| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
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| 1g | |||
| Other Sizes |
| Targets |
PTP1B-IN-8 targets protein tyrosine phosphatase-1B (PTP1B), an enzyme that removes phosphate groups from tyrosine residues in proteins, thereby affecting signal transduction and cellular processes. By inhibiting PTP1B, it modulates insulin and leptin signaling pathways, making it a potential target for the treatment of type 2 diabetes and obesity.
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|---|---|
| ln Vitro |
In vitro, PTP1B-IN-8 demonstrates potent and selective inhibition of PTP1B. Its activity is confirmed in enzyme assays where it inhibits the dephosphorylation of PTP1B substrates. Specific IC50 values are not widely reported.
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| ln Vivo |
In vivo, PTP1B-IN-8 is used as a research tool to study the role of PTP1B in disease models. By inhibiting PTP1B, it can improve insulin sensitivity and glucose tolerance in animal models of type 2 diabetes.
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| Enzyme Assay |
The in vitro PTP1B enzyme assay involves incubating the enzyme with a phosphorylated peptide substrate in the presence of varying concentrations of PTP1B-IN-8. The amount of phosphate released is measured using a colorimetric or fluorometric method, and the IC50 is calculated from the inhibition curve.
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| Cell Assay |
In vitro cell-based assays for PTP1B-IN-8 utilize cells expressing PTP1B, such as hepatocytes or adipocytes. Cells are treated with the compound, and the phosphorylation of insulin receptor and its downstream signaling molecules is measured by Western blotting.
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| Animal Protocol |
In vivo animal experiments for PTP1B-IN-8 are performed in rodent models of type 2 diabetes, such as the db/db mouse or the high-fat diet-fed mouse. The compound is administered orally or intraperitoneally, and its effect on blood glucose levels and insulin sensitivity is assessed.
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| ADME/Pharmacokinetics |
PTP1B-IN-8 has a molecular weight of 413.12 g/mol and is soluble in DMSO. It is typically stored as a powder at -20°C for up to 3 years. In solution, it is stable at -20°C for 6 months.
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| Toxicity/Toxicokinetics |
Toxicological data for PTP1B-IN-8 are limited, as it is a research compound. It is not intended for human use. Standard safety precautions for handling chemical reagents should be followed.
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| References | |
| Additional Infomation |
PTP1B-IN-8 is a research compound with no clinical approval. It is a valuable tool for studying PTP1B biology and the role of PTP1B in insulin signaling and metabolism. It is used in drug discovery programs to explore the therapeutic potential of PTP1B inhibitors for the treatment of type 2 diabetes and obesity.
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| Molecular Formula |
C19H13CL4NO
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|---|---|
| Molecular Weight |
413.124621152878
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| Exact Mass |
412.972
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| CAS # |
919091-61-5
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| Related CAS # |
RAMB4;145888-79-5
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| PubChem CID |
5388806
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.463±0.06 g/cm3(Predicted)
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| Boiling Point |
607.5±55.0 °C(Predicted)
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| LogP |
5.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
516
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| Defined Atom Stereocenter Count |
0
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| SMILES |
N1C/C(=C\C2=CC=C(Cl)C(Cl)=C2)/C(=O)/C(=C/C2=CC=C(Cl)C(Cl)=C2)/C1
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| InChi Key |
GJPXGFGIFQWUOC-ACFHMISVSA-N
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| InChi Code |
InChI=1S/C19H13Cl4NO/c20-15-3-1-11(7-17(15)22)5-13-9-24-10-14(19(13)25)6-12-2-4-16(21)18(23)8-12/h1-8,24H,9-10H2/b13-5+,14-6+
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| Chemical Name |
(3E,5E)-3,5-bis[(3,4-dichlorophenyl)methylidene]piperidin-4-one
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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) |
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
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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 | 2.4206 mL | 12.1030 mL | 24.2060 mL | |
| 5 mM | 0.4841 mL | 2.4206 mL | 4.8412 mL | |
| 10 mM | 0.2421 mL | 1.2103 mL | 2.4206 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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