VU0364439

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Chemical Information

Product name：VU0364439	Purity：98% min
CAS NO：1246086-78-1	Solubility：DMSO : 50 mg/mL (118.40 mM)
Molecular Formula：C₁₈H₁₃Cl₂N₃O₃S	Package：Package according to customer requirements
Molecular Weight：422.285	Storage：Store at -20℃

Quality control

Remarks

VU 0364439 is a mGlu4 positive allosteric modulator (PAM), with EC50 of 19.8 nM. IC50 Value: 19.8 nM(EC50) Target: mGluR in vitro: in vivo: VU 0364439 possess less than ideal PK properties preventing their use as in vivo tools. It shows better stability in HLM (63% remaining) than RLM (2% remaining).

References

[1]. Hong, Sang-Phyo; Liu, Kevin G.; Ma, Gil et al. Tricyclic Thiazolopyrazole Derivatives as Metabotropic Glutamate Receptor 4 Positive Allosteric Modulators. Journal of Medicinal Chemistry (2011), 54(14), 5070-5081.

[2]. Engers, Darren W.; Gentry, Patrick R.; Williams, Richard et al. Synthesis and SAR of novel 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS). Bioorganic & Medicinal Chem