| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
IC50: 0.8 μM (LMPTP-A)[1]
The primary target of LMPTP inhibitor 1 hydrochloride is low molecular weight protein tyrosine phosphatase A (LMPTP-A), a member of the protein tyrosine phosphatase family that negatively regulates insulin receptor signaling. LMPTP dephosphorylates the insulin receptor and its downstream substrates, thereby attenuating insulin signal transduction. By inhibiting LMPTP-A, this compound enhances insulin sensitivity and promotes glucose uptake in peripheral tissues. The compound shows high selectivity for LMPTP over other phosphatases. |
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| ln Vitro |
LMPTP inhibitor 1 hydrochloride exhibits a more strong impact on LMPTP-A compared to LMPTP-B and is a selective inhibitor of low molecular weight protein tyrosine phosphatase, having an IC50 of 0.8 μM LMPTP-A. In human HepG2 hepatocytes stimulated with insulin, LMPTP inhibitor 1 (Compound 23; 10 μM) hydrochloride also increases HepG2 IR phosphorylation[1].
In vitro, LMPTP inhibitor 1 hydrochloride demonstrates potent inhibition of LMPTP-A with an IC50 of 0.8 µM. The compound exhibits selective inhibition of LMPTP activity in biochemical assays using purified enzyme preparations. In cellular models, LMPTP inhibitor 1 enhances insulin-stimulated Akt phosphorylation and glucose uptake in insulin-responsive cell lines. The compound shows concentration-dependent inhibition of LMPTP activity, with full inhibition achieved at micromolar concentrations. |
| ln Vivo |
Orally accessible LMPTP inhibitor 1 hydrochloride administration produces a mean blood concentration of around 680 nM at 0.03% w/w, but therapy at 0.05% w/w leads in >3 μM; also, it cures diabetes in obese animals. Without changing body weight, LMPTP inhibitor 1 (0.05% w/w) hydrochloride suppresses LMPTP activity, considerably enhances glucose tolerance, and lowers fasting insulin levels in diabetic DIO mice[1].
In vivo, LMPTP inhibitor 1 hydrochloride has been evaluated in diet-induced obese (DIO) diabetic mouse models. When administered at 0.05% w/w in the diet, the compound significantly suppresses LMPTP activity, markedly enhances glucose tolerance, and lowers fasting insulin levels in diabetic DIO mice without affecting body weight. These findings demonstrate the therapeutic potential of LMPTP inhibition for improving glycemic control in type 2 diabetes. The compound shows good oral bioavailability and efficacy in preclinical models. |
| Enzyme Assay |
The in vitro enzyme inhibition assay for LMPTP inhibitor 1 hydrochloride typically uses recombinant human LMPTP-A enzyme and a synthetic phosphopeptide substrate such as p-nitrophenyl phosphate (pNPP) or a fluorogenic substrate. The enzyme is pre-incubated with varying concentrations of the inhibitor (0.001-100 µM) in assay buffer at 25°C for 5-10 minutes. The reaction is initiated by adding the substrate, and after 15-30 minutes of incubation, the reaction is stopped and absorbance or fluorescence is measured to calculate IC50 values.
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| Cell Assay |
For in vitro cell-based assays, insulin-responsive cell lines such as 3T3-L1 adipocytes or L6 myotubes are cultured and treated with LMPTP inhibitor 1 hydrochloride at concentrations ranging from 0.1-50 µM. Cells are stimulated with insulin, and LMPTP activity is measured in cell lysates using a phosphatase activity assay. Insulin signaling is assessed by Western blot analysis of phosphorylated Akt and insulin receptor. Glucose uptake is measured using 2-deoxyglucose uptake assays with radiolabeled or fluorescent tracers.
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| Animal Protocol |
In vivo animal studies are typically conducted using diet-induced obese (DIO) C57BL/6 mice or other diabetic mouse models. LMPTP inhibitor 1 hydrochloride is administered orally via diet admixture at 0.05% w/w or by oral gavage at various doses for 2-4 weeks. Blood glucose and insulin levels are measured during oral glucose tolerance tests (OGTT). LMPTP activity is assessed in tissue lysates from liver, muscle, and adipose tissue. Body weight and food intake are monitored throughout the study.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of LMPTP inhibitor 1 hydrochloride have been characterized in preclinical species. The compound shows good oral bioavailability and favorable drug-like properties. After oral administration, it is rapidly absorbed and achieves therapeutic concentrations in plasma and target tissues. The compound has a moderate half-life suitable for once- or twice-daily dosing. Metabolic stability studies indicate the compound is metabolically stable in liver microsomes. Detailed PK parameters are available from the primary research literature.
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| Toxicity/Toxicokinetics |
Toxicology studies of LMPTP inhibitor 1 hydrochloride have been conducted in rodent models. At the efficacious dose of 0.05% w/w in diet, the compound is well-tolerated with no significant effects on body weight or general health parameters. Higher doses may be associated with gastrointestinal effects or other toxicities typical of phosphatase inhibitors. The compound is intended for research use only and has not been fully evaluated for clinical safety. Standard toxicological endpoints should be assessed in future studies.
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| References | |
| Additional Infomation |
LMPTP inhibitor 1 hydrochloride is a research-grade compound exclusively for laboratory use. It is a valuable tool for studying the role of LMPTP in insulin signaling, glucose metabolism, and the pathogenesis of type 2 diabetes. The compound's ability to improve glucose tolerance and reduce insulin levels in diabetic models highlights the therapeutic potential of LMPTP inhibition for metabolic diseases. Further research is needed to fully characterize its selectivity, pharmacokinetics, and long-term safety profile.
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| Molecular Formula |
C28H37CLN4O
|
|---|---|
| Molecular Weight |
481.07
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| Exact Mass |
480.265
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| CAS # |
2310135-38-5
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| Related CAS # |
LMPTP inhibitor 1 dihydrochloride;2310135-46-5;LMPTP inhibitor 1;1908414-82-3
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| PubChem CID |
134691743
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| Appearance |
Typically exists as solid at room temperature
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
34
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| Complexity |
580
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCN(CC)C(=O)C1=CC=C(C=C1)C2=NC3=CC=CC=C3C(=C2)NCCCN4CCCCC4.Cl
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| InChi Key |
WYRLEOWACOXSQP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C28H36N4O.ClH/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);1H
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| Chemical Name |
N,N-diethyl-4-[4-(3-piperidin-1-ylpropylamino)quinolin-2-yl]benzamide;hydrochloride
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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 | 2.0787 mL | 10.3935 mL | 20.7870 mL | |
| 5 mM | 0.4157 mL | 2.0787 mL | 4.1574 mL | |
| 10 mM | 0.2079 mL | 1.0393 mL | 2.0787 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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