2. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  3. GPR119 TRP Channel
  4. AS1269574

AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes.

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AS1269574 Chemical Structure

AS1269574 Chemical Structure

CAS No. : 330981-72-1

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Based on 1 publication(s) in Google Scholar

AS1269574 Related Antibodies

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TRPC TRPM TRPV TRPA TRPML

  • Biological Activity

  • Purity & Documentation

  • References

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Description

AS1269574 is a potent, orally available GPR119 agonist, with an EC50 of 2.5 μM in HEK293 cells expressing human GPR119. AS1269574 activates TRPA1 cation channels to stimulate glucagon-like peptide-1 (GLP-1) secretion. AS1269574 specifically induces glucose-dependent insulin secretion from pancreatic β-cells only under high-glucose conditions. AS1269574 has the potential for the research of type 2 diabetes[1][2].

IC50 & Target[1][2]

GPR119

 

TRPA1

 

Cellular Effect
Cell Line Type Value Description References
HEK293 EC50
2.5 μM
Compound: 9a
Agonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assay
Agonist activity at human GPR119 expressed in HEK293 cells co-transfected with pCRE-Luc assessed as induction in cAMP level after 6 hrs by luciferase reporter gene assay
[PMID: 22365911]
In Vivo

AS1269574 sgnificantly reduced the blood glucose AUC after 2 h (AUC0-2h) of administration[1].

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

Animal Model: Eight-week-old ICR mice[1]
Dosage: 100 mg/kg
Administration: P.o.
Result: Sgnificantly reduced the blood glucose AUC after 2 h (AUC0-2h) of administration. Similarly, plasma insulin AUC0-2h was significantly higher in the mice.
Molecular Weight

308.17

Formula

C13H14BrN3O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OCCNC1=NC(C2=CC=C(Br)C=C2)=NC(C)=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (811.24 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 3.2450 mL 16.2248 mL 32.4496 mL
5 mM 0.6490 mL 3.2450 mL 6.4899 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 (protect from light). 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
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Volume
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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: ≥ 2.08 mg/mL (6.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (6.75 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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 (protect from light). 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 3.2450 mL 16.2248 mL 32.4496 mL 81.1241 mL
5 mM 0.6490 mL 3.2450 mL 6.4899 mL 16.2248 mL
10 mM 0.3245 mL 1.6225 mL 3.2450 mL 8.1124 mL
15 mM 0.2163 mL 1.0817 mL 2.1633 mL 5.4083 mL
20 mM 0.1622 mL 0.8112 mL 1.6225 mL 4.0562 mL
25 mM 0.1298 mL 0.6490 mL 1.2980 mL 3.2450 mL
30 mM 0.1082 mL 0.5408 mL 1.0817 mL 2.7041 mL
40 mM 0.0811 mL 0.4056 mL 0.8112 mL 2.0281 mL
50 mM 0.0649 mL 0.3245 mL 0.6490 mL 1.6225 mL
60 mM 0.0541 mL 0.2704 mL 0.5408 mL 1.3521 mL
80 mM 0.0406 mL 0.2028 mL 0.4056 mL 1.0141 mL
100 mM 0.0324 mL 0.1622 mL 0.3245 mL 0.8112 mL
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AS1269574 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:

AS1269574330981-72-1AS 1269574AS-1269574GPR119TRP ChannelG Protein-Coupled Receptor 119Transient receptor potential channelsglucoseinsulinsecretioncationchannelstype2diabetesInhibitorinhibitorinhibit

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