GRI977143
Based on 1 Customer Validation
GRI977143 is a specific LPA2 receptor agonist, with an EC50 of 3.3 μM .
For research use only. We do not sell to patients.
- Purity: 99.29%
- CAS No.: 325850-81-5
- Formula: C22H17NO4S
- Molecular Weight:391.44
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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LPA2 Receptor 3.3 μM (EC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MEF | EC50 |
3.3 μM
Compound: 3, GRI-977143
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Agonist activity at human LPA2 expressed in LPA1xLPA2 double knockout mouse MEF cells by Fura-2AM dye based Ca2+ mobilization assay
Agonist activity at human LPA2 expressed in LPA1xLPA2 double knockout mouse MEF cells by Fura-2AM dye based Ca2+ mobilization assay
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[PMID: 25100502] |
| MEF | IC50 |
6.6 μM
Compound: 3, GRI-977143
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Antagonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells assessed as reduction in LP18:1-induced calcium mobilization by Fura-2AM dye based Ca2+ mobilization assay
Antagonist activity at human LPA3 expressed in LPA1xLPA2 double knockout mouse MEF cells assessed as reduction in LP18:1-induced calcium mobilization by Fura-2AM dye based Ca2+ mobilization assay
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[PMID: 25100502] |
GRI977143 (10 μM, 24-72 h) is effective in reducing activation of caspases 3, 7, 8, and 9 and inhibits poly(ADP-ribose)polymerase 1 cleavage and DNA fragmentation in different extrinsic and intrinsic models of apoptosis[1].
GRI977143 is an effective stimulator of extracellular signal-regulated kinase 1/2 activation and promotes the assembly of a macromolecular signaling complex consisting of LPA2, Na+-H+ exchange regulatory factor 2, and thyroid receptor interacting protein 6[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Vector- and LPA2-transduced MEF cells (2 × 104)[1].
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Concentration:10 μM.
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Incubation Time:24-72 h.
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Result:Did not cause a significant increase in vector cell proliferation except at 72 h (p < 0.05).
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Cell Line:Doxorubicin-induced apoptotic signaling in vector-transduced or LPA2-transduced MEF.
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Concentration:10 μM.
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Incubation Time:24 h.
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Result:Reduced caspase 3 and 7 activation on LPA2-transduced MEF cells by 51 ± 3% and was approximately as potent as 3 μM LPA or OTP.
Protected against doxorubicin-induced apoptosis by inhibiting caspase 3, 7, 8, and 9 and reducing DNA fragmentation.
Chemical Information
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CAS No. 325850-81-5
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Appearance Solid
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Molecular Weight 391.44
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Formula C22H17NO4S
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Color White to off-white
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SMILES
O=C(O)C1=CC=CC=C1SCCCN(C(C2=CC=CC3=CC=CC4=C23)=O)C4=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 50 mg/mL (127.73 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 (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.
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.
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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
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Data Sheet (277 KB)
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SDS (597 KB)
- English - EN (597 KB)
- Français - FR (597 KB)
- Deutsch - DE (597 KB)
- Norwegian - NO (597 KB)
- Español - ES (597 KB)
- Swedish - SV (597 KB)
- Italian - IT (597 KB)
- Korean - KR (597 KB)
- Portuguese - PT (597 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, 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 | 2.5547 mL | 12.7733 mL | 25.5467 mL | 63.8667 mL |
| 5 mM | 0.5109 mL | 2.5547 mL | 5.1093 mL | 12.7733 mL | |
| 10 mM | 0.2555 mL | 1.2773 mL | 2.5547 mL | 6.3867 mL | |
| 15 mM | 0.1703 mL | 0.8516 mL | 1.7031 mL | 4.2578 mL | |
| 20 mM | 0.1277 mL | 0.6387 mL | 1.2773 mL | 3.1933 mL | |
| 25 mM | 0.1022 mL | 0.5109 mL | 1.0219 mL | 2.5547 mL | |
| 30 mM | 0.0852 mL | 0.4258 mL | 0.8516 mL | 2.1289 mL | |
| 40 mM | 0.0639 mL | 0.3193 mL | 0.6387 mL | 1.5967 mL | |
| 50 mM | 0.0511 mL | 0.2555 mL | 0.5109 mL | 1.2773 mL | |
| 60 mM | 0.0426 mL | 0.2129 mL | 0.4258 mL | 1.0644 mL | |
| 80 mM | 0.0319 mL | 0.1597 mL | 0.3193 mL | 0.7983 mL | |
| 100 mM | 0.0255 mL | 0.1277 mL | 0.2555 mL | 0.6387 mL |
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