| Identification | Back Directory | [Name]
1-Methyl-3-(4-methyl-3-pyridinyl)-6-(2-pyridinylmethoxy)-1H-pyrazolo[3,4-b]pyrazine | [CAS]
1539296-45-1 | [Synonyms]
PF-06297470
PF-06297470 >=98% (HPLC)
1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)pyrazolo[3,4-b]pyrazine
1-Methyl-3-(4-methyl-3-pyridinyl)-6-(2-pyridinylmethoxy)-1H-pyrazolo[3,4-b]pyrazine
1H-Pyrazolo[3,4-b]pyrazine, 1-methyl-3-(4-methyl-3-pyridinyl)-6-(2-pyridinylmethoxy)- | [Molecular Formula]
C18H16N6O | [MDL Number]
MFCD28100803 | [MOL File]
1539296-45-1.mol | [Molecular Weight]
332.36 |
| Chemical Properties | Back Directory | [Boiling point ]
526.8±45.0 °C(Predicted) | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: soluble5mg/mL, clear (warmed) | [form ]
powder | [pka]
3.12±0.12(Predicted) | [color ]
white to beige | [InChI]
1S/C18H16N6O/c1-12-6-8-19-9-14(12)16-17-18(24(2)23-16)22-15(10-21-17)25-11-13-5-3-4-7-20-13/h3-10H,11H2,1-2H3 | [InChIKey]
RDLSKDOSNKLEAQ-UHFFFAOYSA-N | [SMILES]
CN(N=C1C2=C(C)C=CN=C2)C3=C1N=CC(OCC4=NC=CC=C4)=N3 |
| Safety Data | Back Directory | [Hazard Codes ]
Xn | [Risk Statements ]
22 | [WGK Germany ]
3 | [Storage Class]
11 - Combustible Solids | [Hazard Classifications]
Acute Tox. 4 Oral |
| Hazard Information | Back Directory | [Uses]
PF470 (PF-06297470) is a negative allosteric modulator of metabotropic glutamate receptor 5 (mGluR5) with significant efficacy in Parkinson's disease models, but clinical development was halted due to potential issues found in toxicology studies. | [Biological Activity]
PF-06297470 is a potent negative allosteric modulator of the Metabotropic Glutamate Receptor 5 (mGluR5). PF-06297470 binds to mGluR5 with a Ki of 0.9 nM. The compound PF-06297470 displays slight antagonism of mGluR1 (IC50 = 30.5 mM)with no agonist or antagonist activities against any other mGlu receptor subtype at concentrations up to 50 mM. PF-06297470 reduces dyskinesia in a rodent (MPTP)-rendered Parkinsonian model of L-DOPA-induced dyskinesia (PD-LID). | [References]
[1] Discovery and preclinical characterization of 1-methyl-3-(4-methylpyridin-3-yl)-6-(pyridin-2-ylmethoxy)-1H-pyrazolo-[3,4-b]pyrazine (PF470): a highly potent, selective, and efficacious metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulator |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|