1. GPCR/G Protein
  2. GPR4
  3. GPR4 antagonist 1

GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM.

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

GPR4 antagonist 1 Chemical Structure

GPR4 antagonist 1 Chemical Structure

CAS No. : 1197879-16-5

Size Price Stock Quantity
Oil + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 638 In-stock
Solution
10 mM * 1 mL in DMSO USD 638 In-stock
Oil
5 mg USD 580 In-stock
10 mg USD 920 In-stock
25 mg USD 1850 In-stock
50 mg USD 3000 In-stock
100 mg USD 4800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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  • Biological Activity

  • Purity & Documentation

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Description

GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM.

IC50 & Target

IC50: 189 nM (GPR4)[1].

Molecular Weight

431.62

Formula

C27H37N5

CAS No.
Appearance

Oil

Color

Light yellow to yellow

SMILES

CC1=C2C(N(CC3=CC=C(/C=C/CN4CCN(C(C)C)CC4)C=C3)C(CC)=N2)=NC(C)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (289.61 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 2.3169 mL 11.5843 mL 23.1685 mL
5 mM 0.4634 mL 2.3169 mL 4.6337 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: ≥ 2.08 mg/mL (4.82 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 (4.82 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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).
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

Purity: 98.92%

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 2.3169 mL 11.5843 mL 23.1685 mL 57.9213 mL
5 mM 0.4634 mL 2.3169 mL 4.6337 mL 11.5843 mL
10 mM 0.2317 mL 1.1584 mL 2.3169 mL 5.7921 mL
15 mM 0.1545 mL 0.7723 mL 1.5446 mL 3.8614 mL
20 mM 0.1158 mL 0.5792 mL 1.1584 mL 2.8961 mL
25 mM 0.0927 mL 0.4634 mL 0.9267 mL 2.3169 mL
30 mM 0.0772 mL 0.3861 mL 0.7723 mL 1.9307 mL
40 mM 0.0579 mL 0.2896 mL 0.5792 mL 1.4480 mL
50 mM 0.0463 mL 0.2317 mL 0.4634 mL 1.1584 mL
60 mM 0.0386 mL 0.1931 mL 0.3861 mL 0.9654 mL
80 mM 0.0290 mL 0.1448 mL 0.2896 mL 0.7240 mL
100 mM 0.0232 mL 0.1158 mL 0.2317 mL 0.5792 mL
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GPR4 antagonist 1 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.

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Product Name:
GPR4 antagonist 1
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HY-101536
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