| Identification | Back Directory | [Name]
N-(4-Chloro-3-methoxyphenyl)-2-pyridinecarboxamide | [CAS]
1161205-04-4 | [Synonyms]
ML128
CS-626
VU 0361737
CID-44191096
VU0361737(ML128)
VU 0361737, >98%
1-(3,4-DICHLOROBENZYL)INDOLINE-2,3-DIONE
N-(4-CHLORO-3-METHOXYPHENYL)PICOLINAMIDE
VU 0361737;ML-128; VU-0361737; VU 0361737
ML-128; VU-0361737; VU 0361737;ML128;ML 128
N-(4-Chloro-3-methoxyphenyl)pyridine-2-carboxamide
N-(4-Chloro-3-methoxyphenyl)-2-pyridinecarboxamide
2-Pyridinecarboxamide, N-(4-chloro-3-methoxyphenyl)-
N-(4-Chloro-3-methoxyphenyl)-2-pyridinecarboxamide USP/EP/BP | [EINECS(EC#)]
200-256-5 | [Molecular Formula]
C13H11CIN2O2 | [MDL Number]
MFCD16618402 | [MOL File]
1161205-04-4.mol | [Molecular Weight]
263 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at RT | [solubility ]
DMSO: soluble15mg/mL (clear solution) | [form ]
film | [color ]
white | [InChI]
1S/C13H11ClN2O2/c1-18-12-8-9(5-6-10(12)14)16-13(17)11-4-2-3-7-15-11/h2-8H,1H3,(H,16,17) | [InChIKey]
ARYUXFNGXHNNDM-UHFFFAOYSA-N | [SMILES]
COc1cc(NC(=O)c2ccccn2)ccc1Cl |
| Safety Data | Back Directory | [Hazard Codes ]
Xn | [Risk Statements ]
22-36 | [Safety Statements ]
26 | [WGK Germany ]
3 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Acute Tox. 4 Oral
Eye Irrit. 2 |
| Hazard Information | Back Directory | [Uses]
VU0361737 is an mGluR4-specific positive allosteric modulator (PAM). | [Biological Activity]
vu0361737 is a selective, positive allosteric modulator and brain-permeable for mglur4 (mglu4 receptor), (ec?? = 240 and 110 nm for human and rat receptors respectively), >50 fold selectivity over other mglur subtypes. inactive at mglur-1, mglur-2, mglur-3, mglur-6 and mglur-7 receptors and showed weak activity at mglur-5 and mglur-8 receptors. [1]the mglur (metabotropic glutamate receptor) is a group of g-protein coupled receptors and is active through an indirect metabotropic process. mglur4 are invoinved in parkinson as it decrease gabaerigic transmission at inhibitory striato-pallidal synapse with the basal ganglia.[1][2]following the administration of vu0361737 into rat intraperitoneally (10mg/kg), the amount of compound present in brain and plasma was determined at 0.5, 1 and 8 hours. it showed a short half-life (t1/2 20 minutes) and a pronounced brain exposure (brain: plasma ratio = 4.1) [1] | [in vivo]
VU0361737 exhibits terminal elimination half-lives (rat 1.9 h) due to high plasma clearance (894 mL/min/kg) following Intraperitoneal injection ( rat 10 mg/kg)[1].
| Animal Model: | Male Sprague-Dawley rats (225-250 g)[1] | | Dosage: | 10 mg/kg (Pharmacokinetic Analysis) | | Administration: | Intraperitoneal injection | | Result: | T1/2 (1.9 h). |
| [IC 50]
Human mGlu4: 240 nM (EC50); Rat mGlu4: 110 nM (EC50) | [storage]
Room temperature | [References]
[1] engers dw, niswender cm, weaver cd, jadhav s, menon un, zamorano r, conn pj, lindsley cw, hopkins cr. 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.
[2] engers dw, field jr, le u, zhou y, bolinger jd, zamorano r, blobaum al, jones ck, jadhav s, weaver cd, conn pj, lindsley cw, niswender cm, hopkins cr. 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 chem. 2011 feb 24;54(4):1106-10. |
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