| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Lymphoid tyrosine phosphatase (LYP / PTPN22). LTV-1 inhibits LYP with an IC50 of 508 nM. It shows 3-fold selectivity over TCPTP (IC50=1.52 microM) and PTP1B (IC50=1.59 microM), 46-fold over SHP1 (IC50=23.2 microM), and 59-fold over CD45 (IC50=30.1 microM), and >200-fold over PTP-PEST (IC50 >100 microM).
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|---|---|
| ln Vitro |
Even at the highest tested concentration of 40 μM, LTV-1 (1.25-40 μM) did not significantly affect cell viability as measured by the metabolic rate assay. Consequently, HeLa cells, Jurkat TAg T cells, and peripheral blood mononuclear cells (PBMC) do not respond negatively to LTV-1 [1].
LTV-1 inhibits lymphoid tyrosine phosphatase (LYP) with an IC50 of 508 nM. It is a highly potent, cell-permeable, and reversible inhibitor. LTV-1 shows selectivity for LYP over other phosphatases including TCPTP, PTP1B, SHP1, CD45, and PTP-PEST. The compound has potential for autoimmunity treatment. |
| ln Vivo |
No specific in vivo activity data is available for LTV-1. Based on its inhibition of LYP, a key regulator of T-cell receptor signaling, LTV-1 has potential for in vivo studies in autoimmune disease models. Such studies would evaluate its effects on T-cell activation and autoimmune pathology.
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| Enzyme Assay |
In vitro enzyme assays for LTV-1 involve measuring its inhibition of LYP (PTPN22) phosphatase activity using synthetic substrates (e.g., p-nitrophenyl phosphate or fluorogenic substrates). The IC50 is determined from dose-response curves. Selectivity is assessed by testing against a panel of related phosphatases (TCPTP, PTP1B, SHP1, CD45, PTP-PEST).
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: HeLa cells, Jurkat TAg T cells and PBMC Tested Concentrations: 1.25, 2.5, 5.0, 10, 20 and 40 μM Incubation Duration: 48 hrs (hours) Experimental Results: No significant effect on cell viability (metabolism) rate assay), even at the highest concentration tested (40 μM). The in vitro cellular activity of LTV-1 is evaluated in T cells. Cells are treated with the compound, and LYP activity is measured using phosphatase assays. Effects on T-cell receptor signaling (e.g., phosphorylation of signaling proteins, cytokine production) are assessed to confirm target engagement and functional activity. The compound's cell permeability allows for intracellular target engagement. |
| Animal Protocol |
No specific in vivo animal experimental protocols are available for LTV-1. For studying LYP inhibition in autoimmune disease models, the compound would typically be administered via intraperitoneal injection or oral gavage in rodent models of autoimmunity (e.g., experimental autoimmune encephalomyelitis, collagen-induced arthritis). Endpoints would include disease severity, immune cell activation, and cytokine profiles.
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| ADME/Pharmacokinetics |
No specific pharmacokinetic data is available for LTV-1. As a small molecule (molecular weight 472.51, formula C26H20N2O5S), it is expected to have moderate lipophilicity and cell permeability. The compound is a reversible inhibitor, suggesting potential for pharmacological modulation.
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| Toxicity/Toxicokinetics |
No specific toxicological data is available for LTV-1. As a research compound intended for laboratory use, standard safety precautions should be observed. No clinical toxicity studies have been reported. The compound has not been evaluated for genotoxicity, carcinogenicity, or reproductive toxicity.
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| References | |
| Additional Infomation |
LTV-1 is a potent, cell-permeable, reversible inhibitor of lymphoid tyrosine phosphatase (LYP/PTPN22) with an IC50 of 508 nM. It shows selectivity over other phosphatases and has potential for autoimmune disease research. It is not approved for clinical use and is intended for research purposes only.
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| Molecular Formula |
C26H20N2O5S
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|---|---|
| Molecular Weight |
472.5124
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| Exact Mass |
472.109
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| CAS # |
347379-29-7
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| PubChem CID |
1920999
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| Appearance |
Yellow to brown solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.723
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| LogP |
4.99
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
34
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| Complexity |
835
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=CC=CC=C1N2C(=O)/C(=C/C3=CC=C(C=C3)OCC4=CC(=CC=C4)C(=O)O)/C(=O)NC2=S
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| InChi Key |
DSYDHTCEVHUCPE-KGENOOAVSA-N
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| InChi Code |
InChI=1S/C26H20N2O5S/c1-16-5-2-3-8-22(16)28-24(30)21(23(29)27-26(28)34)14-17-9-11-20(12-10-17)33-15-18-6-4-7-19(13-18)25(31)32/h2-14H,15H2,1H3,(H,31,32)(H,27,29,34)/b21-14+
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| Chemical Name |
3-[[4-[(E)-[1-(2-methylphenyl)-4,6-dioxo-2-sulfanylidene-1,3-diazinan-5-ylidene]methyl]phenoxy]methyl]benzoic 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 |
| 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 : ~22.73 mg/mL (~48.10 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.29 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: 2.08 mg/mL (4.40 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1164 mL | 10.5818 mL | 21.1636 mL | |
| 5 mM | 0.4233 mL | 2.1164 mL | 4.2327 mL | |
| 10 mM | 0.2116 mL | 1.0582 mL | 2.1164 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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