MT-110
Based on 1 Customer Validation
MT-110 (BPN-0027490) is a non-muscle myosin NMIIB-selective inhibitor with high brain penetration and favorable safety profile. MT-110 specifically disrupts NMIIB-dependent actin dynamics in dendritic spines, while it exerts no significant adverse effects on cardiac myosin II and cardiac functions (such as cardiac output and heart rate) at tested concentrations. A single administration of MT-110 produces long-lasting (sustained for several weeks) blockade of methamphetamine motivation associated with environmental cues. MT-110 exhibits extremely high specificity, with no interference with cocaine motivation, hippocampus-dependent memory, fear memory, or locomotor and anxiety-like behaviors. MT-110 serves as a valuable tool compound for investigating the mechanisms of methamphetamine use disorder.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.48%
- No. CAS: 2404652-82-8
- Fòrmula: C23H21N3O2
- Peso molecular:371.43
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Clinical Compound Library
HY-L026
-
CNS-Penetrant Compound Library
HY-L028
-
Cytoskeleton Compound Library
HY-L060
-
Protein-protein Interaction Inhibitor Library
HY-L109
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Actividad biológica
MT-110 (0-50 μM) potently inhibits non-muscle myosin IIB, non-muscle myosin IIA, smooth muscle myosin II, and skeletal muscle myosin II, and shows no inhibition of cardiac muscle myosin II at concentrations up to 50 μM[1].
MT-110 (0-11 μM; 24 h) potently inhibits NMIIB-dependent cytokinesis in COS-7 cells with an EC50 of 0.68 μM and does not induce cytotoxicity at concentrations up to 11 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | Tmax | T1/2 |
|---|---|---|---|---|
| Mice[1] | 2 mg/kg | i.v. | 0.08 h | 3.1 h |
MT-110 (1-2 mg/kg; i.v.; single dose) disrupts methamphetamine-seeking behavior in male Sprague-Dawley rats, with the 2 mg/kg dose producing a persistent effect for at least 14 days[1].
MT-110 (7.5 mg/kg; i.p.; single dose) does not disrupt cocaine-associated conditioned place preference in male C57BL/6 mice[1].
MT-110 (0.5-5 mg/kg; i.v.; single infusion) produces no acute adverse effects on cardiac output or heart rate in Sprague-Dawley rats[1].
MT-110 (10-20 mg/kg; i.v.; once weekly; 3 doses) produces no significant adverse effects in male and female Sprague-Dawley rats, with a no adverse effect level equal to or higher than 20 mg/kg[1].
MT-110 (0.5-16.5 mg/kg; i.v.; single dose) does not alter locomotor activity or anxiety-like behavior in male C57BL/6 mice tested in an open field[1].
MT-110 (15-30 mg/kg; i.v.; single dose) produces only modest, non-significant changes in respiratory rate and tidal volume, with no effect on minute volume, in Sprague-Dawley rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6 mice (adult, male, 25-30 g, methamphetamine-associated conditioned place preference training)[1]
-
Dosage:0.5 mg/kg; 1 mg/kg; 2.5 mg/kg
-
Administration:i.p.; single dose
-
Result:Eliminated the significant preference for the methamphetamine-paired chamber observed in vehicle-treated mice.
Produced disruption that persisted for at least 24 hours after a single dose, with no significant chamber preference detected in retesting.
-
Animal Model:Sprague-Dawley mice (adult, male, methamphetamine self-administration training followed by 4 days of forced abstinence)[1]
-
Dosage:1 mg/kg; 2 mg/kg
-
Administration:i.v.; single dose
-
Result:Reduced active lever pressing (a measure of methamphetamine seeking) during the first test at 1 mg/kg and 2 mg/kg doses.
Produced a persistent reduction in active lever pressing that remained significant 14 days after the single 2 mg/kg dose.
