1. GPCR/G Protein
  2. mGluR

VU6005649 

Cat. No.: HY-107982 Purity: 98.91%
Handling Instructions

VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.

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

VU6005649 Chemical Structure

VU6005649 Chemical Structure

CAS No. : 2137047-43-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 556 In-stock
Estimated Time of Arrival: December 31
1 mg USD 228 In-stock
Estimated Time of Arrival: December 31
5 mg USD 708 In-stock
Estimated Time of Arrival: December 31
10 mg USD 1068 In-stock
Estimated Time of Arrival: December 31
25 mg USD 2148 In-stock
Estimated Time of Arrival: December 31
50 mg USD 3240 In-stock
Estimated Time of Arrival: December 31
100 mg USD 4440 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

VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively.

IC50 & Target

EC50: 0.65 μM (mGlu7 receptor ), 2.6 μM (mGlu8 receptor)[1]

In Vitro

VU6005649 is a CNS penetrant mGlu7/8 receptor agonist with EC50s of 0.65 μM and 2.6 μM for mGlu7 receptor and mGlu8 receptor, respectively. VU6005649 displays a terminal Kp of 2.43 with total brain levels ~9× above the mGlu7 positive allosteric modulator (PAM) in vitro EC50[1].

In Vivo

When VU6005649 (compound 9f) is dosed at 30 mg/kg IP in 10% Tween 80/H2O (0.75 mg/kg. s.c. amphetamine), no efficacy is observed in this assay. VU6005649 shows modest but significant pro-cognitive effects on associative learning in wild-type mice and the first example of efficacy of an mGlu7/8 positive allosteric modulator (PAM) in this model[1].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7989 mL 13.9946 mL 27.9893 mL
5 mM 0.5598 mL 2.7989 mL 5.5979 mL
10 mM 0.2799 mL 1.3995 mL 2.7989 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[1]

Tissue distribution studies with VU6005649 (compound 9f) in mice are performed by formulating VU6005649 in 10% polysorbate 80 and dosing via intraperitoneal injection to 20 week old female C57/Bl6 mice (3 per time point). At 0.25, 0.5, 1, 3, and 6 hours post dose, animals are euthanized and decapitated, blood is collected via cardiac puncture and the brains are removed, thoroughly washed in cold phosphate-buffered saline, and immediately frozen on dry ice[1].

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

References
Molecular Weight

357.28

Formula

C₁₆H₁₂F₅N₃O

CAS No.

2137047-43-7

SMILES

CC1=NN2C(N=C(C)C=C2C(F)(F)F)=C1C3=CC=C(OC)C(F)=C3F

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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Product Name:
VU6005649
Cat. No.:
HY-107982
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VU6005649

Cat. No.: HY-107982