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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].
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| 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].
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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. |
| 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. |
| 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. |
| 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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