Cat. No.: HY-15209

Copy Link Print Information

Repaglinide

(Synonyms: AG-EE 623ZW)

2 Cited Publications

Customer Review

Based on 2 publication(s) in Google Scholar

Repaglinide is an insulin secretagogue for the treatment of type-2 diabetes mellitus.

For research use only. We do not sell to patients.

Purity: 99.89%
CAS No.: 135062-02-1
Formula: C₂₇H₃₆N₂O₄
Molecular Weight:452.59

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Repaglinide Chemical Structure

CAS No.: 135062-02-1

Size

Price

Stock

Quantity

Amount: USD 0.00

* Please select Quantity before adding items.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (2)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

Repaglinide is an insulin secretagogue for the treatment of type-2 diabetes mellitus^[1].

Cellular Effect

Cell Line	Type	Value	Description	References
COS-1	IC₅₀	106 nM Compound: repaglinide	In vitro displacement of [3H]glibenclamide (IC50=0.61) from COS-1 cells expressing Sulfonylurea receptor 1 (SUR-1) In vitro displacement of [3H]glibenclamide (IC50=0.61) from COS-1 cells expressing Sulfonylurea receptor 1 (SUR-1)	[PMID: 15380228]
HEK293	IC₅₀	9.2 μM Compound: repaglinide	Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy Inhibition of 4-(4-(dimethylamino)styryl)-N-methylpyridinium uptake at human OCT1 expressed in HEK293 cells by confocal microscopy	[PMID: 18788725]
INS1(832/13)	IC₅₀	1.25 μM Compound: Repaglinide	Antidiabetic activity in glucose-treated rat INS1(832/13) cells assessed as increase in insulin release in presence of 3 mM glucose measured after 2 hrs by radioimmunoassay Antidiabetic activity in glucose-treated rat INS1(832/13) cells assessed as increase in insulin release in presence of 3 mM glucose measured after 2 hrs by radioimmunoassay	[PMID: 31812034]

In Vitro

Repaglinide reduces postprandial glucose levels by enhancing the early phase of insulin secretion and increasing the total amount of insulin secreted^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Repaglinide (AG-EE 623ZW) is very rapidly absorbed (t_max less than 1 hour) with a t_1/2 of less than one hour. Furthermore, Repaglinide is inactivated in the liver and more than 90 % excreted via the bile. Repaglinide (1 mg/kg p.o.) is effective (P<0.001) as an insulin-releasing agent in a rat model (low-dose streptozotocin) of type 2 diabetes.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 135062-02-1
Appearance Solid
Molecular Weight 452.59
Formula C₂₇H₃₆N₂O₄
Color White to off-white
SMILES

CC(C)C[C@H](NC(CC1=CC(OCC)=C(C(O)=O)C=C1)=O)C2=CC=CC=C2N3CCCCC3
Synonyms

AG-EE 623ZW
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (2)

All

Sort by:

Journal Impact Factor

Nat Commun

Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]

2026 Feb 12;17(1):1214. PMID: 41680175
Anal Biochem

Development and validation of a sensitive and fast bioanalytical LC-MS/MS assay for the quantitation of venetoclax and azacitidine in Rat Plasma: Application to pharmacokinetic study. [Abstract]

2025 Mar:698:115741. PMID: 39638140

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (110.48 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.2095 mL

11.0475 mL

22.0951 mL

5 mM

0.4419 mL

2.2095 mL

4.4190 mL

10 mM

0.2210 mL

1.1048 mL

2.2095 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.52 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Wang LC, et al. Characteristics of repaglinide and its mechanism of action on insulin secretion in patients with newly diagnosed type-2 diabetes mellitus.Medicine (Baltimore). 2018 Sep;97(38):e12476. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.2095 mL	11.0475 mL	22.0951 mL	55.2376 mL
	5 mM	0.4419 mL	2.2095 mL	4.4190 mL	11.0475 mL
	10 mM	0.2210 mL	1.1048 mL	2.2095 mL	5.5238 mL
	15 mM	0.1473 mL	0.7365 mL	1.4730 mL	3.6825 mL
	20 mM	0.1105 mL	0.5524 mL	1.1048 mL	2.7619 mL
	25 mM	0.0884 mL	0.4419 mL	0.8838 mL	2.2095 mL
	30 mM	0.0737 mL	0.3683 mL	0.7365 mL	1.8413 mL
	40 mM	0.0552 mL	0.2762 mL	0.5524 mL	1.3809 mL
	50 mM	0.0442 mL	0.2210 mL	0.4419 mL	1.1048 mL
	60 mM	0.0368 mL	0.1841 mL	0.3683 mL	0.9206 mL
	80 mM	0.0276 mL	0.1381 mL	0.2762 mL	0.6905 mL
	100 mM	0.0221 mL	0.1105 mL	0.2210 mL	0.5524 mL

Keywords

Product Name:
Cat. No.:
Quantity:
MCE Japan Authorized Agent:

Product Name:
CAS No.:
Species:
Purity:
Quantity:

Repaglinide

Anti-diabetic Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

Chemical Probe Library

FDA Approved & Pharmacopeial Drug Library

Anti-Alzheimer's Disease Compound Library

Anti-Pancreatic Cancer Compound Library

Neurodegenerative Disease-related Compound Library

Rare Diseases Drug Library

EMA-Approved Drug Library

Potassium Channel Compound Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Withdrawn Drug Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Mitochondrial Toxicity Compound Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Immunology/Inflammation Compound Library

Membrane Transporter/Ion Channel Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) Repaglinide

Biological Activity

Chemical Information

Publications (2)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Repaglinide Related Classifications

HY-15209 Related Classifications