| Identification | Back Directory | [Name]
ML 254 | [CAS]
1428630-86-7 | [Synonyms]
ML 254
5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide
5-[2-(3-fluorophenyl)ethynyl]-N-(3-methyloxetan-3-yl)pyridine-2-carboxamide
2-Pyridinecarboxamide, 5-[2-(3-fluorophenyl)ethynyl]-N-(3-methyl-3-oxetanyl)- | [Molecular Formula]
C18H15FN2O2 | [MDL Number]
MFCD28386364 | [MOL File]
1428630-86-7.mol | [Molecular Weight]
310.32 |
| Hazard Information | Back Directory | [Description]
ML-254, also known as VU0430644; is Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction. ML254 is highly selective for mGlu5 versus other mGlu receptors, has a clean ancillary Ricerca profile, and suitable dystrophia myotonica protein kinase (DMPK) properties for systemic dosing in rodents. Preliminary experiments at a single dose in an in vivo model of psychosis using ML254 demonstrates a robust reversal of amphetamine induced hyperlocomotion. ML254 will serve as a significant pure-PAM tool compound for the field with potential for studies within in vivo paradigms. Structure activity relationship (SAR) and characterization of ML254 are described. | [Uses]
ML254 is a potent mGlu5 potentiator, with EC50 and pEC50 of 9.3 nM and 8.03 nM for rat mGlu5, respectively. ML254 can be used for researching schizophrenia[1]. ML254 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. | [IC 50]
rat mGluR5: 9.3 nM (EC50); rat mGluR5: 8.03 nM (pEC50) | [References]
[1] Turlington M, Noetzel MJ, Chun A, et al. Exploration of allosteric agonism structure-activity relationships within an acetylene series of metabotropic glutamate receptor 5 (mGlu5) positive allosteric modulators (PAMs): discovery of 5-((3-fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254). J Med Chem. 2013;56(20):7976-7996. DOI:10.1021/jm401028t |
|
| Company Name: |
SPIRO PHARMA
|
| Tel: |
|
| Website: |
www.spiropharma.com.cn |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
|