2. GPCR/G Protein
  3. GCGR
  4. GCGR antagonist 2

GCGR antagonist 2, a Furan-2-carbohydrazide, is an orally active glucagon receptor antagonist. GCGR antagonist 2 binds to hGluR with an Kd value of 2.3 nM, and inhibits rat receptor with an IC50 value of 0.43 nM. GCGR antagonist 2 inhibits glucagon-stimulated glycogenolysis.

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GCGR antagonist 2 Chemical Structure

GCGR antagonist 2 Chemical Structure

CAS No. : 280134-25-0

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Based on 1 publication(s) in Google Scholar

GCGR antagonist 2 Related Antibodies

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  • Purity & Documentation

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Description

GCGR antagonist 2, a Furan-2-carbohydrazide, is an orally active glucagon receptor antagonist. GCGR antagonist 2 binds to hGluR with an Kd value of 2.3 nM, and inhibits rat receptor with an IC50 value of 0.43 nM. GCGR antagonist 2 inhibits glucagon-stimulated glycogenolysis[1][2].

In Vitro

GCGR antagonist 2 (compound 74) (25 nM, 250 nM, and 2500 nM; 70 min) inhibits 5 nM glucagon-induced glycogenolysis in primary rat hepatocytes, with an IC50 value of 160 nM[1].
GCGR antagonist 2 (25 nM, 250 nM, and 2500 nM; 60 min) inhibits glucagon-stimulated cAMP level with the recombinant human glucagon receptor in BHK cells[1].
GCGR antagonist 2 (1 nM, 10 nM, and 100 nM; 60 min) inhibits glucagon-stimulated cAMP level with isolated rat liver glucagon receptor in BHK cells[1].

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

GCGR antagonist 2 Related Antibodies
In Vivo

GCGR antagonist 2 (0.5 mg/kg for IV, or 2 mg/kg for PO; single dose) shows mean half-lives of 1.11 h and 1.40 h, respectively[1].
GCGR antagonist 2 (0 mg/kg, 3 mg/kg, and 10 mg/kg; p.o.) at least partly, inhibits the action of the endogenous glucagon responsible for maintenance of euglycemia in glucagon-challenged Sprague-Dawley rats[1].

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

450.53

Formula

C28H26N4O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=CC(C(N/N=C/C2=CC=CC3=C2C=CN3CC4=C(C)C(C)=CC(C)=C4C)=O)=CC=C1O
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 (221.96 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 2.2196 mL 11.0980 mL 22.1961 mL
5 mM 0.4439 mL 2.2196 mL 4.4392 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
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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

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Volume (start)

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C2

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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 (5.55 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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% Corn Oil

    Solubility: 2.5 mg/mL (5.55 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL. 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

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 2.2196 mL 11.0980 mL 22.1961 mL 55.4902 mL
5 mM 0.4439 mL 2.2196 mL 4.4392 mL 11.0980 mL
10 mM 0.2220 mL 1.1098 mL 2.2196 mL 5.5490 mL
15 mM 0.1480 mL 0.7399 mL 1.4797 mL 3.6993 mL
20 mM 0.1110 mL 0.5549 mL 1.1098 mL 2.7745 mL
25 mM 0.0888 mL 0.4439 mL 0.8878 mL 2.2196 mL
30 mM 0.0740 mL 0.3699 mL 0.7399 mL 1.8497 mL
40 mM 0.0555 mL 0.2775 mL 0.5549 mL 1.3873 mL
50 mM 0.0444 mL 0.2220 mL 0.4439 mL 1.1098 mL
60 mM 0.0370 mL 0.1850 mL 0.3699 mL 0.9248 mL
80 mM 0.0277 mL 0.1387 mL 0.2775 mL 0.6936 mL
100 mM 0.0222 mL 0.1110 mL 0.2220 mL 0.5549 mL
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GCGR antagonist 2 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:

GCGR antagonist 2280134-25-0GCGR antagonist2GCGR antagonist-2GCGRGlucagon ReceptorInhibitorinhibitorinhibit

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