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  4. GPR34 receptor antagonist 3

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 .

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GPR34 receptor antagonist 3 Chemical Structure

GPR34 receptor antagonist 3 Chemical Structure

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1 mg USD 156 In-stock
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Based on 1 publication(s) in Google Scholar

GPR34 receptor antagonist 3 Related Antibodies

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Description

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 [1].

IC50 & Target

IC50:0.680 μM G protein receptor (GPR34) [1]
In Vitro

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.

GPR34 receptor antagonist 3 Related Antibodies

Western Blot Analysis[1]

Cell Line: CHO
Concentration: 3,10 and 30 μM
Incubation Time: 72 h
Result: Dose-dependently inhibited the phosphorylation of extracellular signal-regulated kinase1/2 (ERK1/2) induced by LysoPS in CHO cells expressing GPR34.

Cell Viability Assay[1]

Cell Line: HEK293T, COS-7, BEAS-2B, Muller, LX-2 and HUVEC
Concentration: 30 μM
Incubation Time: 72 h
Result: Did not show obvious cytotoxicity against these cell lines with IC50 > 30 μM.
In Vivo

GPR34 receptor antagonist 3 (200 mg/kg, Intraperitoneal injection, twice a day) observes the death of C57BL/6J mice in the acute toxicity experiment, GPR34 receptor antagonist 3 (100 mg/kg, Intraperitoneal injection, twice a day) mice has no damage during repeated toxicity experiment, and the dose was safe [1].
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.

Animal Model: Neuropathic pain mice model[1]
Dosage: 10 or 20 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Reduced mechanical pain in a mouse neuropathic pain model
Animal Model: Oxicity mice model[1]
Dosage: 200 or 100 mg/kg
Administration: Intraperitoneal injection (i.p.)
Result: Indicated 100 mg/kg was a safe dosage.
Molecular Weight

515.98

Formula

C30H26ClNO5
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9381 mL 9.6903 mL 19.3806 mL
5 mM 0.3876 mL 1.9381 mL 3.8761 mL
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.
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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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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:
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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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
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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GPR34 receptor antagonist 3 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GPR34 receptor antagonist 3OthersGRP34AntagonistCHOMouseERK1/2Animal model of neuropathic painInhibitorinhibitorinhibit

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