LPA2 antagonist 1
Based on 4 publication(s) in Google Scholar
LPA2 antagonist 1 is a LPA2 antagonist with an IC50 of 17 nM.
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- Purity: 98.63%
- CAS No.: 1017606-66-4
- 화학식: C20H23Cl2N5O2S2
- 분자량:500.46
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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용액&용해도
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Publications Citing Use of MedChemExpress (MCE) LPA2 antagonist 1
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Biological Activity
IC50: 17 nM (LPA2)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| RH7777 | IC50 |
>50 μM
Compound: 35
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Antagonist activity at LPA1 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay
Antagonist activity at LPA1 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay
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[PMID: 18178086] |
| RH7777 | IC50 |
>50 μM
Compound: 35
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Antagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay
Antagonist activity at LPA3 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay
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[PMID: 18178086] |
| RH7777 | IC50 |
0.017 μM
Compound: 35
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Antagonist activity at LPA2 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay
Antagonist activity at LPA2 expressed in RH7777 cells with Gi4-protein and aequorin by calcium mobilization assay
|
[PMID: 18178086] |
LPA2 antagonist 1 inhibits the phosphorylation of Erk induced by LPA in a concentration dependent manner. LPA2 antagonist 1 inhibits HCT-116 colon cancer cell proliferation caused by LPA in a doses dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1017606-66-4
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Appearance Solid
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분자량 500.46
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화학식 C20H23Cl2N5O2S2
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Color White to off-white
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SMILES
ClC1=C(Cl)C=C(S(=O)(N2CCN(C[C@@H](NC3=NC=NC4=C3SC=C4C)C)CC2)=O)C=C1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (4)
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Journal Impact Factor
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Most Recent
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Cell Mol Life Sci
Prevention of age-associated neuronal hyperexcitability with improved learning and attention upon knockout or antagonism of LPAR2. [Abstract]2021 Feb;78(3):1029-1050. PMID: 32468095 -
Biomolecules
2022 Dec 2;12(12):1805. PMID: 36551233 -
Vet Microbiol
Lipid metabolism is a novel and practical source of potential targets for antiviral discovery against porcine parvovirus. [Abstract]2021 Oct:261:109177. PMID: 34391196 -
용액&용해도
DMSO : ≥ 100 mg/mL (199.82 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : ≥ 100 mg/mL (199.82 mM)
* "≥" means soluble, but saturation unknown.
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.
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.
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 (5.00 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 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 (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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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.
순도&문서
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Data Sheet (275 KB)
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SDS (396 KB)
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- Portuguese - PT (396 KB)
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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, 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 / DMF | 1 mM | 1.9982 mL | 9.9908 mL | 19.9816 mL | 49.9540 mL |
| 5 mM | 0.3996 mL | 1.9982 mL | 3.9963 mL | 9.9908 mL | |
| 10 mM | 0.1998 mL | 0.9991 mL | 1.9982 mL | 4.9954 mL | |
| 15 mM | 0.1332 mL | 0.6661 mL | 1.3321 mL | 3.3303 mL | |
| 20 mM | 0.0999 mL | 0.4995 mL | 0.9991 mL | 2.4977 mL | |
| 25 mM | 0.0799 mL | 0.3996 mL | 0.7993 mL | 1.9982 mL | |
| 30 mM | 0.0666 mL | 0.3330 mL | 0.6661 mL | 1.6651 mL | |
| 40 mM | 0.0500 mL | 0.2498 mL | 0.4995 mL | 1.2489 mL | |
| 50 mM | 0.0400 mL | 0.1998 mL | 0.3996 mL | 0.9991 mL | |
| 60 mM | 0.0333 mL | 0.1665 mL | 0.3330 mL | 0.8326 mL | |
| 80 mM | 0.0250 mL | 0.1249 mL | 0.2498 mL | 0.6244 mL | |
| 100 mM | 0.0200 mL | 0.0999 mL | 0.1998 mL | 0.4995 mL |
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