Description
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.
Product information
CAS Number: 1396337-04-4
Molecular Weight: 325.30
Formula: C16H12FN5O2
Chemical Name: N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)pyridine-2-carboxamide
Smiles: CC1=CC(=CC(=N1)C(=O)NC1=CC=C(F)C=N1)OC1C=NC=NC=1
InChiKey: RBAHIIPVJVMACF-UHFFFAOYSA-N
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)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 22.73 mg/mL (69.87 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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.
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.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.