PZ0219
PF-06297470
≥98% (HPLC)
Synonym(s):
1-Methyl-3-(4-methyl-3-pyridinyl)-6-(2-pyridinylmethoxy)-1H-pyrazolo[3,4-b]pyrazine
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About This Item
Empirical Formula (Hill Notation):
C18H16N6O
CAS Number:
Molecular Weight:
332.36
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
51111800
MDL number:
InChI key
RDLSKDOSNKLEAQ-UHFFFAOYSA-N
SMILES string
CN(N=C1C2=C(C)C=CN=C2)C3=C1N=CC(OCC4=NC=CC=C4)=N3
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 5 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
PF-06297470 is a potent negative allosteric modulator of the Metabotropic Glutamate Receptor 5 (mGluR5).
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).
Features and Benefits
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Gopinath S Palanisamy et al.
Toxicologic pathology, 43(7), 995-1003 (2015-06-11)
Three orally administered metabotropic glutamate receptor 5 (mGluR5) negative allosteric modulators caused skin lesions consistent with delayed type-IV hypersensitivity in cynomolgus macaques in 2- and 12-week toxicity studies. Several monkeys developed macroscopic skin lesions in multiple locations after 8 to
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