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FSCPX 

Cat. No. M28604
FSCPX  Structure
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Quality Control & Documentation
Biological Activity

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.

Chemical Information
Molecular Weight 506.55
Formula C23H27FN4O6S
CAS Number 156547-56-7
Form Solid
Solubility (25°C) DMSO 50 mg/mL (ultrasonic and warming and heat to 60°C)
Storage Powder -20°C
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Gabor Viczjan, et al. Int J Mol Sci. A Body of Circumstantial Evidence for the Irreversible Ectonucleotidase Inhibitory Action of FSCPX, an Agent Known as a Selective Irreversible A1 Adenosine Receptor Antagonist So Far

[2] Adrienn Monika Szabo, et al. Molecules. An Advanced In Silico Modelling of the Interaction between FSCPX, an Irreversible A1 Adenosine Receptor Antagonist, and NBTI, a Nucleoside Transport Inhibitor, in the Guinea Pig Atrium

[3] Tamas Erdei, et al. Molecules. 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

[4] Anthony R Beauglehole, et al. Bioorg Med Chem Lett. New irreversible adenosine A(1) antagonists based on FSCPX

[5] J E van Muijlwijk-Koezen, et al. Bioorg Med Chem Lett. Synthesis and use of FSCPX, an irreversible adenosine A1 antagonist, as a 'receptor knock-down' tool

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Keywords: FSCPX  supplier, Adenosine Receptor, inhibitors, activators


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