PF-06256142

• CAT Number: I019442
• CAS Number: 1609583-14-3
• Molecular Formula: C21H16N4O2
• Molecular Weight: 356.38
• Purity: ≥95%
• Synonyms: 4-[3-methyl-4-(6-methylimidazo[1,2-a]pyrazin-5-yl)phenoxy]furo[3,2-c]pyridine;sulfane
• InChI: InChI=1S/C21H16N4O2.H2S/c1-13-11-15(27-21-17-6-10-26-18(17)5-7-23-21)3-4-16(13)20-14(2)24-12-19-22-8-9-25(19)20;/h3-12H,1-2H3;1H2
• InChIKey: NJSIQRYOTQSXMF-UHFFFAOYSA-N
• SMILES: CC1=C(C=CC(=C1)OC2=NC=CC3=C2C=CO3)C4=C(N=CC5=NC=CN54)C.S

PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 33 nM and 12 nM, respectively. PF-06256142 has the potential for the research of schizophrenia and Parkinson’s disease[1].
PF-06256142 exhibits IC50 values of <5 μM as an antagonist at the following 4 targets: M1 (4.9 μM); CB1 (2.1 μM); H1 (4.6 μM); Nav 1.5 (1.1 μM)[1]. PF-06256142 has an IC50 of approximately 12 μM for hERG[1]. PF-06256142 shows a Ki of 4.8 nM for D5 exquisitely selective than D2 (Ki>10 μM)[1].
PF-06256142 exhibits high oral bioavailability (rat 85%) following oral administration (rat 5 mg/kg)[1].
PF-06256142 exhibits terminal elimination half-life (rat 2.3 h) following intravenous administration (rat 5.0 mg/kg)[1].

Reference

[1]. Davoren JE, et al. Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. J Med Chem. 2018 Nov 15.
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