Bioactivity | NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues[1][2]. | ||||||||||||
Target | IC50: 8.3 µM (AC type V), 132 µM (AC type III) and 1.7 mM (AC type II) | ||||||||||||
Invitro | NKY80 (20 μM) blocks the elevations in both LVP and ventricular cAMP levels produced by the maximal concentration (10 nM)[2]. NKY80 (20 μM; 2 hours) completely blocks the increase in both cAMP content and renin release from isolated JG cells[3]. | ||||||||||||
Name | NKY80 | ||||||||||||
CAS | 299442-43-6 | ||||||||||||
Formula | C12H11N3O2 | ||||||||||||
Molar Mass | 229.23 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [1]. Onda T, et al. Type-specific regulation of adenylyl cyclase. Selective pharmacological stimulation and inhibitionof adenylyl cyclase isoforms. Biol Chem. 2001 Dec 21;276(51):47785-93. [2]. Harney JA, et al. Insulin-like stimulation of cardiac fuel metabolism by physiological levels of glucagon: involvement of PI3K but not cAMP. Am J Physiol Endocrinol Metab. 2008 Jul;295(1):E155-61. [3]. Ortiz-Capisano MC, et al. Adenylyl cyclase isoform v mediates renin release from juxtaglomerular cells. Hypertension. 2007 Mar;49(3):618-24. |