| Identification | Back Directory | [Name]
8-[4-[4-(4-Chlorophenzyl)piperazide-1-sulfonyl)phenyl]]-1-propylxanthine | [CAS]
1092351-10-4 | [Synonyms]
PSB 603
PSB-603 >=98% (HPLC)
8-[4-[4-(4-Chlorophenzyl)piperazide-1-sulfonyl)phenyl]]-1-propylxanthine
1H-Purine-2,6-dione, 8-[4-[[4-(4-chlorophenyl)-1-piperazinyl]sulfonyl]phenyl]-3,9-dihydro-1-propyl- | [Molecular Formula]
C24H25ClN6O4S | [MDL Number]
MFCD11519964 | [MOL File]
1092351-10-4.mol | [Molecular Weight]
529.01 |
| Chemical Properties | Back Directory | [Melting point ]
>298 °C (decomp) | [density ]
1.430±0.06 g/cm3(Predicted) | [storage temp. ]
Store at +4°C | [solubility ]
Soluble to 50 mM in DMSO | [form ]
Powder | [pka]
7.37±0.70(Predicted) | [color ]
Off-white to light brown |
| Hazard Information | Back Directory | [Uses]
PSB-603 is a potent and highly selective A2B adenosine receptor antagonist exhibiting a Ki value of 0.553 nM and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM[1]. | [Biological Activity]
PSB-603 is an adenosine receptor A2b antagonist (IC50 = 1.13 nM against 10 μM A2bR agonist NECA-induced calcium response in Jurk at T cells in the presence of 200 nM A2aR antagonist MSX-2) th at targets A2bR with high affinity (KD = 0.403 nM/human0.457 nM/rat4.09 nM/mouse A2bR; Ki against 0.3 nM [3H]PSB-603 = 0.553 nM/human0.355 nM/rat0.265 nM/mouse A2bR) and selectivityexhibiting little affinity toward A1A2aor A3 adenosine receptors by competition binding assay (Ki >10 μM against 0.4 nM [3H]DPCPX for human/r at A1R1 nM [3H]MSX-2 for human/mouse/r at A2aR10 nM [3H]NECA for human/mouse/r at A3R) with the exception of mouse A1R (Ki = 42.2 nM against 0.4 nM [3H]DPCPX).''PSB-603 is known to modify cellular metabolism and enhance cellular sensitivity for chemotherapy. ThusPSB-603 is recognized to possess anticancer actionwhich has been studied in colorectal cancer. | [in vivo]
PSB-603 shows anti-inflammatory effect in local and systemic inflammation models. PSB-603 (5 mg/kg b.w. ip) significantly reduces inflammation in two mice models of inflammation (local and systemic). PSB-603 significantly decreases levels of the inflammatory cytokines IL-6, TNF-α and of ROS in the inflamed paw and reduces inflammation of the peritoneum by significantly decreasing the infiltration of leukocytes[4].
PSB-603 is administered as suspensions in 1 % Tween 80[4]. | Animal Model: | Adult male Albino Swiss mice, CD-1, weighing 25-30 g[4] | | Dosage: | 1, 5 or 10 mg/kg | | Administration: | Administered intraperitoneally (ip), prior to carrageenan injection | | Result: | Carrageenan-induced edema model. The increase in paw oedema was significantly inhibited in all groups receiving PSB-603. The dose of 5 mg/kg turned out to be the most active.
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| [storage]
Store at -20°C | [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(13):3994-4006. DOI:10.1021/jm900413e
[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. DOI:10.1007/s11302-015-9460-9
[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. DOI:10.1161/CIRCULATIONAHA.116.023365
[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. DOI:10.1016/j.biopha.2020.111164 |
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| Company Name: |
Energy Chemical
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| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
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