1. GPCR/G Protein Neuronal Signaling
  2. mGluR
  3. 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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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)

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.
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

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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VU0409106 Related Classifications

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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.

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Product Name:
VU0409106
Cat. No.:
HY-110180
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