GLPG1205 [1445847-37-9]
Cat# HY-135303-10mg
Size : 10mg
Brand : MedChemExpress
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis. GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
For research use only. We do not sell to patients.
GLPG1205 Chemical Structure
CAS No. : 1445847-37-9
This product is a controlled substance and not for sale in your territory.
Based on 1 publication(s) in Google Scholar
Description |
GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis[1][2]. GLPG1205 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups. |
||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|
In Vitro |
GLPG1205 (0.5?μM) completely inhibits the ZQ16-induced [Ca2+]i response in neutrophils[1]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
In Vivo |
GLPG1250 (orally adminstation; 30mg/kg; twice daily) for 2 weeks, starts from 7 days post-challenge,greatly reduces the Ashcroft score, in idiopathic pulmonary fibrosis model[3].? GLPG1250 (orally adminstation; 30mg/kg; once daily) starts from 18 weeks post irradition, significantly reduces college deposition in the mouse lung. Additionlly, GLPG1250 inhibits the increase in MnSOD in lung bronchial epithelial cells and parenchymal macrophages, in the irradiation model[3].? GLPG1205 dose dependently decreases disease activity, histological activity, neutrophil influx and colonic MPO content,in a mouse IBD model[4]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. |
||||||||||||
Clinical Trial |
|
||||||||||||
Molecular Weight |
378.42 |
||||||||||||
Formula |
C22H22N2O4 |
||||||||||||
CAS No. |
1445847-37-9 |
||||||||||||
Appearance |
Solid |
||||||||||||
Color |
Light yellow to yellow |
||||||||||||
SMILES |
O=C1N=C(OC[C@H]2OCCOC2)C=C3N1CCC4=C3C=CC(C#CC5CC5)=C4 |
||||||||||||
Shipping | Room temperature in continental US; may vary elsewhere. |
||||||||||||
Storage |
|
||||||||||||
Solvent & Solubility |
In Vitro:
DMSO : 250 mg/mL (660.64 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Preparing
Stock Solutions
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.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol) Concentration (start) × Volume (start) = Concentration (final) × Volume (final) This equation is commonly abbreviated as: C1V1 = C2V2 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:
For the following dissolution methods, please prepare the working solution directly.
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage mg/kgAnimal weight Dosing volume 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
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: 99.64% |
||||||||||||
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
---|
DMSO | 1 mM | 2.6426 mL | 13.2128 mL | 26.4257 mL | 66.0642 mL |
5 mM | 0.5285 mL | 2.6426 mL | 5.2851 mL | 13.2128 mL | |
10 mM | 0.2643 mL | 1.3213 mL | 2.6426 mL | 6.6064 mL | |
15 mM | 0.1762 mL | 0.8809 mL | 1.7617 mL | 4.4043 mL | |
20 mM | 0.1321 mL | 0.6606 mL | 1.3213 mL | 3.3032 mL | |
25 mM | 0.1057 mL | 0.5285 mL | 1.0570 mL | 2.6426 mL | |
30 mM | 0.0881 mL | 0.4404 mL | 0.8809 mL | 2.2021 mL | |
40 mM | 0.0661 mL | 0.3303 mL | 0.6606 mL | 1.6516 mL | |
50 mM | 0.0529 mL | 0.2643 mL | 0.5285 mL | 1.3213 mL | |
60 mM | 0.0440 mL | 0.2202 mL | 0.4404 mL | 1.1011 mL | |
80 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8258 mL | |
100 mM | 0.0264 mL | 0.1321 mL | 0.2643 mL | 0.6606 mL |
GLPG1205 Related Classifications
- GPCR/G Protein
- GPR84