2. Metabolic Enzyme/Protease
  3. Glucokinase
  4. AR453588

AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity.

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

AR453588 Chemical Structure

AR453588 Chemical Structure

CAS No. : 1065609-00-8

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 528 In-stock
Solution
10 mM * 1 mL in DMSO USD 528 In-stock
Solid
1 mg USD 192 In-stock
5 mg USD 480 In-stock
10 mg USD 800 In-stock
25 mg USD 1650 In-stock
50 mg USD 2600 In-stock
100 mg USD 4000 In-stock
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Based on 1 publication(s) in Google Scholar

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AR453588 Related Antibodies

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  • Purity & Documentation

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Description

AR453588 is a potent and orally bioavailable anti-diabetic glucokinase activator, with an EC50 of 42 nM. AR453588 shows anti-hyperglycemic activity[1].

In Vivo

AR453588 (3-30 mg/kg; p.o) lowers post-prandial glucose in normal C57BL/6J mice[1].
AR453588 (3-30 mg/kg; p.o.; once-daily for 14 days) shows anti-hyperglycemic activity in a dose-ranging 14 day ob/ob mouse[1].
AR453588 (10 mg/kg; p.o.) treatment shows that the Tmax, AUCinf, Vss, Cmax and F are 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively[1].
AR453588 (1 mg/kg; i.v.) treatment shows that the CL, AUCinf, Vss, and t1/2 are 21.6 mL/min/kg, 0.77 h μg /mL, 0.746 L/kg and 1.28 hours, respectively[1].

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

Animal Model: Male diabetic ob/ob mice[1]
Dosage: 3, 10, 30 mg/kg
Administration: Orally once-daily for 14 days
Result: Lowered the fasted blood glucose from the control animals on day 14 as well as the AUC of the OGTT (oral glucose tolerance tests).
Animal Model: Male CD-1 mice[1]
Dosage: 10 mg/kg
Administration: p.o. (Pharmacokinetic Analysis)
Result: The Tmax, AUCinf, Vss, Cmax and F were 1.0 mL/min/kg, 4.65 h μg /mL, 1.67 μg /mL and 60.3%, respectively.
Molecular Weight

519.64

Formula

C25H25N7O2S2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(N1CCC(C2=NSC(NC3=NC=C(SC4=NC=CC=C4)C=C3OC5=CC=CN=C5C)=N2)CC1)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (192.44 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9244 mL 9.6220 mL 19.2441 mL
5 mM 0.3849 mL 1.9244 mL 3.8488 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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 (4.81 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 (4.81 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9244 mL 9.6220 mL 19.2441 mL 48.1102 mL
5 mM 0.3849 mL 1.9244 mL 3.8488 mL 9.6220 mL
10 mM 0.1924 mL 0.9622 mL 1.9244 mL 4.8110 mL
15 mM 0.1283 mL 0.6415 mL 1.2829 mL 3.2073 mL
20 mM 0.0962 mL 0.4811 mL 0.9622 mL 2.4055 mL
25 mM 0.0770 mL 0.3849 mL 0.7698 mL 1.9244 mL
30 mM 0.0641 mL 0.3207 mL 0.6415 mL 1.6037 mL
40 mM 0.0481 mL 0.2406 mL 0.4811 mL 1.2028 mL
50 mM 0.0385 mL 0.1924 mL 0.3849 mL 0.9622 mL
60 mM 0.0321 mL 0.1604 mL 0.3207 mL 0.8018 mL
80 mM 0.0241 mL 0.1203 mL 0.2406 mL 0.6014 mL
100 mM 0.0192 mL 0.0962 mL 0.1924 mL 0.4811 mL
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AR453588 Related Classifications

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.

Keywords:

AR4535881065609-00-8AR 453588AR-453588GlucokinaseHexokinase IVHexokinase Dorallybioavailableanti-diabeticanti-hyperglycemicob/obmicetype2diabetesInhibitorinhibitorinhibit

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