1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. Auglurant

Auglurant (Synonyms: VU0424238)

Cat. No.: HY-16617 Purity: 99.40%
Handling Instructions

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.

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

Auglurant Chemical Structure

Auglurant Chemical Structure

CAS No. : 1396337-04-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2250 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3350 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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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[1].

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[1].

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

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 22.73 mg/mL (69.87 mM; Need ultrasonic)

H2O : < 0.1 mg/mL (insoluble)

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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.39 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Auglurant
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