| Chemical Properties | Back Directory | [density ]
1.34±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 200 mg/mL (514.88 mM; Need ultrasonic) | [form ]
Solid | [pka]
4.68±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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]. | [Biological Activity]
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 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]. | [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: | Rat[1] | | Dosage: | 5.0 mg/kg for i.v.; 5 mg/kg for oral (Pharmacokinetic Analysis) | | Administration: | Intravenous injection and oral administration | | Result: | Oral bioavailability (85%), T1/2 (2.3 h). |
| [IC 50]
Human D1 Receptor: 33 nM (EC50) | [References]
[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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| Company Name: |
InvivoChem
|
| Tel: |
13549236410 |
| Website: |
https://www.invivochem.cn/ |
| Company Name: |
Biorbyt Ltd.
|
| Tel: |
+44 (0)1223 859 353 |
| Website: |
www.biorbyt.com |
|