LPA5 antagonist 1
Based on 1 Customer Validation
LPA5 antagonist 1 (Compound 66) is a potent and selective lysophosphatidic acid receptor 5 (LPA5) antagonist (IC50=32 nM). LPA5 antagonist 1 shows high blood-brain-barrier permeability and anti-nociceptive activity. LPA5 antagonist 1 can be used in inflammatory and neuropathic pain research. LPA5 antagonist 1 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.
- Purity: 98.91%
- CAS No.: 2839471-45-1
- Formula: C28H26N2O4S
- Molecular Weight:486.58
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
IC50: 32 nM (LPA5)[1]
LPA5 antagonist 1 (intraperitoneal injection; 5.6, 10, and 17.8 mg/kg; once) treatment reduces mechanical allodynia in inflammatory pain model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:CFA-induced inflammatory pain model in Sprague-Dawley rats[1]
-
Dosage:5.6, 10, and 17.8 mg/kg
-
Administration:Intraperitoneal injection; 5.6, 10, and 17.8 mg/kg; once
-
Result:Reduced mechanical allodynia in a dose-dependent manner.
-
Animal Model:Male Sprague-Dawley rats[1]
-
Dosage:17.8 mg/kg
-
Administration:Intraperitoneal injection; 17.8 mg/kg; once
-
Result:Showed brain concentrations of 652 ng/mL, after treatment 30 minutes.
Chemical Information
-
CAS No. 2839471-45-1
-
Appearance Solid
-
Molecular Weight 486.58
-
Formula C28H26N2O4S
-
Color Off-white to light yellow
-
SMILES
O=C1N(C2=CC=C3C(C(C)=CS3)=C2)C=C(C(N4CCC(C#C)CC4)=O)C5=C1C=C(OC)C(OC)=C5
-
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
DMSO : 100 mg/mL (205.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
-
Data Sheet (279 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Handling Instructions (2659 KB)
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 | 2.0552 mL | 10.2758 mL | 20.5516 mL | 51.3790 mL |
| 5 mM | 0.4110 mL | 2.0552 mL | 4.1103 mL | 10.2758 mL | |
| 10 mM | 0.2055 mL | 1.0276 mL | 2.0552 mL | 5.1379 mL | |
| 15 mM | 0.1370 mL | 0.6851 mL | 1.3701 mL | 3.4253 mL | |
| 20 mM | 0.1028 mL | 0.5138 mL | 1.0276 mL | 2.5690 mL | |
| 25 mM | 0.0822 mL | 0.4110 mL | 0.8221 mL | 2.0552 mL | |
| 30 mM | 0.0685 mL | 0.3425 mL | 0.6851 mL | 1.7126 mL | |
| 40 mM | 0.0514 mL | 0.2569 mL | 0.5138 mL | 1.2845 mL | |
| 50 mM | 0.0411 mL | 0.2055 mL | 0.4110 mL | 1.0276 mL | |
| 60 mM | 0.0343 mL | 0.1713 mL | 0.3425 mL | 0.8563 mL | |
| 80 mM | 0.0257 mL | 0.1284 mL | 0.2569 mL | 0.6422 mL | |
| 100 mM | 0.0206 mL | 0.1028 mL | 0.2055 mL | 0.5138 mL |