For research use only. Not for therapeutic Use.
FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium[1][2].
FSCPX irreversibly blocks the binding of [3H]-8-cyclopentyl-1,3dipropylxanthine ([3H]DPCPX), with an IC50 of 11.8±3.2 nM in DDT1 MF2 cells[1].
FSCPX (20 μM; 48 h) attenuates protection from necrosis and apoptosis in A1AR-overexpressing LLC-PK1 cells[3].
FSCPX (2-20 μM; 48 h) reverses the upregulation of HSP27 mRNA and protein in A1AR-overexpressing LLC-PK1 cells without an effect on the mRNA or protein for HSP70[3].
Catalog Number | M099974 |
CAS Number | 156547-56-7 |
Synonyms | 3-(8-cyclopentyl-2,6-dioxo-1-propyl-7H-purin-3-yl)propyl 4-fluorosulfonylbenzoate |
Molecular Formula | C23H27FN4O6S |
Purity | ≥95% |
InChI | InChI=1S/C23H27FN4O6S/c1-2-12-28-21(29)18-20(26-19(25-18)15-6-3-4-7-15)27(23(28)31)13-5-14-34-22(30)16-8-10-17(11-9-16)35(24,32)33/h8-11,15H,2-7,12-14H2,1H3,(H,25,26) |
InChIKey | XJLGXHIRSHTRPQ-UHFFFAOYSA-N |
SMILES | CCCN1C(=O)C2=C(N=C(N2)C3CCCC3)N(C1=O)CCCOC(=O)C4=CC=C(C=C4)S(=O)(=O)F |
Reference | [1]. Beauglehole AR, et, al. New irreversible adenosine A(1) antagonists based on FSCPX. Bioorg Med Chem Lett. 2002 Nov 4; 12(21): 3179-82. [2]. Erdei T, et, al. FSCPX, a Chemical Widely Used as an Irreversible A₁ Adenosine Receptor Antagonist, Modifies the Effect of NBTI, a Nucleoside Transport Inhibitor, by Reducing the Interstitial Adenosine Level in the Guinea Pig Atrium. Molecules. 2018 Aug 3 [3]. Lee HT, et, al. Renal tubule necrosis and apoptosis modulation by A1 adenosine receptor expression. Kidney Int. 2007 Jun;71(12):1249-61. |