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| Targets |
RPTPbeta/zeta is a receptor-type protein tyrosine phosphatase. MY33-3 HCl is a potent and selective inhibitor of RPTPbeta/zeta (IC50 ~0.1 microM) and also inhibits PTP-1B (IC50 ~0.7 microM). By inhibiting RPTPbeta/zeta, it blocks ethanol-induced TrkA and ALK activation and reduces LPS-induced nitrite production and iNOS expression in microglia. It also has effects on reducing ethanol consumption and neuroinflammation.
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| ln Vitro |
In SH-SY5Y cells, ethanol-induced TrkA and ALK activation is blocked by MY33-3 hydrochloride (1 μM; 5 min pretreatment) [1]. LPS-induced nitrite production and iNos increase in BV2 microglia is inhibited by MY33-3 hydrochloride (0.1-10 μM; 24 hours) [2].
In SH-SY5Y cells, ethanol-induced TrkA and ALK activation is blocked by MY33-3 HCl (1 microM, 5 min pretreatment). In BV2 microglia, LPS-induced nitrite production and iNOS increase is inhibited by MY33-3 HCl (0.1-10 microM, 24 hours). The compound also reverses sevoflurane-induced decrease in discriminating index and reduced motor learning capacity in vivo. |
| ln Vivo |
On days 3 and 4, MY33-3 hydrochloride (60 mg/kg; p.o.) decreased the amount of ethanol consumed in comparison to days 2 and 3. On day 3, ethanol solution preference is decreased by MY33-3 hydrochloride [1]. The decrease in discriminating index and reduced motor learning capacity caused by sevoflurane are reversed by MY33-3 hydrochloride (ip) [3].
In rodent models, MY33-3 HCl (60 mg/kg, p.o.) decreases ethanol consumption on days 3 and 4 compared to baseline on days 2 and 3. The compound reduces ethanol solution preference on day 3. MY33-3 HCl also reverses sevoflurane-induced cognitive dysfunction when administered intraperitoneally. These effects are consistent with its mechanism as an RPTPbeta/zeta inhibitor. |
| Enzyme Assay |
Not explicitly detailed in reference sources. A typical protein tyrosine phosphatase assay involves incubating recombinant RPTPbeta/zeta with a fluorogenic substrate such as DiFMUP (6,8-difluoro-4-methylumbelliferyl phosphate) in the presence of MY33-3 HCl at varying concentrations. Dephosphorylation is monitored by fluorescence increase over time, and IC50 is calculated from dose-response curves.
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| Cell Assay |
For LPS-induced nitrite production, BV2 microglial cells are treated with MY33-3 HCl (0.1-10 microM) for 24 hours, then stimulated with LPS (1 microg/mL) for an additional 24 hours. Nitrite levels in culture supernatants are measured using the Griess reagent, and iNOS protein expression is detected by Western blot.
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| Animal Protocol |
In the ethanol consumption model, rats or mice are given access to a 2% ethanol solution in a two-bottle choice paradigm for several days. MY33-3 HCl is administered orally at 60 mg/kg once daily, and ethanol consumption and preference are measured. In the sevoflurane-induced cognitive dysfunction model, MY33-3 HCl (ip) is administered before sevoflurane exposure, and cognitive function is assessed using the Morris water maze or novel object recognition test.
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| ADME/Pharmacokinetics |
MY33-3 HCl has a molecular weight of 433.86 and formula C16H14ClF6NS2. It is soluble in DMSO (up to 40 mg/mL). Storage should be at -20degC as powder, protected from moisture and light. For in vivo use, oral administration is feasible at 60 mg/kg, and intraperitoneal administration is also used. The compound is for research use only.
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| Toxicity/Toxicokinetics |
No detailed toxicity data for MY33-3 HCl are provided in the reference sources. In the referenced behavioral studies, the compound was administered at 60 mg/kg (p.o.) without reported adverse effects. Comprehensive toxicology studies would be required for clinical development. The compound is for research use only and not intended for human use.
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| References |
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| Additional Infomation |
MY33-3 HCl is a research compound not yet approved for clinical use. It is being studied for potential applications in alcohol use disorder, neuroinflammation, and cognitive dysfunction. The compound shows promising effects in reducing ethanol consumption and reversing anesthesia-induced cognitive deficits. Further studies are needed to evaluate its clinical potential.
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| Molecular Formula |
C16H14CLF6NS2
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|---|---|
| Molecular Weight |
433.86
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| Exact Mass |
433.016
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| CAS # |
2204280-42-0
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| Related CAS # |
MY33-3;2204280-41-9
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| PubChem CID |
164516786
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
26
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| Complexity |
349
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1(=CC=C(C=C1)CNCC1C=CC(=CC=1)SC(F)(F)F)SC(F)(F)F.Cl
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| InChi Key |
NCXYCGGCHBSQDC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H13F6NS2.ClH/c17-15(18,19)24-13-5-1-11(2-6-13)9-23-10-12-3-7-14(8-4-12)25-16(20,21)22;/h1-8,23H,9-10H2;1H
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| Chemical Name |
1-[4-(trifluoromethylsulfanyl)phenyl]-N-[[4-(trifluoromethylsulfanyl)phenyl]methyl]methanamine;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 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 : ~25 mg/mL (~57.62 mM)
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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 | 2.3049 mL | 11.5245 mL | 23.0489 mL | |
| 5 mM | 0.4610 mL | 2.3049 mL | 4.6098 mL | |
| 10 mM | 0.2305 mL | 1.1524 mL | 2.3049 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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