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ST034307

CAS No.: 133406-29-8

ST034307 is an effective and selective inhibitor of adenylyl cyclase 1 (IC50: 2.3 μM).
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Description ST034307 is an effective and selective inhibitor of adenylyl cyclase 1 (IC50: 2.3 μM).
In vitro ST034307 显著抑制在稳定表达AC1的HEK细胞中,由forskolin或isoproterenol刺激产生的AC1活性。ST034307 显著降低海马匀浆中Ca2+/calmodulin刺激下的cAMP积累。ST034307 剂量依赖性地抑制MOR介导的AC1敏感化的发展和维持。ST034307 显示出对AC1的选择性抑制,并在较小程度上增强AC8活性,但这种增强不具有显著性。ST034307 增强了由AC2催化的,phorbol 12-myristate 13-acetate (PMA)刺激下的cAMP产生。ST034307 对野生型HEK细胞没有显著影响[1]。
In vivo ST034307 在老鼠疼痛模型中展示了其止痛效力的估计中位有效剂量(E50)值为0.28 μg。ST034307(0.25 μg)在老鼠中引发了明显的CFA诱发的炎症疼痛缓解[1]。
Target activity AC type I:2.3 μM
molecular weight 297.95
Molecular formula C10H4Cl4O2
CAS 133406-29-8
Storage Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Solubility DMSO: 50 mg/mL (167.81 mM), Sonication and heating are recommended.
References 1. Brust TF, et al. Identification of a selective small-molecule inhibitor of type 1 adenylyl cyclase activity with analgesic properties. Sci Signal. 2017 Feb 21;10(467).