2. GPCR/G Protein Neuronal Signaling
  3. GPR55
  4. CID 16020046

CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function.

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CID 16020046 Chemical Structure

CID 16020046 Chemical Structure

CAS No. : 834903-43-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
1 mg USD 30 In-stock
5 mg USD 70 In-stock
10 mg USD 100 In-stock
25 mg USD 200 In-stock
50 mg USD 290 In-stock
100 mg USD 420 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

CID 16020046 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE CID 16020046

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

CID 16020046 is a potent and selective GPR55 antagonist and inhibits GPR55 constitutive activity with an IC50 of 0.15 μM. CID 16020046 inhibits GPR55-mediated Ca2+ signaling and GPR55-mediated ERK1/2 phosphorylation. CID 16020046 reduces wound healing in endothelial cells and is involved in the regulation of platelet function[1].

In Vitro

CID 16020046 has weak activities close for inhibition of the acetylcholinesterase (pIC50=4.4), antagonism of the m-opioid receptor (pIC50=4.6), and blockade of KCNH2, the hERG channel (pIC50=4.6) 6 in human embryonic kidney (HEK)-G protein–coupled receptor 55 (GPR55) cells[1].
CID 16020046 (2.5 μM; for ≥25 minutes) significantly inhibits the lysophosphatidylinositol (LPI; 2.5 μM) induced ERK1/2 phosphorylation. CID 16020046 alone fails to induce intracellular Ca2+ release in HEK-GPR55, HEKCB1 cells and shows no ERK1/2 phosphorylation[1].
Pretreatment with CID16020046 (0.01, 0.1, 1, 10 μM) leads to a concentration-dependent decrease in GPR55-mediated NFAT activation, NF-kB activation, and SRE induction in response to 1 μM LPI or GSK319197A in HEKGPR55 and HEK-CB1 cells[1].
CID16020046 (2.5 μM) antagonizes GPR55-mediated activation and nuclear translocation of transcription factors but has no effect on CB1-mediated CREB activation[1].
Pretreatment CID16020046 (1 μM) abolished the LPI-induced stimulation of wound healing in HMVEC-Ls[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CID 16020046 Related Antibodies

Western Blot Analysis

Cell Line: HEK-CB1 and HEK-CB2 cells[1]
Concentration: 2.5 μM
Incubation Time: For ≥25 minutes
Result: Significantly inhibited the LPI (2.5 μM) induced ERK1/2 phosphorylation.
Treatment alone showed no ERK1/2 phosphorylation and did not alter WIN55,212-2 (2.5 μM) induced ERK1/2 phosphorylation in HEK-CB1 and HEK-CB2 cells.
Molecular Weight

425.44

Formula

C25H19N3O4
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)C1=CC=C(N(C2C3=CC=CC(O)=C3)C(C4=C2C(C5=CC=C(C)C=C5)=NN4)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (235.05 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 2.3505 mL 11.7525 mL 23.5051 mL
5 mM 0.4701 mL 2.3505 mL 4.7010 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, 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.

  • Molarity Calculator

  • Dilution Calculator

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

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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: ≥ 2.5 mg/mL (5.88 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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.88 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  20% PEG300    80% Saline

    Solubility: 25 mg/mL (58.76 mM); Suspended solution; Need ultrasonic

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

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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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

Purity: 99.87%

COA (258 KB) LCMS (262 KB) Elemental Analysis Report (116 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, 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 1 mM 2.3505 mL 11.7525 mL 23.5051 mL 58.7627 mL
5 mM 0.4701 mL 2.3505 mL 4.7010 mL 11.7525 mL
10 mM 0.2351 mL 1.1753 mL 2.3505 mL 5.8763 mL
15 mM 0.1567 mL 0.7835 mL 1.5670 mL 3.9175 mL
20 mM 0.1175 mL 0.5876 mL 1.1753 mL 2.9381 mL
25 mM 0.0940 mL 0.4701 mL 0.9402 mL 2.3505 mL
30 mM 0.0784 mL 0.3918 mL 0.7835 mL 1.9588 mL
40 mM 0.0588 mL 0.2938 mL 0.5876 mL 1.4691 mL
50 mM 0.0470 mL 0.2351 mL 0.4701 mL 1.1753 mL
60 mM 0.0392 mL 0.1959 mL 0.3918 mL 0.9794 mL
80 mM 0.0294 mL 0.1469 mL 0.2938 mL 0.7345 mL
100 mM 0.0235 mL 0.1175 mL 0.2351 mL 0.5876 mL
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CID 16020046 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:

CID 16020046834903-43-4CID16020046CID-16020046GPR55G protein-coupled receptor 55Ca2+ERK1/2phosphorylationwoundhealingendothelialcellsplateletfunctionacetylcholinesterasem-opioidKCNH2 hERGHEKlysophosphatidylinositolLPIHMVECInhibitorinhibitorinhibit

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