VU0448088
Based on 1 Customer Validation
VU0448088 (ML253) is a potent and cross the blood-brain barrier tricyclic muscarinic acetylcholine receptor subtype 4 (M4) positive allosteric modulator with EC50 values of 56, 176 nM for human and rat, respectively. VU0448088 has the potential for the research of psychotic.
For research use only. We do not sell to patients.
- Purity: 98.67%
- CAS No.: 1417616-42-2
- Formula: C16H15ClN4OS
- Molecular Weight:346.83
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Storage: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]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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mAChR4 56 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO-K1 | EC50 |
>30 μM
Compound: 4, ML253 (VU0448088)
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Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M1 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
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[PMID: 23177787] |
| CHO-K1 | EC50 |
>30 μM
Compound: 4, ML253 (VU0448088)
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Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M2 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
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[PMID: 23177787] |
| CHO-K1 | EC50 |
>30 μM
Compound: 4, ML253 (VU0448088)
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Positive allosteric modulation of human muscarinic M3 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M3 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
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[PMID: 23177787] |
| CHO-K1 | EC50 |
>30 μM
Compound: 4, ML253 (VU0448088)
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Positive allosteric modulation of human muscarinic M5 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M5 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
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[PMID: 23177787] |
| CHO-K1 | EC50 |
56 nM
Compound: 4, ML253 (VU0448088)
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Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
Positive allosteric modulation of human muscarinic M4 receptor expressed in CHO-K1 cells assessed as leftward shift in acetylcholine response treated for 144 secs prior to acetylcholine addition measured for 5 mins by Fluo-4-AM based calcium mobilization
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[PMID: 23177787] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rat (amphetamine-induced hyperlocomotion)[1]
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Dosage:3, 10, 30, 56.6, 100 mg/kg
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Administration:IP
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Result:Reversed amphetamine-induced hyperlocomotion in a dose-dependent manner, showed a modest reduction of 26% at a dose of 10 mg/kg; at the three highest doses (30, 56.6 and 100 mg/kg), showed significant reductions of 47.9%, 53.7% and 57.3%, respectively.
Chemical Information
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CAS No. 1417616-42-2
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Appearance Solid
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Molecular Weight 346.83
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Formula C16H15ClN4OS
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Color White to off-white
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SMILES
CC1=C(Cl)C(C)=NC2=C1C(N)=C(C(NCC3=CC=NC=C3)=O)S2
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Synonyms
ML253
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 5 mg/mL (14.42 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)
Purity & Documentation
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Data Sheet (273 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Le U, et al. Discovery of a selective M₄ positive allosteric modulator based on the 3-amino-thieno[2,3-b]pyridine-2-carboxamide scaffold: development of ML253, a potent and brain penetrant compound that is active in a preclinical model of schizophrenia. Bioorg Med Chem Lett. 2013 Jan 1;23(1):346-50. [Content Brief]
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 | 2.8833 mL | 14.4163 mL | 28.8326 mL | 72.0814 mL |
| 5 mM | 0.5767 mL | 2.8833 mL | 5.7665 mL | 14.4163 mL | |
| 10 mM | 0.2883 mL | 1.4416 mL | 2.8833 mL | 7.2081 mL |
VU0448088 Related Classifications
HY-162663 Related Classifications
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