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Activity Type | Activity Value -log(M) | Mechanism of Action | Activity Reference | Publications (PubMed IDs) |
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SKU | Size | Availability | Price | Qty |
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A650970-5mg | 5mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $450.90 | |
A650970-10mg | 10mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $750.90 | |
A650970-50mg | 50mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $2,250.90 | |
A650970-100mg | 100mg | Available within 8-12 weeks(?) Production requires sourcing of materials. We appreciate your patience and understanding. | $3,350.90 |
Synonyms | BDBM50257064 | GRN8X62ZW2 | MFCD28386341 | N-(5-Fluoro-2-pyridinyl)-6-methyl-4-(5-pyrimidinyloxy)-2-pyridinecarboxamide | RBAHIIPVJVMACF-UHFFFAOYSA-N | VU 0424238 | SCHEMBL12499337 | CS-0009173 | VU 238 | MS-24851 | Auglurant | N-(5-fluoropyridin-2-yl)-6- |
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Specifications & Purity | ≥99% |
Biochemical and Physiological Mechanisms | Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC 50 value of 11 nM (rat) and an IC 50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration. |
Storage Temp | Store at -20°C |
Shipped In | Ice chest + Ice pads |
Product Description | Auglurant (VU0424238) is a novel and selective mGlu5 antagonist with an IC 50 value of 11 nM (rat) and an IC 50 value of 14 nM (human). Auglurant (VU0424238) has an acceptable CNS penetration In Vitro Auglurant (VU0424238) with an IC 50 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Form:Solid IC50& Target:rat mGluR5 11 nM (IC 50 ) human mGluR5 14 nM (IC 50 ) |
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IUPAC Name | N-(5-fluoropyridin-2-yl)-6-methyl-4-pyrimidin-5-yloxypyridine-2-carboxamide |
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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) |
InChi Key | RBAHIIPVJVMACF-UHFFFAOYSA-N |
Canonical SMILES | CC1=CC(=CC(=N1)C(=O)NC2=NC=C(C=C2)F)OC3=CN=CN=C3 |
Isomeric SMILES | CC1=CC(=CC(=N1)C(=O)NC2=NC=C(C=C2)F)OC3=CN=CN=C3 |
Alternate CAS | 1396337-04-4 |
PubChem CID | 60168069 |
MeSH Entry Terms | N-(5-fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide;VU0424238 |
Molecular Weight | 325.30 |
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Solubility | DMSO : 22.73 mg/mL (69.87 mM; Need ultrasonic) |
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