VU 0364770
VU 0364770 Basic information
- Product Name:
- VU 0364770
- Synonyms:
-
- VU 0364770
- 2-PyridinecarboxaMide, N-(3-chlorophenyl)-
- N-(3-Chlorophenyl)picolinamide
- N-(3-chlorophenyl)pyridine-2-carboxamide
- VU 0364770 100MG
- VU0364770;VU-0364770
- VU 0364770 USP/EP/BP
- SKL856
- CAS:
- 61350-00-3
- MF:
- C12H9ClN2O
- MW:
- 232.67
- Product Categories:
-
- Aromatics, Heterocycles
- Inhibitors
- Mol File:
- 61350-00-3.mol
VU 0364770 Chemical Properties
- Melting point:
- 81-83 °C
- Boiling point:
- 293.6±20.0 °C(Predicted)
- Density
- 1.341±0.06 g/cm3(Predicted)
- storage temp.
- Inert atmosphere,Store in freezer, under -20°C
- solubility
- DMF: 30 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 25 mg/ml; Ethanol: 5 mg/ml
- form
- Powder
- pka
- 11.24±0.70(Predicted)
- color
- Light yellow to yellow
VU 0364770 Usage And Synthesis
Uses
N-(3-Chlorophenyl)-2-pyridinecarboxamide shows positive allosteric modulation at the mGlu4 receptors in combination with other antagonists resulting in treatment for the neurodegenerative Parkinson’s disease (1).
in vivo
VU0364770 exhibits suitable pharmacokinetic properties for systemic dosing in animal models. After intravenous administration, VU0364770 is rapidly clears from the systemic circulation (165 ml/min/kg) and exhibits a volume of distribution of 2.92 L/kg. VU0364770 is a highly protein-bound ligand displaying free fractions of 2.7 and 1.8% in human and rat plasma, respectively. VU0364770 also shows an improved pharmacokinetic profile relative to previously reported mGlu4 PAMs with enhanced central penetration and a total brain-to-plasma ratio of more than 1 after systemic administration of a 10 mg/kg dose. VU0364770 produces a dose-dependent reversal of haloperidol-induced catalepsy. VU0364770 dose-dependently reverses haloperidol (0.75 mg/kg)-induced catalepsy in rats, significant at doses of 10 to 56.6 mg/kg, after subcutaneous dosing (F6,69=8.04; p<0.001)[1].
IC 50
Rat mGlu4: 290 nM (EC50); Human mGlu4: 1.1 μM (EC50); mGlu6: 6.8 μM (EC50); mGlu5: 17.9 μM (EC50)
VU 0364770Supplier
- Tel
- sales@boylechem.com
- Tel
- 18210857532; 18210857532
- jkinfo@jkchemical.com
- Tel
- 0757-86329057 18934348241
- sales4.gd@hwrkchemical.com
- Tel
- 0411-62910999 13889544652
- sales@meilune.com
- Tel
- 400-6206333 13167063860
- anhua.mao@aladdin-e.com
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