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NKY 80

Names

[ CAS No. ]:
299442-43-6

[ Name ]:
NKY 80

[Synonym ]:
BCX 34
PELDESINE
2-Amino-7-(2-furanyl)-7,8-dihydro-5(6H)-quinazolinone
Peldesine

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Adenylate Cyclase
Research Areas >> Metabolic Disease

[Target]

IC50: 8.3 µM (AC type V), 132 µM (AC type III) and 1.7 mM (AC type II)[1]


[In Vitro]

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].

[References]

[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.

Chemical & Physical Properties

[ Molecular Formula ]:
C12H11N3O2

[ Molecular Weight ]:
229.23500

[ Exact Mass ]:
229.08500

[ PSA ]:
82.01000

[ LogP ]:
2.14570

[ Storage condition ]:
2-8°C

MSDS

Safety Information

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ Hazard Codes ]:
T

[ RIDADR ]:
UN 2811 6.1 / PGIII

[ HS Code ]:
2934999090

Customs

[ HS Code ]: 2934999090

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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