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MedChemExpress - Model PF-06256142 -1609583-14-3
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].MCE products for research use only. We do not sell to patients.
PF-06256142
MCE China：PF-06256142
Brand：MedChemExpress (MCE)
Cat. No.HY-119943
CAS：1609583-14-3
Purity：99.90%
Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Shipping：Room temperature in continental US; may vary elsewhere.
Description：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.
In Vitro：PF-06256142 exhibits IC50 values of 1 (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].
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].
IC50 & Target：Human D1 Receptor 33 nM (EC50)
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References：
[1]. Davoren JE, et al. Discovery and Lead Optimization of Atropisomer D1 Agonists with Reduced Desensitization. J Med Chem. 2018 Nov 15. [Content Brief]
Brand introduction:
• MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
• More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
• The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
• Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
• It has a professional experimental center and strict quality control and verification system；
• Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
• The biological activity of the products has been verified by the experiments of customers in various countries；
• A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
• Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
• It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。