GPR34 receptor antagonist 3
Based on 1 Customer Validation
GPR34 receptor antagonist 3 (Compound 5e) is a class of GRP34 antagonists, IC50 is 0.680 μM. GPR34 receptor antagonist 3 inhibited ERK1/2 phosphorylation induced by lysophosphatidylserine in a dose-dependent way without obvious cytotoxicity. GPR34 receptor antagonist 3 shows antisensory activity in mouse neuropathic pain model .
For research use only. We do not sell to patients.
- Purity: 99.88%
- CAS No.: 3049949-94-9
- Formula: C30H26ClNO5
- Molecular Weight:515.98
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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
IC50:0.680 μM G protein receptor (GPR34) [1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BEAS-2B | IC50 |
>30 μM
Compound: 5e
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Cytotoxicity against human BEAS-2B cells incubated for 72 hrs by MTT assay
Cytotoxicity against human BEAS-2B cells incubated for 72 hrs by MTT assay
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[PMID: 37949379] |
| COS-7 | IC50 |
>30 μM
Compound: 5e
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Cytotoxicity against African green monkey COS-7 cells incubated for 72 hrs by MTT assay
Cytotoxicity against African green monkey COS-7 cells incubated for 72 hrs by MTT assay
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[PMID: 37949379] |
| HEK293 | IC50 |
>30 μM
Compound: 5e
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Cytotoxicity against HEK293 cells incubated for 72 hrs by MTT assay
Cytotoxicity against HEK293 cells incubated for 72 hrs by MTT assay
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[PMID: 37949379] |
| HUVEC | IC50 |
>30 μM
Compound: 5e
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Cytotoxicity against human HUVEC cells incubated for 72 hrs by MTT assay
Cytotoxicity against human HUVEC cells incubated for 72 hrs by MTT assay
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[PMID: 37949379] |
| LX-2 | IC50 |
>30 μM
Compound: 5e
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Cytotoxicity against human LX2 cells incubated for 72 hrs by MTT assay
Cytotoxicity against human LX2 cells incubated for 72 hrs by MTT assay
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[PMID: 37949379] |
GPR34 receptor antagonist 3 (30 μM, 72 h) in HEK293T、COS-7、BEAS-2B、Muller、LX-2 and HUVEC cells do not show obvious cytotoxicity against these cell lines with IC50 > 30 μM[1].
GPR34 receptor antagonist 3 (3, 10 and 30 μM, 72 h) dose-dependently inhibited the phosphorylation of extracellular signal-regulated kinase1/2 (ERK1/2) induced by LysoPS in CHO cells expressing GPR34[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CHO
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Concentration:3,10 and 30 μM
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Incubation Time:72 h
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Result:Dose-dependently inhibited the phosphorylation of extracellular signal-regulated kinase1/2 (ERK1/2) induced by LysoPS in CHO cells expressing GPR34.
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Cell Line:HEK293T, COS-7, BEAS-2B, Muller, LX-2 and HUVEC
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Concentration:30 μM
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Incubation Time:72 h
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Result:Did not show obvious cytotoxicity against these cell lines with IC50 > 30 μM.
GPR34 receptor antagonist 3 (10 or 20 mg/kg, Intraperitoneal injection,twice a day) can significantly reduce mechanical pain in a mouse neuropathic pain model [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Neuropathic pain mice model[1]
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Dosage:10 or 20 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Reduced mechanical pain in a mouse neuropathic pain model
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Animal Model:Oxicity mice model[1]
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Dosage:200 or 100 mg/kg
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Administration:Intraperitoneal injection (i.p.)
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Result:Indicated 100 mg/kg was a safe dosage.
Chemical Information
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CAS No. 3049949-94-9
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Appearance Solid
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Molecular Weight 515.98
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Formula C30H26ClNO5
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Color White to off-white
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SMILES
O=C(COC1=CC=C(C2=CC(Cl)=CC=C2)C=C1)N[C@H](C(O)=O)CC(C=C3)=CC=C3OCC4=CC=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 85 mg/mL (164.74 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: 5 mg/mL (9.69 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Purity & Documentation
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Data Sheet (272 KB)
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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)
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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. 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 | 1.9381 mL | 9.6903 mL | 19.3806 mL | 48.4515 mL |
| 5 mM | 0.3876 mL | 1.9381 mL | 3.8761 mL | 9.6903 mL | |
| 10 mM | 0.1938 mL | 0.9690 mL | 1.9381 mL | 4.8451 mL | |
| 15 mM | 0.1292 mL | 0.6460 mL | 1.2920 mL | 3.2301 mL | |
| 20 mM | 0.0969 mL | 0.4845 mL | 0.9690 mL | 2.4226 mL | |
| 25 mM | 0.0775 mL | 0.3876 mL | 0.7752 mL | 1.9381 mL | |
| 30 mM | 0.0646 mL | 0.3230 mL | 0.6460 mL | 1.6150 mL | |
| 40 mM | 0.0485 mL | 0.2423 mL | 0.4845 mL | 1.2113 mL | |
| 50 mM | 0.0388 mL | 0.1938 mL | 0.3876 mL | 0.9690 mL | |
| 60 mM | 0.0323 mL | 0.1615 mL | 0.3230 mL | 0.8075 mL | |
| 80 mM | 0.0242 mL | 0.1211 mL | 0.2423 mL | 0.6056 mL | |
| 100 mM | 0.0194 mL | 0.0969 mL | 0.1938 mL | 0.4845 mL |
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