1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. VU 0357121

VU 0357121 

Cat. No.: HY-15393 Purity: 99.85%
Handling Instructions

VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes.

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

VU 0357121 Chemical Structure

VU 0357121 Chemical Structure

CAS No. : 433967-28-3

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 456 In-stock
Estimated Time of Arrival: December 31
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200 mg   Get quote  

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Description

VU 0357121 is a positive and highly selective mGlu5R allosteric modulator (PAM) with an EC50 of 33 nM. VU 0357121 is inactive or very weakly antagonizing at other mGlu receptor subtypes[1].

IC50 & Target[1]

mGlu5 Receptor

33 nM (EC50)

In Vitro

VU 0357121 has the ability to enhance glutamate sensitivity of mGlu5 is likely due to the interaction at a site on the receptor distinct from the MPEP binding site. VU 0357121 does not bind at the MPEP allosteric site of mGlu5, thus does not possess mGlu5 NAM activity. The A809V/rmGlu5 mutation inhibited the ability of VU 0357121 to shift the glutamate concentration response curve, whereas the response to VU 0357121 is not altered by the F585I/rmGlu5 mutation. VU 0357121 shows weaker cooperativity in the Ca2+ mobilization assay in the low-expressing HEK293A-mGlu5 cell line[1].

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

Molecular Weight

305.32

Formula

C₁₇H₁₇F₂NO₂

CAS No.

433967-28-3

SMILES

O=C(NC1=CC=C(F)C=C1F)C2=CC=C(OCCCC)C=C2

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 : ≥ 50 mg/mL (163.76 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2753 mL 16.3763 mL 32.7525 mL
5 mM 0.6551 mL 3.2753 mL 6.5505 mL
10 mM 0.3275 mL 1.6376 mL 3.2753 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 (8.19 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (8.19 mM); Clear solution

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

VU 0357121VU0357121VU-0357121mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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Product Name:
VU 0357121
Cat. No.:
HY-15393
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