1. GPCR/G Protein
  2. EBI2/GPR183
  3. GPR183 antagonist-3

GPR183 antagonist-3 (compound 33) is an oral active GPR183 antagonist with the IC50 of 8.7 μM. GPR183 antagonist-3 displays strong in vitro antimigration and anti-inflammatory activity in monocytes, and improves the pathological symptoms of DSS-induced experimental colitis.

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GPR183 antagonist-3 Chemical Structure

GPR183 antagonist-3 Chemical Structure

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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10 mM * 1 mL in DMSO In-stock
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Based on 1 publication(s) in Google Scholar

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Description

GPR183 antagonist-3 (compound 33) is an oral active GPR183 antagonist with the IC50 of 8.7 μM. GPR183 antagonist-3 displays strong in vitro antimigration and anti-inflammatory activity in monocytes, and improves the pathological symptoms of DSS-induced experimental colitis[1].

Molecular Weight

471.37

Formula

C21H19BrN4O2S

Appearance

Solid

Color

Off-white to light yellow

SMILES

BrC1=CC=C(C=C1)/C=C/C(N2CCN(CC2)C(C3=CC=C4N=C(SC4=C3)N)=O)=O

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 : 100 mg/mL (212.15 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 2.1215 mL 10.6074 mL 21.2148 mL
5 mM 0.4243 mL 2.1215 mL 4.2430 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
×
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    90% Corn Oil

    Solubility: ≥ 5 mg/mL (10.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). 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 (50.0 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).

*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 2.1215 mL 10.6074 mL 21.2148 mL 53.0369 mL
5 mM 0.4243 mL 2.1215 mL 4.2430 mL 10.6074 mL
10 mM 0.2121 mL 1.0607 mL 2.1215 mL 5.3037 mL
15 mM 0.1414 mL 0.7072 mL 1.4143 mL 3.5358 mL
20 mM 0.1061 mL 0.5304 mL 1.0607 mL 2.6518 mL
25 mM 0.0849 mL 0.4243 mL 0.8486 mL 2.1215 mL
30 mM 0.0707 mL 0.3536 mL 0.7072 mL 1.7679 mL
40 mM 0.0530 mL 0.2652 mL 0.5304 mL 1.3259 mL
50 mM 0.0424 mL 0.2121 mL 0.4243 mL 1.0607 mL
60 mM 0.0354 mL 0.1768 mL 0.3536 mL 0.8839 mL
80 mM 0.0265 mL 0.1326 mL 0.2652 mL 0.6630 mL
100 mM 0.0212 mL 0.1061 mL 0.2121 mL 0.5304 mL
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GPR183 antagonist-3 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:
GPR183 antagonist-3
Cat. No.:
HY-157939
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