PSB-603

Research use only, not for human use.

Adenosine A2B receptor antagonist.

Adenosine A2B receptor antagonist.(In Vitro):In peripheral T cells, PSB-603 (100 nM) inhibits NECA-stimulated IL-6 release about 3-fold. PSB-603 (10 μM) shows no affinity for the human and rat A1 and A2A and human A3 receptors.(In Vivo):PSB-603 (5 mg/kg; i.p.) significantly reduces inflammation in local and systemic mice models of inflammation. In the inflamed paw, PSB-603 significantly decreases the levels of the inflammatory cytokines including IL-6, TNF-α and of ROS. PSB-603 reduces inflammation of the peritoneum by decreasing the infiltration of leukocytes.

PSB-603 is a potent and selective adenosine A2B receptor antagonist exhibiting a Ki value of 0.553 nM at the human A2B receptor and virtually no affinity for the human and rat A1 and A2A and the human A3 receptors up to a concentration of 10 μM. Cell Viability Assay Cell Line:Peripheral T cells Concentration:100 nM Incubation Time:24 hours Result:Significantly inhibited NECA stimulated IL-6 release ≈3-fold.

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. PSB-603 is administered as suspensions in 1 % Tween 80. Animal Model:Adult male Albino Swiss mice, CD-1, weighing 25-30 g 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.

PSB 603

Others

Other Targets

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1092351-10-4

529.01

C24H25ClN6O4S

>98% (HPLC)

In Vitro:?DMSO : 32.5 mg/mL (61.44 mM)

CCCn1c(O)nc2nc([nH]c2c1=O)-c1ccc(cc1)S(=O)(=O)N1CCN(CC1)c1ccc(Cl)cc1

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(-20℃)

With Ice Pack

≥ 2 years