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    Neuronal Signaling
  2. mGluR
  3. VU6005649

VU6005649 

Cat. No.: HY-107982 Purity: 98.67%
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

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10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 150 In-stock
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50 mg USD 650 In-stock
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100 mg USD 1100 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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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[1]

mGlu7 Receptor

0.65 μM (EC50)

mGlu8 Receptor

2.6 μM (EC50)

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].

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

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].

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

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

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
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
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Keywords:

VU6005649VU 6005649VU-6005649mGluRMetabotropic glutamate receptorsInhibitorinhibitorinhibit

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VU6005649
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HY-107982
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