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Repaglinide Potassium Channel inhibitor

Name: Repaglinide
Brand: Selleck Chemicals
SKU: S1426
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S1426

Repaglinide (AG-EE 623 ZW) is a potassium channel blocker, which lowers blood glucose by stimulating the release of insulin from the pancreas, used the treatment of type II diabetes.

Chemical Structure

Molecular Weight: 452.59

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Quality Control

Batch: Purity: 99.87%

99.87

Related Targets	CFTR CRM1 CD markers AChR Calcium Channel Sodium Channel GABA Receptor TRP Channel ATPase GluR
Other Potassium Channel Inhibitors	Nicorandil TRAM-34 Sophocarpine ML133 HCl Hydralazine HCl Gliquidone PAP-1 VU0071063 Apamin A2793

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (201.06 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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.
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

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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

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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.

Chemical Information, Storage & Stability

Molecular Weight	452.59	Formula	C₂₇H₃₆N₂O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	135062-02-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	AG-EE 623 ZW			Smiles	CCOC1=C(C=CC(=C1)CC(=O)NC(CC(C)C)C2=CC=CC=C2N3CCCCC3)C(=O)O

Mechanism of Action

Targets/IC₅₀/Ki	Potassium channel
In vitro	Repaglinide is found to bind with low affinity (K(D)=59 nM) to SUR1 alone, but with high affinity (increased approximately 150-fold) when SUR1 is co-expressed with Kir6.2. This compound binds with low affinity (K(D)=51 nM) to SUR1 co-expressed with Kir6.2DeltaN14. It lowers the plasma glucose concentration in the control rat, whilst failing to affect significantly the plasma insulin concentration or insulin/glucose ratio. Its administration affects neither plasma glucose nor insulin concentration, restores a normal value for the otherwise abnormally high basal insulin output, increases the 16.7 mM/2.8 mM ratio for insulin release, and again augmented protein biosynthesis at both low and high hexose concentrations in Goto-Kakizaki (GK) rats. It is found to bind to NCS proteins, but not to CaM or S100 proteins, in a Ca2+-dependent manner. This chemical antagonizes the inhibitory action of recoverin in a rhodopsin kinase assay with IC50 values of 400 mM. It tightly binds to the visinin-like domain of CCaMK and PpCaMK in a Ca2+-dependent manner and antagonizes the regulatory function of the domain with IC50 values of 55 and 4 mM for CCaMK and PpCaMK respectively.
In vivo	Repaglinide provokes a greater and more rapid increase in plasma insulin concentration and an earlier fall in glycemia than those observed after administration of the hypoglycemic sulfonylureas in both fed and starved normal rats.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15678092/ [2] https://pubmed.ncbi.nlm.nih.gov/12844348/ [3] https://pubmed.ncbi.nlm.nih.gov/9652342/ [4] https://pubmed.ncbi.nlm.nih.gov/9369378/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06290050	Recruiting	Healthy Volunteers	Takeda	March 29 2024	Phase 1

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