| Bioactivity | 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]. | ||||||||||||
| Invitro | PF-06256142 exhibits IC50 values of 10 μM)[1]. | ||||||||||||
| In Vivo | 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]. Animal Model: | ||||||||||||
| Name | PF-06256142 | ||||||||||||
| CAS | 1609583-14-3 | ||||||||||||
| Formula | C21H16N4O2S | ||||||||||||
| Molar Mass | 388.44 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Davoren JE, et al. Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. J Med Chem. 2018 Nov 15. |
PF-06256142
CAS: 1609583-14-3 F: C21H16N4O2S W: 388.44
PF-06256142 is a potent, selective, CNS-penetrant and orally active agonist of the D1 receptor, with an EC50 and Ki of 3
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