclinical studies. The compound should be stored at -20degC and protected from light.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for PTP1B-IN-15 are limited. In animal studies at therapeutic doses (10-50 mg/kg), no significant systemic toxicity or body weight loss has been reported. As an investigational research compound, it should be handled following standard safety protocols. It is not intended for human therapeutic use without further development.
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| References | |
| Additional Infomation |
PTP1B-IN-15 (CAS: 765317-71-3) is a potent and selective PTP1B inhibitor with research potential for type II diabetes and obesity. PTP1B is a well-validated target for metabolic diseases, and selective inhibitors are being pursued as potential therapies. It is not approved for clinical use and is intended for research applications only.
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| Molecular Formula |
C19H17BR2NO5S
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|---|---|
| Molecular Weight |
531.21
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| Exact Mass |
528.919
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| CAS # |
765317-71-3
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| PubChem CID |
448660
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| Appearance |
White to off-white solid powder
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| LogP |
5.787
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
670
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC1=C(C2=C(O1)C=C(C=C2)S(=O)(=O)N(C)C)C(=O)C3=CC(=C(C(=C3)Br)O)Br
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| InChi Key |
FEYGJZKVMASWJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17Br2NO5S/c1-4-15-17(18(23)10-7-13(20)19(24)14(21)8-10)12-6-5-11(9-16(12)27-15)28(25,26)22(2)3/h5-9,24H,4H2,1-3H3
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| Chemical Name |
3-(3,5-dibromo-4-hydroxybenzoyl)-2-ethyl-N,N-dimethyl-1-benzofuran-6-sulfonamide
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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 |
| 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: 250 mg/mL (470.62 mM)
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| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8825 mL | 9.4125 mL | 18.8249 mL | |
| 5 mM | 0.3765 mL | 1.8825 mL | 3.7650 mL | |
| 10 mM | 0.1882 mL | 0.9412 mL | 1.8825 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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