Nicorandil

Nicorandil is a potassium channel activator and stimulates guanylate cyclase to increase formation of cyclic GMP cGMP

Product information

CAS Number: 65141-46-0

Molecular Weight: 211.17

Formula: C8H9N3O4

Synonym:

SG-75

Chemical Name: 2-Nicotinamidoethyl nitrate

Smiles: [O-][N+](=O)OCCNC(=O)C1=CN=CC=C1

InChiKey: LBHIOVVIQHSOQN-UHFFFAOYSA-N

InChi: InChI=1S/C8H9N3O4/c12-8(7-2-1-3-9-6-7)10-4-5-15-11(13)14/h1-3,6H,4-5H2,(H,10,12)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 33 mg/mL (156.27 mM)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

Nicorandil (SG-75) activates ATP-sensitive K+ channels composed of Kir6.2 and either sulfonylurea receptor (SUR) 2A or 2B[1]. Nicorandil is a vasodilatory drug used to treat angina. Nicorandil (SG-75) stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). cGMP activates protein kinase G (PKG) which phosphorylates and inhibits GTPase RhoA and decreases Rho-kinase activity. Reduced Rho-kinase activity permits an increase in myosin phosphatase activity, decreasing the calcium sensitivity of the smooth muscle. PKG also activates the sarcolemma calcium pump to remove activating calcium. PKG acts on K+ channels to promote K+ efflux and the ensuing hyperpolarization inhibits voltage-gated calcium channels. Overall, this leads to relaxation of the smooth muscle and coronary vasodilation[2][3].

References:

1. Mitsuhiko Yamada, et al. The nucleotide-binding domains of sulfonylurea receptor 2A and 2B play different functional roles in nicorandil-induced activation of ATP-sensitive K+ channels. Mol Pharmacol. 2004 May;65(5):1198-207.
2. Nakae, I., et al., Effects of intravenous nicorandil on coronary circulation in humans: plasma concentration and action mechanism. J Cardiovasc Pharmacol, 2000. 35(6): p. 919-25.
3. Sauzeau, V., et al., Cyclic GMP-dependent protein kinase signaling pathway inhibits RhoA-induced Ca2+ sensitization of contraction in vascular smooth muscle. J Biol Chem, 2000. 275(28): p. 21722-9.

Products are for research use only. Not for human use.