| Bioactivity | AB-MECA is a high affinity A3 adenosine receptor agonist with a binding Ki of 430.5 nM for human A3 receptors in CHO cells. AB-MECA can enhance plasma histamine level[1][2][3][4]. | ||||||||||||
| Invitro | AB-MECA (1, 10, 100 μM; 24 小时) 在人肺癌细胞系 A549 中表现出剂量依赖性的细胞毒性[2]。 [125I]AB-MECA 在转染的 CHO 细胞和 RBL-2H3 细胞中与 A3 受体结合的 KD 值分别为 1.48 和 3.61 nM[3]。 Cell Cytotoxicity Assay[2] Cell Line: | ||||||||||||
| In Vivo | AB-MECA (3 ug/kg; 静脉注射) 可以提高小鼠血浆组胺水平[4]。 AB-MECA (0.3 mg/kg; 静脉注射) 增强雄性白化豚鼠 (体重 180-220 g) 中抗原诱导的支气管收缩[5]。 Animal Model: | ||||||||||||
| Name | AB-MECA | ||||||||||||
| CAS | 152918-26-8 | ||||||||||||
| Formula | C18H21N7O4 | ||||||||||||
| Molar Mass | 399.40 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. L Yates, et al. Radioligand binding and functional responses of ligands for human recombinant adenosine A(3) receptors. Auton Autacoid Pharmacol. 2006 Apr;26(2):191-200. [2]. Solanki, N. D., et al. In Vitro Evaluation Of Anti-Cancer Potential Of A3 Adenosine Receptor Agonist On A549 Human Lung Cancer Cell Line. Int J Pharm Pharm Sci ; 2019 Jun; 11(6): 106-108. [3]. X D Ji, et al. A selective agonist affinity label for A3 adenosine receptors. Biochem Biophys Res Commun. 1994 Aug 30;203(1):570-6. [4]. Endre G Mikus, et al. Interaction of SSR161421, a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo. Eur J Pharmacol. 2013 Jan 15;699(1-3):62-6. [5]. Endre G Mikus, et al. Evaluation of SSR161421, a novel orally active adenosine A3 receptor antagonist on pharmacology models. Eur J Pharmacol. 2013 Jan 15;699(1-3):172-9. |