| Identification | Back Directory | [Name]
2-PyridinecarboxaMide, N-(5-fluoro-2-pyridinyl)-6-Methyl-4-(5-pyriMidinyloxy)- | [CAS]
1396337-04-4 | [Synonyms]
Auglurant
VU0424238
N-(5-FLUOROPYRIDIN-2-YL)-6-METHYL-4-(PYRIMIDIN-5-YLOXY)PICOLINAMIDE
N-(5-Fluoro-2-pyridinyl)-6-methyl-4-(5-pyrimidinyloxy)-2-pyridinecarboxamide
2-PyridinecarboxaMide, N-(5-fluoro-2-pyridinyl)-6-Methyl-4-(5-pyriMidinyloxy)- | [Molecular Formula]
C16H12FN5O2 | [MDL Number]
MFCD28386341 | [MOL File]
1396337-04-4.mol | [Molecular Weight]
325.3 |
| Chemical Properties | Back Directory | [Boiling point ]
441.3±45.0 °C(Predicted) | [density ]
1.400±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 22.73 mg/mL (69.87 mM; Need ultrasonic) | [form ]
Solid | [pka]
10.08±0.70(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration[1]. | [in vivo]
Auglurant (VU0424238) had a clearance of 19.3 mL/min/kg in rats and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.8 mg/kg in rats. Plus, it also had a clearance of 15.5 mL/min/kg in cynomolgus monkeys and demonstrates 50% mGlu5 PET ligand occupancy at an oral dose of 0.06 mg/kg in baboons[1]. | [IC 50]
rat mGluR5: 11 nM (IC50); human mGluR5: 14 nM (IC50) | [References]
[1] Felts AS, et al. Discovery of N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide (VU0424238): A Novel Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 5 Selected for Clinical Evaluation. J Med Chem. 2017 Jun 22;60(12):5072-5085. DOI:10.1021/acs.jmedchem.7b00410 |
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| Company Name: |
AstaTech, Inc
|
| Tel: |
(215) 785 3197 |
| Website: |
www.astatechinc.com |
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