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Nicorandil Potassium Channel activator

Name: Nicorandil
SKU: S1971
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S1971

Nicorandil (SG-75) is a potassium channel activator, and stimulates guanylate cyclase to increase formation of cyclic GMP (cGMP).

Chemical Structure

Molecular Weight: 211.17

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.92%

99.92

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Chemical Information, Storage & Stability

Molecular Weight	211.17	Formula	C₈H₉N₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	65141-46-0	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	SG-75			Smiles	C1=CC(=CN=C1)C(=O)NCCO[N+](=O)[O-]

Solubility

In vitro
Batch:

DMSO : 42 mg/mL (198.89 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 34 mg/mL

Water : 21 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	2.1mg/ml (9.94mM)	Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	Potassium channel ^[1]
In vitro	Nicorandil (100 mM) increases Flavoprotein oxidation but not membrane current; a 10-fold higher concentration recruits both mitoK(ATP) and surfaceK(ATP) channels. This compound bluntes the rate of cell death in a pelleting model of ischemia; this cardioprotective effect is prevented by the mitoK(ATP) channel blocker 5-hydroxydecanoate but is unaffected by the surfaceK(ATP) channel blocker HMR1098. ^[1] This chemical suppresses TUNEL positivity, cytochrome c translocation, caspase-3 activation and dissipation of mitochondrialinner membrane potential (Delta(Psi)(m)). It prevents Delta(Psi)(m) depolarization in a concentration-dependent manner (EC(50) approximately 40 mM, with saturation by 100 mM), as shown by fluorescence-activated cell sorter analysis of cells stained with a fluorescent Delta(Psi)(m)-indicator, tetramethylrhodamine ethyl ester (TMRE). ^[2] This compound activates a weakly inwardly-rectifying, glibenclamide-sensitive 80 pS K+ channel in both the transfected cells. It preferentially activates the K(ATP) channels containing SUR2B in HEK293T cells. ^[3] This chemical significantly suppresses the number of cells with TUNEL-positive nuclei and the increase in caspase-3 activity induced by 20 mM H2O2. It prevents the loss of DeltaPsim induced by H2O2 in a concentration-dependent manner. ^[4]
In vivo	Nicorandil (2.5 mg/kg daily, p.o.) combined with Amlodipine (5.0 mg/kg daily, p.o.) for 3 days significantly prevents these alterations and restored the enzyme activities to near normal in rats. ^[5]
References	[1] https://pubmed.ncbi.nlm.nih.gov/10676702/ [2] https://pubmed.ncbi.nlm.nih.gov/12204514/ [3] https://pubmed.ncbi.nlm.nih.gov/8768747/ [4] https://pubmed.ncbi.nlm.nih.gov/14568328/ [5] https://pubmed.ncbi.nlm.nih.gov/12619898/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06249581	Active not recruiting	Chronic Stable Angina	Auxilius Pharma sp.z.o.o.	November 27 2023	Early Phase 1
NCT02809456	Unknown status	Radiation Pneumonitis	Taipei Medical University WanFang Hospital	July 2016	Phase 2
NCT01396395	Completed	Stable Angina\|Coronary Disease	Merck KGaA Darmstadt Germany\|Merck Serono Co. Ltd. China	September 2011	Phase 4

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