-
Animal Model:C57BL/6 mice (adult, male, 25-30 g, cocaine-associated conditioned place preference training)[1]
-
Dosage:7.5 mg/kg
-
Administration:i.p.; single dose
-
Result:Did not alter the significant preference for the cocaine-paired chamber observed in vehicle-treated mice.
Showed no difference in chamber preference detected between vehicle and MT-110-treated groups.
-
Animal Model:Sprague-Dawley rats (adult, male and female, healthy)[1]
-
Dosage:0.5 mg/kg; 5 mg/kg
-
Administration:i.v.; single infusion
-
Result:Produced no significant changes in cardiac output compared to baseline or vehicle controls at both tested doses.
Maintained normal heart rate at all tested doses.
-
Animal Model:Sprague-Dawley mice (adult, male and female, healthy)[1]
-
Dosage:10 mg/kg; 15 mg/kg; 20 mg/kg
-
Administration:i.v.; once weekly; 3 doses
-
Result:Caused no significant MT-110-related adverse effects, including no changes in body weight, complete blood count parameters, clinical chemistry values, urinalysis, or histopathologic tissue evaluation.
Noted only intermittent hypoactivity and exopthalmia, with no other toxicities detected.
-
Animal Model:C57BL/6 mice (adult, male, 25-30 g, healthy)[1]
-
Dosage:0.5, 1, 2.5, 6, 12, or 16.5 mg/kg
-
Administration:i.v.; single dose
-
Result:Produced no significant changes in distance traveled, average velocity, or time spent in the center versus the sides/corners of the open field compared to vehicle-treated mice.
Showed no effects on locomotion or anxiety-like behavior.
-
Animal Model:Sprague-Dawley rats (adult, male and female, healthy)[1]
-
Dosage:15 mg/kg; 30 mg/kg
-
Administration:i.v.; single dose
-
Result:Produced only modest, non-significant increases in respiratory rate (approximately 20% change) and corresponding decreases in tidal volume at both tested doses.
Caused no significant change in minute volume compared to vehicle controls.
Produced only acute transient motor effects (gait changes and stereotypical chewing).
Caused no significant effects on reflexes, physiological measurements (including body temperature, grip strength, and pupillary reflex), or other behavioral endpoints.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
No. CAS 2404652-82-8
-
Appearance Powder
-
Peso molecular 371.43
-
Fòrmula C23H21N3O2
-
Color Light yellow to yellow
-
SMILES
O=C1[C@@]2(O)C(N(C3=CC=C4N=C(C)C=CC4=C3)CC2)=NC5=C1C=C(C)C(C)=C5
-
Synonyms
BPN-0027490
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 100 mg/mL (269.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
-
Ficha de datos (286 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6923 mL | 13.4615 mL | 26.9230 mL | 67.3074 mL |
| 5 mM | 0.5385 mL | 2.6923 mL | 5.3846 mL | 13.4615 mL | |
| 10 mM | 0.2692 mL | 1.3461 mL | 2.6923 mL | 6.7307 mL | |
| 15 mM | 0.1795 mL | 0.8974 mL | 1.7949 mL | 4.4872 mL | |
| 20 mM | 0.1346 mL | 0.6731 mL | 1.3461 mL | 3.3654 mL | |
| 25 mM | 0.1077 mL | 0.5385 mL | 1.0769 mL | 2.6923 mL | |
| 30 mM | 0.0897 mL | 0.4487 mL | 0.8974 mL | 2.2436 mL | |
| 40 mM | 0.0673 mL | 0.3365 mL | 0.6731 mL | 1.6827 mL | |
| 50 mM | 0.0538 mL | 0.2692 mL | 0.5385 mL | 1.3461 mL | |
| 60 mM | 0.0449 mL | 0.2244 mL | 0.4487 mL | 1.1218 mL | |
| 80 mM | 0.0337 mL | 0.1683 mL | 0.3365 mL | 0.8413 mL | |
| 100 mM | 0.0269 mL | 0.1346 mL | 0.2692 mL | 0.6731 mL |
MT-110 Related Classifications
HY-175188 Related Classifications
Powered by Bioz