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Purity: ≥98%
Nicorandil (formerly RP46417; SG-75; SG75; RP-46417; Dancor and Adancor) is a potassium channel activator that has been approved as a vasodilatory drug to treat angina. It stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP). Nicorandil causes vasodilatation of arterioles and large coronary arteries. Nicorandal's nitrate-like properties produce venous vasodilation through stimulation of guanylate cyclase.
| ln Vitro |
Nicorandil (SG-75) activates ATP-sensitive K+ channels consisting of Kir6.2 and either sulfonylurea receptor (SUR) 2A or 2B[1]. Nicorandil is a vasodilatory medication used to treat angina. Nicorandil (SG-75) activates guanylate cyclase to promote synthesis of cyclic GMP (cGMP). cGMP stimulates protein kinase G (PKG) which phosphorylates and inhibits GTPase RhoA and reduces Rho-kinase activity. Reduced Rho-kinase activity promotes an increase in myosin phosphatase activity, lowering the calcium sensitivity of the smooth muscle. PKG also activates the sarcolemma calcium pump to remove activating calcium. PKG operates on K+ channels to increase K+ efflux and the resulting hyperpolarization inhibits voltage-gated calcium channels. Overall, this leads to relaxation of the smooth muscle and coronary vasodilation[2][3].
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| ln Vivo |
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| 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. |
| Molecular Formula |
C8H9N3O4
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| Molecular Weight |
211.17
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| CAS # |
65141-46-0
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| Related CAS # |
Nicorandil-d4;1132681-23-2
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| SMILES |
O(C([H])([H])C([H])([H])N([H])C(C1=C([H])N=C([H])C([H])=C1[H])=O)[N+](=O)[O-]
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| InChi Key |
LBHIOVVIQHSOQN-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-(nicotinamido)ethyl nitrate
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.84 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.84 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.7355 mL | 23.6776 mL | 47.3552 mL | |
| 5 mM | 0.9471 mL | 4.7355 mL | 9.4710 mL | |
| 10 mM | 0.4736 mL | 2.3678 mL | 4.7355 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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