Nicorandil

SKU: orb1224341

Description

Nicorandil(Ikorel)is potassium channel activator. It acts by relaxing the smooth muscle of the blood vessels, especially those of the venous system. It does this through two methods. Firstly, by activating potassium channels, and secondly by donating nitric oxide to activate the enzyme guanylate cyclase. Guanylate cyclase causes activation of cGMP leading to both arterial and venous vasodilatation by de-phosphorylation of the myosin light chain.(In Vitro):Nicorandil (SG-75) activates ATP-sensitive K+ channels composed of Kir6.2 and either sulfonylurea receptor (SUR) 2A or 2B.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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 65141-46-0
• MW: 211.18
• Purity: >98% (HPLC)
• Formula: C₈H₉N₃O₄
• SMILES: O=[N+]([O-])OCCNC(C1=CN=CC=C1)=O
• Target: Potassium Channel
• Solubility: Ethanol: 42 mg/mL (198.89 mM); Water: 17 mg/mL (80.5 mM); DMSO: 42 mg/mL (198.89 mM)

Bioactivity

• In Vitro:
  Nicorandil (SG-75) activates ATP-sensitive K+ channels composed of Kir6.2 and either sulfonylurea receptor (SUR) 2A or 2B. 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.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

2-Nicotinamidoethyl nitrate | SG-75

Quick Database Links

Gene Symbol

Potassium Channel