MedChemExpress LLC (MCE)

MedChemExpress - Model PSB-603 - 1092351-10-4

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].

PSB-603

MCE China：PSB-603

Brand：MedChemExpress (MCE)

Cat. No.HY-103166

CAS：1092351-10-4

Purity：98.79%

Storage：Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Shipping：Room temperature in continental US; may vary elsewhere.

Description：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.

In Vitro：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[1].

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].

References：

[1]. Thomas Borrmann, et al. 1-alkyl-8-(piperazine-1-sulfonyl)phenylxanthines: development and characterization of adenosine A_2B receptor antagonists and a new radioligand with subnanomolar affinity and subtype specificity. J Med Chem. 2009 Jul 9;52(13):3994-4006. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[4]. Magdalena Kotańska, et al. PSB 603 - a known selective adenosine A_2B receptor antagonist-has anti-inflammatory activity in mice. Biomed Pharmacother. 2021 Mar;135:111164. [Content Brief]

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