1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. mGluR2 antagonist 1

mGluR2 antagonist 1 

Cat. No.: HY-133555 Purity: 99.06%
Handling Instructions

mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability.

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

mGluR2 antagonist 1 Chemical Structure

mGluR2 antagonist 1 Chemical Structure

CAS No. : 1432728-49-8

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 800 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1550 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2350 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
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Customer Review

Based on 1 publication(s) in Google Scholar

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Description

mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability[1].

IC50 & Target[1]

mGluR2

9 nM (IC50)

In Vivo

In vivo, mGluR2 antagonist 1 (Compound 25) reverses the effect of mGluR2 agonist LY379268 in amphetamine-induced hyperlocomotion and shows good efficacy in the mouse delayed non-match to position assay at 10 mg/kg.

Molecular Weight

377.37

Formula

C₂₁H₁₆FN₃O₃

CAS No.

1432728-49-8

SMILES

NC(C1=NC2=CC(CN3C(CCC3=O)=O)=CC=C2C(C4=CC=C(F)C=C4)=C1)=O

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 : 100 mg/mL (264.99 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6499 mL 13.2496 mL 26.4992 mL
5 mM 0.5300 mL 2.6499 mL 5.2998 mL
10 mM 0.2650 mL 1.3250 mL 2.6499 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (6.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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This equation is commonly abbreviated as: C1V1 = C2V2

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Keywords:

mGluR2 antagonist 1mGluRMetabotropic glutamate receptorsMetabotropicglutamatereceptormGluR2CognitionAlzheimerInhibitorinhibitorinhibit

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Product Name:
mGluR2 antagonist 1
Cat. No.:
HY-133555
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