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| Targets |
PSB603's primary target is the adenosine A2B receptor (A2B-AR, A2BR), a G protein-coupled receptor activated by adenosine. It acts as a potent and selective antagonist, binding to the receptor with high affinity (Ki = 0.553 nM) and blocking the effects of adenosine. Its selectivity for A2B over A1, A2A, and A3 receptors is >17,000-fold, making it one of the most selective A2B antagonists available. This selectivity allows researchers to specifically study the role of A2B receptors without interference from other adenosine receptor subtypes.
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| ln Vitro |
PSB-603 possesses a Ki value of 0.553 nM for human A2B receptors, making it a strong and specific adenosine A2B receptor antagonist. It exhibits nearly minimal activity against human and rat A1 and A2A receptors, as well as human A3 receptors, at doses as low as 10 μM. Indifferent [1].
In vitro, PSB603 is a potent antagonist of the adenosine A2B receptor with a Ki of 0.553 nM. It displays >17,000-fold selectivity over A1, A2A, and A3 receptors. The compound shows virtually no affinity for human and rat A1 and A2A receptors and human A3 receptors up to 10 µM. Its activity is characterized by its ability to inhibit A2B receptor-mediated signaling, including cAMP production and calcium mobilization. PSB603 is a valuable tool for studying the physiological and pathological roles of A2B receptors. |
| ln Vivo |
PSB-603 exhibits anti-inflammatory effects in local and systemic inflammation models. PSB-603 (5 mg/kg bw ip) significantly reduced inflammation in two mouse models of inflammation (local and systemic). PSB-603 significantly reduces the levels of inflammatory cytokines IL-6, TNF-α, and ROS in inflamed paws and reduces peritoneal inflammation by significantly reducing leukocyte infiltration [4]. PSB-603 is administered as a suspension in 1% Tween 80 [4].
In vivo, PSB603 is used as a research tool to study the role of A2B adenosine receptors in various physiological and pathological processes. It has been used to investigate the involvement of A2B receptors in inflammation, fibrosis, cancer, and cardiovascular diseases. The compound's high selectivity and potency make it suitable for in vivo studies to elucidate the functions of A2B receptors. However, specific in vivo efficacy data is not detailed in the provided search results. |
| Enzyme Assay |
The in vitro activity of PSB603 is assessed using radioligand binding assays and functional assays. In radioligand binding assays, membrane preparations from cells expressing the A2B receptor are incubated with a radiolabeled A2B receptor ligand (e.g., [³H]PSB-603 or [³H]ZM-241385) in the presence of varying concentrations of PSB603. The displacement of the radiolabeled ligand is measured to determine the Ki. For selectivity profiling, binding assays are performed with A1, A2A, and A3 receptors using appropriate radioligands. In functional assays, cells expressing the A2B receptor are treated with PSB603 and stimulated with an A2B receptor agonist (e.g., NECA or BAY 60-6583). The inhibition of agonist-induced cAMP accumulation or calcium mobilization is measured to determine the antagonist potency.
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| Cell Assay |
Cell viability assay [3]
Cell Types: Peripheral T cells Tested Concentrations: 100 nM Incubation Duration: 24 hrs (hours) Experimental Results: Dramatically inhibited NECA-stimulated IL-6 release approximately 3-fold. For cellular assays, cells expressing the A2B receptor (e.g., CHO cells stably transfected with human A2B receptor) are cultured in appropriate media. Cells are treated with various concentrations of PSB603 (typically 0.01 nM to 10 µM) for 15-30 minutes before stimulation with an A2B receptor agonist. The inhibition of cAMP accumulation is measured using a competitive ELISA or by using a cAMP-sensitive reporter gene. Calcium mobilization is measured using fluorescent dyes (e.g., Fluo-4). The IC50 is determined from dose-response curves. Cell viability is assessed using MTT assays to ensure that observed effects are not due to cytotoxicity. |
| Animal Protocol |
Animal/Disease Models: Adult male albino Swiss mouse, CD-1, body weight 25-30 g[4]
Doses: 1, 5 or 10 mg/kg Route of Administration: intraperitonealprior to carrageenan injection Experimental Results: Carrageenan-induced edema model. The increase in paw edema was Dramatically inhibited in all groups receiving PSB-603. A dose of 5 mg/kg proved to be the most effective. In vivo, PSB603 is typically administered intraperitoneally or orally to animal models. The compound is formulated in a suitable vehicle (e.g., saline, DMSO, or a mixture of DMSO and saline) and administered at various doses (typically 0.1-10 mg/kg). The effects on A2B receptor-mediated responses are assessed by measuring relevant physiological or pathological parameters. For example, in models of inflammation, the compound's effect on inflammatory cytokine production or tissue damage is assessed. In models of fibrosis, the effect on collagen deposition and organ function is assessed. Specific protocols depend on the disease model being studied. |
| ADME/Pharmacokinetics |
PSB603 has a molecular weight of 528.01 g/mol and a molecular formula of C24H25ClN6O4S. It is soluble in DMSO. The compound should be stored at -20°C under appropriate conditions to maintain stability. Specific pharmacokinetic data (absorption, distribution, metabolism, excretion) is not available in the provided search results. Its bioavailability and half-life would require further investigation.
