Description
PF-04957325 is a highly potent and selective PDE8 inhibitor, with IC50s of 0.7 nM and 0.3 nM for PDE8A and PDE8B, respectively.
Product information
CAS Number: 1305115-80-3
Molecular Weight: 400.38
Formula: C14H15F3N8OS
Chemical Name: 3-{[(2R)-4-[(1,3-thiazol-2-yl)methyl]morpholin-2-yl]methyl}-5-(trifluoromethyl)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-7-amine
Smiles: NC1=NC(=NC2=C1N=NN2C[C@H]1CN(CC2=NC=CS2)CCO1)C(F)(F)F
InChiKey: VNLPYEMGHGDRRZ-MRVPVSSYSA-N
InChi: InChI=1S/C14H15F3N8OS/c15-14(16,17)13-20-11(18)10-12(21-13)25(23-22-10)6-8-5-24(2-3-26-8)7-9-19-1-4-27-9/h1,4,8H,2-3,5-7H2,(H2,18,20,21)/t8-/m1/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : ≥ 100 mg/mL (249.76 mM).
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-04957325 is over two orders of magnitude less efficient than PICL in suppressing polyclonal Teff cell proliferation, and shows no effect on cytokine gene expression in these cells, despite its robust effect on T cell adhesion. PF-04957325 is a selective PDE8 inhibitor and inhibits breast cancer cell migration. PF-04957325 greatly potentiates steroidogenesis in WT adrenal cells. PF-04957325 shows a reported IC50 of 0.7 nM against PDE8A, 0.2 nM against PDE8B, and > 1.5 μM against all other PDE isoforms. PF-04957325 treatment of WT Leydig cells or MA10 cells increases steroid production but has no effect in PDE8A (-/-)/B(-/-) double-knockout cells, confirming the selectivity of the drug. Moreover, under basal conditions, cotreatment with PF-04957325 plus rolipram, a PDE4-selective inhibitor, synergistically potentiates steroid production.
Products are for research use only. Not for human use.
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