| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
PTP1B (protein tyrosine phosphatase 1B). CPT-157633 is a difluoro-phosphonomethyl phenylalanine analogue that acts as a potent PTP1B inhibitor, blocking the dephosphorylation of insulin receptor substrates.
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| ln Vitro |
CPT-157633 inhibits PTP1B enzymatic activity in vitro, blocking the dephosphorylation of the insulin receptor and its downstream substrates. By preventing PTP1B-mediated negative regulation of insulin signaling, it enhances insulin sensitivity and glucose uptake. This mechanism underlies its ability to prevent binge drinking-induced glucose intolerance.
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| ln Vivo |
In rats, intracerebroventricular infusion of CPT-157633 (0.2 µg/day) reduces hypothalamic inflammation and glucose intolerance brought on by binge drinking[1].
In vivo, CPT-157633 (0.2 ug/day; intracerebroventricular infusion) prevents glucose intolerance induced by binge drinking in rats. It also protects against alcohol-induced inflammation and metabolic dysfunction. By inhibiting PTP1B in key metabolic tissues, it improves insulin sensitivity and glucose homeostasis, making it a promising tool for studying alcohol-related metabolic disorders. |
| 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. CPT-157633 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.
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| Cell Assay |
For cell-based assays, hepatocytes or myotubes are treated with CPT-157633 (1-50 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 uptake assays. Cellular PTP1B activity in lysates is measured using fluorogenic substrates.
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| Animal Protocol |
For animal studies, CPT-157633 is administered via intracerebroventricular (ICV) infusion at 0.2 ug/day or intraperitoneally in rodent models of binge drinking or diet-induced insulin resistance. Blood glucose levels are measured by glucose tolerance tests (GTT) or insulin tolerance tests (ITT). Insulin signaling markers (p-IR, p-AKT) in liver and muscle are assessed by Western blot. Inflammatory cytokines (IL-6, TNF-alpha) are measured by ELISA.
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| ADME/Pharmacokinetics |
CPT-157633 is typically dissolved in DMSO for in vitro use. For in vivo administration via ICV infusion, it is dissolved in artificial cerebrospinal fluid (aCSF). Detailed pharmacokinetic parameters (half-life, bioavailability) have not been extensively reported, but the compound is designed to be stable and active in the central nervous system.
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| Toxicity/Toxicokinetics |
Toxicological data for CPT-157633 are limited to preclinical studies. At the doses used in binge drinking models (0.2 ug/day ICV), no significant systemic toxicity or behavioral abnormalities have been reported. Standard safety precautions for handling research chemicals should be followed. It is not intended for human use.
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| References | |
| Additional Infomation |
CPT-157633 (CAS: 888213-72-7) has a molecular formula of C12H16BrF2NO6P and a molecular weight of 465.20. It is a difluorophosphonomethylphenylalanine derivative that serves as a potent PTP1B inhibitor. This compound is valuable for studying the role of PTP1B in insulin resistance, metabolic syndrome, and alcohol-induced metabolic dysfunction. It is not an approved drug.
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| Molecular Formula |
C12H16BRF2N2O6PS
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|---|---|
| Molecular Weight |
465.204809188843
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| Exact Mass |
463.961
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| CAS # |
888213-72-7
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| PubChem CID |
91826021
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| Appearance |
White to off-white solid powder
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| LogP |
0.1
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
25
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| Complexity |
638
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| Defined Atom Stereocenter Count |
1
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| SMILES |
C(C1C=CC(C[C@H](NS(=O)(=O)C)C(=O)NC)=CC=1Br)(F)(F)P(O)(O)=O
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| InChi Key |
GNQQLTLSVIWPPQ-JTQLQIEISA-N
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| InChi Code |
InChI=1S/C12H16BrF2N2O6PS/c1-16-11(18)10(17-25(2,22)23)6-7-3-4-8(9(13)5-7)12(14,15)24(19,20)21/h3-5,10,17H,6H2,1-2H3,(H,16,18)(H2,19,20,21)/t10-/m0/s1
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| Chemical Name |
[[2-bromo-4-[(2S)-2-(methanesulfonamido)-3-(methylamino)-3-oxopropyl]phenyl]-difluoromethyl]phosphonic acid
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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, 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: 200 mg/mL (429.92 mM)
H2O: 100 mg/mL (214.96 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (10.75 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 (10.75 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 (10.75 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 | 2.1496 mL | 10.7481 mL | 21.4961 mL | |
| 5 mM | 0.4299 mL | 2.1496 mL | 4.2992 mL | |
| 10 mM | 0.2150 mL | 1.0748 mL | 2.1496 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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