1. GPCR/G Protein
  2. mGluR

JNJ-46778212 (Synonyms: VU 0409551)

Cat. No.: HY-19559 Purity: 99.24%
Handling Instructions

JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.

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

JNJ-46778212 Chemical Structure

JNJ-46778212 Chemical Structure

CAS No. : 1363281-27-9

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 170 In-stock
Estimated Time of Arrival: December 31
25 mg USD 390 In-stock
Estimated Time of Arrival: December 31
50 mg USD 690 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

JNJ-46778212 (VU 0409551) is an mGlu5 positive allosteric modulator with an EC50 of 260 nM.

IC50 & Target

EC50: 260 nM (mGlu5)[1]

In Vivo

In oral brain/plasma studies, JNJ-46778212 displays excellent CNS penetration[1]. JNJ-46778212 enhances NMDAR function and rescues long-term potentiation in hippocampal slices obtained from SR−/− mice. The administration of JNJ-46778212 to SR−/− mice reverses their deficits in several neuroplasticity signaling pathways and improves their contextual fear memory[2].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 125 mg/mL (354.75 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8380 mL 14.1900 mL 28.3801 mL
5 mM 0.5676 mL 2.8380 mL 5.6760 mL
10 mM 0.2838 mL 1.4190 mL 2.8380 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 (5.90 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (5.90 mM); Clear solution

References
Animal Administration
[1]

Mice[1]

SR−/− mice receive once daily, intraperitoneal (i.p.) injections of vehicle (20% hydroxypropyl β-cyclodextran) or VU0409551 for 5 days at a volume of 10 mL/kg. For the in vivo pharmacokinetic and dose-finding experiments, WT mice (n=5–6/dose) receive vehicle or VU0409551 (10 and 30 mg/kg). For the SR−/− mice reversal studies, WT mice receive vehicle and SR−/− mice receive either vehicle or VU0409551 (30 mg/kg). All mice are killed 2 h after the last injection on day 5[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

352.36

Formula

C₂₀H₁₇FN₂O₃

CAS No.

1363281-27-9

SMILES

O=C(N1CCC2=C(OC(COC3=CC=CC=C3)=N2)C1)C4=CC=C(F)C=C4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

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Product Name:
JNJ-46778212
Cat. No.:
HY-19559
Quantity:

JNJ-46778212

Cat. No.: HY-19559