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.
Product information
CAS Number: 1609583-14-3
Molecular Weight: 356.38
Formula: C21H16N4O2
Chemical Name: (S)-5-(4-{furo[3, 2-c]pyridin-4-yloxy}-2-methylphenyl)-6-methylimidazo[1, 2-a]pyrazine
Smiles: CC1N=CC2=NC=CN2C=1C1=CC=C(C=C1C)OC1N=CC=C2OC=CC2=1
InChiKey: HWAIAGZSWHOLLK-UHFFFAOYSA-N
InChi: InChI=1S/C21H16N4O2/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
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 200 mg/mL (514.88 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
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). PF-06256142 has an IC50 of approximately 12 μM for hERG. PF-06256142 shows a Ki of 4.8 nM for D5 exquisitely selective than D2 (Ki>10 μM).
In Vivo:
PF-06256142 exhibits high oral bioavailability (rat 85%) following oral administration (rat 5 mg/kg). PF-06256142 exhibits terminal elimination half-life (rat 2.3 h) following intravenous administration (rat 5.0 mg/kg).
Products are for research use only. Not for human use.
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