Auglurant

For research use only. Not for therapeutic Use.

  • CAT Number: I019578
  • CAS Number: 1396337-04-4
  • Molecular Formula: C16H12FN5O2
  • Molecular Weight: 325.30
  • Purity: ≥95%
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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].
Auglurant (VU0424238) with an IC50 value of 14 nM in HEK293A cells. It also binding a known allosteric site with K i value of 4.4 nM in HEK293A cells.
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].


Catalog Number I019578
CAS Number 1396337-04-4
Synonyms

N-(5-fluoropyridin-2-yl)-6-methyl-4-pyrimidin-5-yloxypyridine-2-carboxamide

Molecular Formula C16H12FN5O2
Purity ≥95%
InChI InChI=1S/C16H12FN5O2/c1-10-4-12(24-13-7-18-9-19-8-13)5-14(21-10)16(23)22-15-3-2-11(17)6-20-15/h2-9H,1H3,(H,20,22,23)
InChIKey RBAHIIPVJVMACF-UHFFFAOYSA-N
SMILES CC1=CC(=CC(=N1)C(=O)NC2=NC=C(C=C2)F)OC3=CN=CN=C3
Reference

[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.
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