| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Adenosine A1 receptor. FSCPX is a potent and selective antagonist of the adenosine A1 receptor. It has a high affinity for the A1 receptor, with a Ki in the low nanomolar range. It shows significantly lower affinity for other adenosine receptor subtypes, making it a valuable tool for studying the role of A1 receptors.
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| ln Vitro |
In DDT1 MF2 cells, FSCPX has an IC50 of 11.8±3.2 nM, which is an irreversible block of [3H]-8-cyclopentyl-1,3dipropylxanthine ([3H]DPCPX; 1]. When applied to A1AR-overexpressing LLC-PK1 cells, FSCPX (20 μM; 48 hours) reduces their resistance to necrosis and apoptosis [3]. A1AR-overexpressing LLC-PK1 cells that have their HSP27 mRNA and protein overexpressed reversed when treated with FSCPX (2–20 μM) after 48 hours [3]. HSP70 mRNA and protein unaffected.
FSCPX potently antagonizes the adenosine A1 receptor in vitro. In receptor binding assays, it has a high affinity for the A1 receptor. In functional assays, it can block the effects of A1 agonists, such as the inhibition of adenylate cyclase. Its selectivity over other adenosine receptor subtypes has been characterized. |
| ln Vivo |
In vivo, FSCPX has been used to study the role of adenosine A1 receptors in a variety of physiological processes. It has been shown to modulate cardiovascular function, neuroprotection, and pain perception in animal models. By blocking A1 receptors, it can reverse the effects of A1 agonists, providing insights into the specific functions of this receptor subtype.
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| Enzyme Assay |
In vitro receptor binding assays for FSCPX involve measuring its affinity for adenosine A1, A2A, A2B, and A3 receptors using radioligand binding techniques. Membranes from cells expressing the receptors are incubated with radiolabeled ligands, such as [3H]DPCPX, and increasing concentrations of FSCPX. Ki values are determined.
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| Cell Assay |
Cellular assays for FSCPX involve treating cells expressing adenosine A1 receptors with the compound and measuring its effects on receptor-mediated signaling, such as the inhibition of adenylate cyclase. The compound's ability to block agonist-induced inhibition of cAMP accumulation is assessed.
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| Animal Protocol |
In vivo animal studies for FSCPX typically involve administration to rodent models to assess its effects on cardiovascular function, neuroprotection, or pain. The compound's ability to reverse the effects of A1 agonists, such as the bradycardic effect of adenosine, is often assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for FSCPX is limited. As a research tool, its properties such as bioavailability and half-life are typically characterized in preclinical studies.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of FSCPX are limited. As a research tool, its safety profile is primarily assessed in the context of in vivo efficacy studies.
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| References |
[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. |
| Additional Infomation |
FSCPX is a potent and selective antagonist of the adenosine A1 receptor, used as a research tool to study the role of A1 receptors in cardiovascular function, neuroprotection, and pain modulation.
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| Molecular Formula |
C23H27N4O6FS
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|---|---|
| Molecular Weight |
506.54708
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| Exact Mass |
506.164
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| CAS # |
156547-56-7
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| PubChem CID |
133012
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| Appearance |
Solid powder
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| Vapour Pressure |
3.28E-21mmHg at 25°C
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| LogP |
3.94
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
35
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| Complexity |
898
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCN1C(=O)N(CCCOC(C2C=CC(S(F)(=O)=O)=CC=2)=O)C2N=C(NC=2C1=O)C1CCCC1
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| InChi Key |
XJLGXHIRSHTRPQ-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
3-(8-cyclopentyl-2,6-dioxo-1-propyl-7H-purin-3-yl)propyl 4-fluorosulfonylbenzoate
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| HS Tariff Code |
2934.99.03.00
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~98.71 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.94 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9741 mL | 9.8707 mL | 19.7414 mL | |
| 5 mM | 0.3948 mL | 1.9741 mL | 3.9483 mL | |
| 10 mM | 0.1974 mL | 0.9871 mL | 1.9741 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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