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| Toxicity/Toxicokinetics |
Specific toxicity data for PSB603 is not available in the provided search results. As a highly selective A2B receptor antagonist, it is not expected to have significant off-target toxicity. However, A2B receptor antagonism may affect various physiological processes, including inflammation, fibrosis, and vascular function. The compound should be used with caution in studies involving these processes. Comprehensive toxicological studies are required to establish its full safety profile. The compound should be handled with standard laboratory safety precautions.
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| References |
[1]. Thomas Borrmann, et al. 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity. J Med Chem. 2009 Jul 9;52
[2]. Mohamad Wessam Alnouri, et al. Selectivity is species-dependent: Characterization of standard agonists and antagonists at human, rat, and mouse adenosine receptors. Purinergic Signal. 2015 Sep;11(3):389-407. [3]. Nadine Borg, et al. CD73 on T Cells Orchestrates Cardiac Wound Healing After Myocardial Infarction by Purinergic Metabolic Reprogramming. Circulation. 2017 Jul 18;136(3):297-313. [4]. Magdalena Kotańska, et al. PSB 603 - a known selective adenosine A2B receptor antagonist-has anti-inflammatory activity in mice. Biomed Pharmacother. 2021 Mar;135:111164. |
| Additional Infomation |
PSB603 is a research compound used to study the role of adenosine A2B receptors in various physiological and pathological processes. Its high potency (Ki = 0.553 nM) and exceptional selectivity (>17,000-fold over other adenosine receptors) make it one of the most valuable tools available for A2B receptor research. The compound has been used in numerous studies to investigate the involvement of A2B receptors in inflammation, cancer, fibrosis, cardiovascular diseases, and other conditions. PSB603 is not approved for clinical use and is intended for research purposes only. It is available from chemical suppliers for research applications.
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| Molecular Formula |
C24H25CLN6O4S
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| Molecular Weight |
529.01
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| Exact Mass |
528.135
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| CAS # |
1092351-10-4
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| PubChem CID |
44185871
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| Appearance |
Off-white to light brown solid powder
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| LogP |
3.737
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
36
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| Complexity |
908
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCN1C(=O)NC2N=C(C3=CC=C(S(N4CCN(C5=CC=C(Cl)C=C5)CC4)(=O)=O)C=C3)NC=2C1=O
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| InChi Key |
OVHCTHHFOHMNFV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H25ClN6O4S/c1-2-11-31-23(32)20-22(28-24(31)33)27-21(26-20)16-3-9-19(10-4-16)36(34,35)30-14-12-29(13-15-30)18-7-5-17(25)6-8-18/h3-10H,2,11-15H2,1H3,(H,26,27)(H,28,33)
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| Chemical Name |
8-[4-[4-(4-chlorophenyl)piperazin-1-yl]sulfonylphenyl]-1-propyl-3,7-dihydropurine-2,6-dione
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| Synonyms |
PSB-603; PSB 603; PSB603
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| HS Tariff Code |
2934.99.9001
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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 : ~32.5 mg/mL (~61.44 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.67 mg/mL (3.16 mM) in 50% PEG300 +50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8903 mL | 9.4516 mL | 18.9032 mL | |
| 5 mM | 0.3781 mL | 1.8903 mL | 3.7806 mL | |
| 10 mM | 0.1890 mL | 0.9452 mL | 1.8903 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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