1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. Repaglinide

Repaglinide  (Synonyms: AG-EE 623ZW)

Cat. No.: HY-15209 Purity: 99.88%
SDS COA Handling Instructions

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

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

Repaglinide Chemical Structure

Repaglinide Chemical Structure

CAS No. : 135062-02-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 80 In-stock
Solution
10 mM * 1 mL in DMSO USD 80 In-stock
Solid
50 mg USD 73 In-stock
100 mg USD 131 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Repaglinide:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

Cellular Effect
Cell Line Type Value Description References
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 (tmax less than 1 hour) with a t1/2 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
Molecular Weight

452.59

Formula

C27H36N2O4

CAS No.
Appearance

Solid

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

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
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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2095 mL 11.0475 mL 22.0951 mL
5 mM 0.4419 mL 2.2095 mL 4.4190 mL
View the Complete Stock Solution Preparation Table

* 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

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* 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.

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Repaglinide
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HY-15209
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