1. GPCR/G Protein
  2. mGluR

VU0424238 

Cat. No.: HY-16617
Handling Instructions

VU0424238 is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). VU0424238 has an acceptable CNS penetration.

For research use only. We do not sell to patients.

VU0424238 Chemical Structure

VU0424238 Chemical Structure

CAS No. : 1396337-04-4

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

VU0424238 is a novel and selective mGlu5 antagonist with an IC50 value of 11 nM (rat) and an IC50 value of 14 nM (human). VU0424238 has an acceptable CNS penetration[1].

In Vitro

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

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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0741 mL 15.3704 mL 30.7409 mL
5 mM 0.6148 mL 3.0741 mL 6.1482 mL
10 mM 0.3074 mL 1.5370 mL 3.0741 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

325.30

Formula

C₁₆H₁₂FN₅O₂

CAS No.

1396337-04-4

SMILES

CC1=NC(C(NC2=CC=C(F)C=N2)=O)=CC(OC3=CN=CN=C3)=C1

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
VU0424238
Cat. No.:
HY-16617
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VU0424238

Cat. No.: HY-16617