61350-00-3
2-PyridinecarboxaMide, N-(3-chlorophenyl)-
CAS: 61350-00-3
Molecular Formula: C12H9ClN2O
61350-00-3 - Names and Identifiers
61350-00-3 - Physico-chemical Properties
| Molecular Formula | C12H9ClN2O |
| Molar Mass | 232.67 |
| Density | 1.341±0.06 g/cm3(Predicted) |
| Melting Point | 81-83 °C |
| Boling Point | 293.6±20.0 °C(Predicted) |
| pKa | 11.24±0.70(Predicted) |
| Storage Condition | Inert atmosphere,Store in freezer, under -20°C |
| Physical and Chemical Properties | Bioactive VU0364770 is an effective selective mGlu4 positive allosteric regulator (PAM). The EC50 of the VU0346770 to rat mGlu4 and human mGlu4 receptors was 290 nM and 1.1 μM, respectively. VU0364770 has antagonistic activity to mGlu5, EC50 is 17.9 μM,VU0364770 has positive allosteric regulatory activity to mGlu6, EC50 is 6.8 μM. VU0364770 is also active on MAO, and the Ki values acting on human MAO-A and MAO-B are 8.5 and 0.72 μM respectively. |
| Use | Use N-(3-Chlorophenyl)-2-pyridinecarboxamide shows positive allosteric modulation at the mGlu4 receptors in combination with other. |
61350-00-3 - Upstream Downstream Industry
| Downstream Products | 2-AMINO-4-CHLOROBENZOTRIFLUORIDE |
61350-00-3 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 4.298 ml | 21.49 ml | 42.979 ml |
| 5 mM | 0.86 ml | 4.298 ml | 8.596 ml |
| 10 mM | 0.43 ml | 2.149 ml | 4.298 ml |
| 5 mM | 0.086 ml | 0.43 ml | 0.86 ml |
Last Update：2024-01-02 23:10:35
61350-00-3 - Uses and synthesis methods
in vitro study
VU0364770 is a selective positive allosteric modulator of mGlu 4 in recombinant systems. VU0364770 is a potent PAM of multiple signaling pathways that enhances the response of the rat and human mGlu 4 receptors to the endogenous agonist glutamate. VU0364770 produces a concentration-dependent potentiation of the response to an EC 20 concentration of glutamate with EC 50 of 1.1±0.2 μM and increases the maximal response to glutamate from 100 to 227±17%. Because of concerns that this chemical scaffold might possess activity at MAO, full IC 50 determinations is performed for VU0364770 at the MAO-A and MAO-B isoforms; these studies result in K I s of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively. When tested at a 10 μM concentration at each mGlu receptor, VU0364770 exhibits weak PAM activity (4.3-fold left shift of the glutamate CRC) at mGlu6 and antagonist activity (3.3-fold right shift of the glutamate CRC) at mGlu5 (compare to the 16.5-fold left shift of the glutamate concentration-response for mGlu 4 at 10 μM). When further evaluated in a full concentration-response curve format, VU0364770 exhibits antagonist activity at mGlu 5 with a potency of 17.9±5.5 μM and PAM activity at mGlu 6 with a potency of 6.8±1.7 μM (compare with the potency of VU0364770 on the rat mGlu 4 receptor of 290±80 nM).
in vivo studies
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 mGlu 4 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 (F 6,69 =8.04; p<0.001).
Last Update：2024-04-09 19:04:55
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Spot supply
Product Name: VU 0364770 Visit Supplier Webpage Request for quotationCAS: 61350-00-3
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
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