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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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LMPTP INHIBITOR 1 is a novel and selective inhibitor of low molecular weight protein tyrosine phosphatase (LMPTP)(IC50 = 0.8 μM LMPTP-A). LMPTP is a key promoter of insulin resistance and that LMPTP inhibitors would be beneficial for treating type 2 diabetes.
ln Vitro |
Having an IC50 of 0.8 μM LMPTP-A, LMPTP INHIBITOR 1 (diHCl) is a selective inhibitor of low molecular weight protein tyrosine phosphatase. Compared to LMPTP-B, it works better against LMPTP-A. Additionally, insulin-stimulated HepG2 IR phosphorylation in human HepG2 hepatocytes is enhanced by LMPTP inhibitor 1 (compound 23; 10 μM) [1].
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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].
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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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Molecular Formula |
C28H38CL2N4O
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Molecular Weight |
517.539
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Exact Mass |
516.24
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Elemental Analysis |
C, 64.98; H, 7.40; Cl, 13.70; N, 10.83; O, 3.09
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CAS # |
2310135-46-5
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Related CAS # |
LMPTP inhibitor 1;1908414-82-3;LMPTP inhibitor 1 hydrochloride;2310135-38-5
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Appearance |
Solid powder
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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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Chemical Name |
C28H38Cl2N4O
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Synonyms |
LMPTP INHIBITOR 1; LMPTP INHIBITOR 1 HCl; LMPTP INHIBITOR 1 dihydrochloride
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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 : ≥ 64 mg/mL (~123.66 mM)
H2O : ~50 mg/mL (~96.61 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.83 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 25.0 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: ≥ 2.5 mg/mL (4.83 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 25.0 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: ≥ 2.5 mg/mL (4.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (193.23 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.9322 mL | 9.6611 mL | 19.3222 mL | |
5 mM | 0.3864 mL | 1.9322 mL | 3.8644 mL | |
10 mM | 0.1932 mL | 0.9661 mL | 1.9322 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.