品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 5 mg/mL, clear (warmed)
儲存溫度
2-8°C
SMILES 字串
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
InChI 密鑰
RDLSKDOSNKLEAQ-UHFFFAOYSA-N
生化/生理作用
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).
特點和優勢
This compound is a featured product for Neuroscience research. Click here to discover more featured Neuroscience products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
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
商品
DISCOVER Bioactive Small Molecules for Neuroscience
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