PSB 603

PSB-603 是一种有效的高选择性 A2B 腺苷受体拮抗剂，Ki 为 0.553 nM，对人和大鼠 A1 和 A2A 以及人 A3 受体几乎没有亲和力。

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5mg

￥1603.00

650.00

- +
10mg

￥2863.00

1000.00

- +
25mg

￥6548.00

2200.00

- +
500mg

￥25000.00

0.00

- +

已选 0 种 0 瓶

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Adenosine A2B receptor antagonist

货号：ajci10548
CAS：1092351-10-4
分子式：C24H25ClN6O4S
分子量：529.01
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

参考文献：

[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.