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| | VU0448088 (ML253) Basic information |
| Product Name: | VU0448088 (ML253) | | Synonyms: | VU0448088 (ML253);Thieno[2,3-b]pyridine-2-carboxamide, 3-amino-5-chloro-4,6-dimethyl-N-(4-pyridinylmethyl)-;VU0448088 | | CAS: | 1417616-42-2 | | MF: | C16H15ClN4OS | | MW: | 346.84 | | EINECS: | | | Product Categories: | | | Mol File: | 1417616-42-2.mol |  |
| | VU0448088 (ML253) Chemical Properties |
| Boiling point | 612.4±55.0 °C(predicted) | | density | 1.402±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(predicted) | | pka | 11.93±0.46(predicted) | | form | Solid | | color | White to off-white |
| | VU0448088 (ML253) Usage And Synthesis |
| Uses | 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[1][2]. | | in vivo | VU0448088 (3, 10, 30, 56.6, 100 mg/kg; i.p.) reverses amphetamine-induced hyperlocomotion in a dose-dependent manner [1]. | Animal Model: | Rat (amphetamine-induced hyperlocomotion)[1] | | Dosage: | 3, 10, 30, 56.6, 100 mg/kg | | Administration: | IP | | 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. |
| | IC 50 | mAChR4: 56 nM (EC50) | | References | [1] Le U, et al. Discovery of a selective M 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. DOI:10.1016/j.bmcl.2012.10.073 |
| | VU0448088 (ML253) Preparation Products And Raw materials |
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