ML 254
- Product Name
- ML 254
- CAS No.
- 1428630-86-7
- Chemical Name
- ML 254
- Synonyms
- ML 254;ML 254, 10 mM in DMSO;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)-;ML 254,inhibit,ML254,ML-254,Inhibitor,Metabotropic glutamate receptors,mGluR,Schizophrenia
- CBNumber
- CB72716289
- Molecular Formula
- C18H15FN2O2
- Formula Weight
- 310.32
- MOL File
- 1428630-86-7.mol
ML 254 Property
- form
- Solid
- color
- Off-white to light yellow
N-Bromosuccinimide Price
- Product number
- DC43016
- Product name
- ML254
- Purity
- >98%
- Packaging
- 100mg
- Price
- $850
- Updated
- 2021/12/16
- Product number
- DC43016
- Product name
- ML254
- Purity
- >98%
- Packaging
- 250mg
- Price
- $1500
- Updated
- 2021/12/16
- Product number
- DC43016
- Product name
- ML254
- Purity
- >98%
- Packaging
- 1g
- Price
- $3000
- Updated
- 2021/12/16
ML 254 Chemical Properties,Usage,Production
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
ML 254 Preparation Products And Raw materials
Raw materials
Preparation Products
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