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| 5mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Targets |
INVIVO-4823 specifically targets low-molecular-weight protein tyrosine phosphatase (LMPTP), an enzyme that plays a role in insulin signaling. Human genetic studies and data from mouse models suggest that LMPTP promotes diabetes and insulin resistance. By inhibiting LMPTP, INVIVO-4823 aims to enhance insulin sensitivity, making it a valuable tool for studying the molecular basis of type 2 diabetes and obesity.
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| ln Vitro |
LMPTP inhibitor 1 (compound 23) is a strong inhibitor of low molecular weight protein tyrosine phosphatase that selectively inhibits LMPTP-A. Its IC50 is 0.8 μM LMPTP-A. In human HepG2 hepatocytes stimulated with insulin, LMPTP inhibitor 1 (10 μM) also increases HepG2 IR phosphorylation [1].
In vitro, INVIVO-4823 is a potent inhibitor of LMPTP-A, with an IC50 of 0.8 μM. This demonstrates its ability to effectively block the activity of this enzyme in biochemical assays. Its potency makes it a useful tool for studying the role of LMPTP in cellular insulin signaling, as it can be used to assess the effects of LMPTP inhibition on downstream pathways in cell-based models. |
| ln Vivo |
LMPTP inhibitor 1 can correct diabetes in obese mice and is orally bioavailable, with typical serum concentrations of about 680 nM after therapy at 0.03% w/w and >3 μM following treatment at 0.05% w/w. Without changing body weight, LMPTP inhibitor 1 (0.05% w/w) dramatically enhances glucose tolerance, lowers fasting insulin levels, and suppresses LMPTP activity in diabetic DIO mice [1].
In vivo, INVIVO-4823 is used in research to study the effects of LMPTP inhibition. While specific in vivo efficacy data are not detailed in the provided sources, its mechanism of enhancing insulin sensitivity makes it a candidate for study in animal models of diabetes and obesity. By inhibiting LMPTP, it could potentially improve glucose metabolism and insulin action. |
| Enzyme Assay |
In vitro enzyme/receptor binding studies for INVIVO-4823 are performed using enzyme activity assays. In these assays, the LMPTP enzyme is incubated with a substrate in the presence of varying concentrations of the inhibitor. The enzyme's activity is measured by detecting the dephosphorylation of the substrate. The IC50 of 0.8 μM against LMPTP-A is determined from these experiments, confirming the compound's direct inhibition of the enzyme.
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| Cell Assay |
In vitro cellular assays for INVIVO-4823 are used to study its effects on insulin signaling. In these experiments, cells (e.g., hepatocytes, adipocytes, or muscle cells) are treated with the compound, and then insulin-stimulated signaling pathways are assessed. Key readouts include the phosphorylation of the insulin receptor and its downstream targets, such as AKT. These assays are crucial for confirming that LMPTP inhibition enhances insulin sensitivity in a cellular context.
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| Animal Protocol |
In vivo animal studies for INVIVO-4823 are conducted in models of diabetes and obesity. In these models, animals would be treated with the compound to assess its effect on glucose tolerance, insulin sensitivity, and other metabolic parameters. While specific protocols are not detailed in the provided sources, such studies are a standard part of evaluating the therapeutic potential of LMPTP inhibitors.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of INVIVO-4823 are indicated by its molecular weight of 444.61 g/mol and its molecular formula of C₂₈H₃₆N₄O. Its solubility and other PK parameters are not detailed in the provided sources. For storage, it is typically kept as a powder at -20°C to maintain stability. These properties are important for its formulation in both in vitro and in vivo experiments.
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| Toxicity/Toxicokinetics |
Toxicological data for INVIVO-4823 are limited, as it is a research compound. Its primary value is as a tool for studying LMPTP biology. While specific toxicity profiles are not detailed, its mechanism of modulating insulin signaling could have significant physiological effects. Comprehensive safety studies are not available in the public domain.
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| References |
[1]. Stanford SM1, et al. Diabetes reversal by inhibition of the low-molecular-weight tyrosine phosphatase. Nat Chem Biol. 2017 Jun;13(6):624-632
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| Additional Infomation |
INVIVO-4823 is a research-use-only compound that acts as a potent inhibitor of LMPTP. Its CAS number is 1908414-82-3. It is also known as LMPTP inhibitor 1 and CS-2789. This compound is a valuable tool for researchers studying the role of LMPTP in metabolic diseases, particularly type 2 diabetes and obesity. It is not an approved drug.
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| Molecular Formula |
C28H36N4O
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| Molecular Weight |
444.623
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| Exact Mass |
444.288
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| CAS # |
1908414-82-3
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| Related CAS # |
LMPTP inhibitor 1 dihydrochloride;2310135-46-5;LMPTP inhibitor 1 hydrochloride;2310135-38-5
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| PubChem CID |
121284761
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
657.7±55.0 °C at 760 mmHg
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| Flash Point |
351.6±31.5 °C
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| Vapour Pressure |
0.0±2.0 mmHg at 25°C
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| Index of Refraction |
1.613
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| LogP |
4.87
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
33
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| Complexity |
580
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.Cl.O=C(C1C=CC(=CC=1)C1=CC(=C2C=CC=CC2=N1)NCCCN1CCCCC1)N(CC)CC
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| InChi Key |
XISMYRQHGUUMGY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H36N4O/c1-3-32(4-2)28(33)23-15-13-22(14-16-23)26-21-27(24-11-6-7-12-25(24)30-26)29-17-10-20-31-18-8-5-9-19-31/h6-7,11-16,21H,3-5,8-10,17-20H2,1-2H3,(H,29,30) SMILES
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| Chemical Name |
N,N-Diethyl-4-[4-(3-piperidin-1-yl-propylamino)-quinolin-2-yl]-benzamide
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| Synonyms |
LMPTP-IN-23 LMPTP-IN 23 LMPTP-IN23 INVIVO-4823 INVIVO 4823 INVIVO4823 LMPTP inhibitor1 LMPTP inhibitor-1.
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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 | 2.2491 mL | 11.2456 mL | 22.4911 mL | |
| 5 mM | 0.4498 mL | 2.2491 mL | 4.4982 mL | |
| 10 mM | 0.2249 mL | 1.1246 mL | 2.2491 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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