2. GPCR/G Protein Neuronal Signaling
  3. mGluR
  4. VU0409106

VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB).

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VU0409106 Chemical Structure

VU0409106 Chemical Structure

CAS No. : 1276617-62-9

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Based on 1 publication(s) in Google Scholar

VU0409106 Related Antibodies

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Description

VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB)[1][2].

IC50 & Target

mGlu5

24 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
HEK293-A IC50
24 nM
Compound: 24, VU0409106
Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization preincubated for 140 seconds prior to glutamate-stimulation measured after 60 seconds
Negative allosteric modulation of rat mGlu5 receptor expressed in HEK293A cells assessed as inhibition of glutamate-induced calcium mobilization preincubated for 140 seconds prior to glutamate-stimulation measured after 60 seconds
[PMID: 24074843]
In Vivo

VU0409106 (10 mg/kg; i.p.; once) penetrates the blood-brain barrier (BBB) and demonstrates good brain to plasma ratio that near unity[1].

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

Animal Model: CD-1 mice[1]
Dosage: 10 mg/kg (10% Tween 80 formulation)
Administration: Intraperitoneal injection.
Result: 1.19 Pharmacokinetic Parameters of VU0409106 in CD-1 mice[1].
IP (10 mg/kg)
Plasma Tmax (h) 0.25
Plasma Cmax (ng/mL) 1450
Brain Tmax (h) 0.25
Brain Cmax (ng/mL) 1350
AUCplasma (ng/mL•h) 702
AUCbrain (ng/mL•h) 696
B/P ratio 0.99
Molecular Weight

330.34

Formula

C15H11FN4O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC1=CSC(NC(C2=CC(F)=CC(OC3=CN=CN=C3)=C2)=O)=N1
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 : 2 mg/mL (6.05 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0272 mL 15.1359 mL 30.2718 mL
5 mM 0.6054 mL 3.0272 mL 6.0544 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0272 mL 15.1359 mL 30.2718 mL 75.6796 mL
5 mM 0.6054 mL 3.0272 mL 6.0544 mL 15.1359 mL
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VU0409106 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VU04091061276617-62-9VU 0409106VU-0409106mGluRMetabotropic glutamate receptorsP450FXSautismantianxietyGERDPD-LIDInhibitorinhibitorinhibit

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