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1161205-04-4

1161205-04-4 structure
1161205-04-4 structure
  • Name: VU 0361737
  • Chemical Name: CID-44191096
  • CAS Number: 1161205-04-4
  • Molecular Formula: C13H11ClN2O2
  • Molecular Weight: 262.692
  • Catalog: Biochemical Inhibitor Neuronal Signaling GluR agonist
  • Create Date: 2017-10-28 12:22:29
  • Modify Date: 2024-01-04 19:10:00
  • VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.IC50 value: 110 nM (EC50, for rat ), 240 nM (EC50, for human)Target: mGlu4in vitro: VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. [3]in vivo: VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). [3]

Name CID-44191096
Synonyms 2-Pyridinecarboxamide (N-(4-chloro-3-methoxyphenyl)
N-(4-Chloro-3-methoxyphenyl)-2-pyridinecarboxamide
N-(4-Chloro-3-methoxyphenyl)pyridine-2-carboxamide
2-Pyridinecarboxamide, N-(4-chloro-3-methoxyphenyl)-
ML128
VU 0361737
VU0361737
Description VU 0361737 is a selective positive allosteric modulator (PAM) for mGlu4 receptor with EC50 of 240 nM and 110 nM at human and rat receptors, respectively, displays weak activity at mGlu5 and mGlu8 receptors, is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors.IC50 value: 110 nM (EC50, for rat ), 240 nM (EC50, for human)Target: mGlu4in vitro: VU0361737 is inactive at mGlu1, mGlu2, mGlu3, mGlu6 and mGlu7 receptors and displays weak activity at mGlu5 and mGlu8 receptors. [3]in vivo: VU0361737 shows high in vivo CL in rat, a short half-life (T1/2 20 min), and demonstrates significant brain exposure (brain-to-plasma ratio of 4.1). [3]
Related Catalog
References

[1]. Jantas D, et al. Neuroprotective effects of metabotropic glutamate receptor group II and III activators against MPP(+)-induced cell death in human neuroblastoma SH-SY5Y cells: the impact of cell differentiation state. Neuropharmacology. 2014 Aug;83:36-53

[2]. Jantas D, et al. Neuroprotective effects of mGluR II and III activators against staurosporine- and doxorubicin-induced cellular injury in SH-SY5Y cells: New evidence for a mechanism involving inhibition of AIF translocation. Neurochem Int. 2015 Sep;88:124

[3]. Engers DW, et al. Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs). J Med Chem. 2009 Jul 23;52(14):4115-8.

[4]. Engers DW, et al. Discovery, synthesis, and structure-activity relationship development of a series of N-(4-acetamido)phenylpicolinamides as positive allosteric modulators of metabotropic glutamate receptor 4 (mGlu(4)) with CNS exposure in rats. J Med Ch

Density 1.3±0.1 g/cm3
Boiling Point 329.8±37.0 °C at 760 mmHg
Molecular Formula C13H11ClN2O2
Molecular Weight 262.692
Flash Point 153.3±26.5 °C
Exact Mass 262.050903
PSA 54.71000
LogP 2.44
Appearance white
Vapour Pressure 0.0±0.7 mmHg at 25°C
Index of Refraction 1.633
Storage condition Store at RT
Water Solubility DMSO: soluble15mg/mL (clear solution)
Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H319
Precautionary Statements P305 + P351 + P338
Hazard Codes Xn
Risk Phrases 22-36
Safety Phrases 26
RIDADR NONH for all modes of transport