Description
PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11.
Product information
CAS Number: 1415637-72-7
Molecular Weight: 413.40
Formula: C20H18F3N7
Chemical Name: 4-[4-(azetidin-1-yl)-1-methyl-1H-pyrazolo[3,4-d]pyrimidin-3-yl]-1-methyl-5-[4-(trifluoromethyl)phenyl]-1H-pyrazole
Smiles: CN1N=CC(=C1C1C=CC(=CC=1)C(F)(F)F)C1=NN(C)C2=NC=NC(=C12)N1CCC1
InChiKey: SHAVEYUXRBIMLA-UHFFFAOYSA-N
InChi: InChI=1S/C20H18F3N7/c1-28-17(12-4-6-13(7-5-12)20(21,22)23)14(10-26-28)16-15-18(29(2)27-16)24-11-25-19(15)30-8-3-9-30/h4-7,10-11H,3,8-9H2,1-2H3
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 62.5 mg/mL (151.19 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-05085727 shows weak activity with IC50 of 162 μM to induce cell death in a cellular toxicity assay using transformed human liver endothelial (THLE) cells. PF-05085727 (3 μM) shows a minimal inhibition of cytochrome P450 enzymes (CYPs), inhibits 1A2, 2C8, 2C9, 2D6 and 3A4 with percentage% of 16%, 18%, 7%, 4%, and 30%, respectively. PF-05085727 (10 μM) inhibits PDE1B, PDE4B, PDE7B and PDE10A with IC50 values of 12.146 μM, 22,503 μM, 13.157 μM and 6.515 μM, respectively.
In Vivo:
PF-05085727 (subcutaneous injection; 3.2 mg/kg/mice; 3 mg/kg/rat) gives a ratio of unbound brain (Cbu) to unbound plasma (Cpu) of ca. 0.27 and 0.37, respectively. PF-05085727 in mice leads to an acute and exposure-dependent elevation in the accumulation of bulk levels of cGMP in cortex, striatum, and hippocampus as measured by enzyme-linked immunosorbent assay.
Products are for research use only. Not for human use.
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