2. GPCR/G Protein
  3. GPR35
  4. CID 2745687

CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM.

For research use only. We do not sell to patients.

CID 2745687 Chemical Structure

CID 2745687 Chemical Structure

CAS No. : 264233-05-8

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Customer Review

Based on 1 publication(s) in Google Scholar

CID 2745687 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

  • References

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Description

CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM[1].

Cellular Effect
Cell Line Type Value Description References
CHO IC50
0.574 μM
Compound: 13, CID 2745687
Antagonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay
Antagonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay
[PMID: 23888932]
HT-29 IC50
10.4 μM
Compound: 13, CID 2745687
Antagonist activity at human GPR35 expressed in human HT29 cells after 1 hr by DMR assay
Antagonist activity at human GPR35 expressed in human HT29 cells after 1 hr by DMR assay
[PMID: 23888932]
U2OS IC50
0.2 μM
Compound: 13, CID 2745687
Antagonist activity at human Gal4-VP16 fused GPR35 expressed in human U2OS cells assessed as beta arrestin translocation by reporter gene assay
Antagonist activity at human Gal4-VP16 fused GPR35 expressed in human U2OS cells assessed as beta arrestin translocation by reporter gene assay
[PMID: 23888932]
In Vitro

For ERK1/2 phosphorylation with 1 μM Pamoic acid as the agonist, the CID 2745687 (CID2745687) Ki is 18 nM[1]. CID 2745687 (CID-2745687) is a potent antagonist in β-arrestin-2 interaction assays only at human GPR35[2].
Using the BRET-based GPR35-β-arrestin-2 interaction assay and an EC80 concentration of Zaprinast (20 μM) as agonist, CID 2745687 behaved as a moderately potent, concentration-dependent antagonist at human GPR35 with pIC50=6.70±0.09[2].
CID 2745687 (pIC50=6.27±0.08) fully reverses the agonist action of Cromolyn disodium [2].

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

CID 2745687 Related Antibodies
In Vivo

CID 2745687 (CID2745687; 1 mg/kg; administrated orally every day for the last 4 weeks), a specific GPR35 antagonist, reverses Lodoxamide-mediated anti-fibrotic effects[3].

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

Animal Model: Six-week-old male C57BL/6 mice[3]
Dosage: 1 mg/kg
Administration: Oral administration, every day for 4 weeks
Result: Inhibited Lodoxamide-mediated protective effects.
Molecular Weight

395.43

Formula

C17H19F2N5O2S
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=C(/C=N/NC(NC(C)(C)C)=S)N(C2=CC=C(C=C2F)F)N=C1)OC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (316.11 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 2.5289 mL 12.6445 mL 25.2889 mL
5 mM 0.5058 mL 2.5289 mL 5.0578 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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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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V2

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    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (5.26 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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 +
% 
+
%
Tween-80 +
%
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 2.5289 mL 12.6445 mL 25.2889 mL 63.2223 mL
5 mM 0.5058 mL 2.5289 mL 5.0578 mL 12.6445 mL
10 mM 0.2529 mL 1.2644 mL 2.5289 mL 6.3222 mL
15 mM 0.1686 mL 0.8430 mL 1.6859 mL 4.2148 mL
20 mM 0.1264 mL 0.6322 mL 1.2644 mL 3.1611 mL
25 mM 0.1012 mL 0.5058 mL 1.0116 mL 2.5289 mL
30 mM 0.0843 mL 0.4215 mL 0.8430 mL 2.1074 mL
40 mM 0.0632 mL 0.3161 mL 0.6322 mL 1.5806 mL
50 mM 0.0506 mL 0.2529 mL 0.5058 mL 1.2644 mL
60 mM 0.0421 mL 0.2107 mL 0.4215 mL 1.0537 mL
80 mM 0.0316 mL 0.1581 mL 0.3161 mL 0.7903 mL
100 mM 0.0253 mL 0.1264 mL 0.2529 mL 0.6322 mL
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CID 2745687 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 2745687264233-05-8CID2745687CID-2745687GPR35G Protein-Coupled Receptor 35GPR35 antagonistArrestinG Protein-coupled ReceptorsGPCRInhibitorinhibitorinhibit

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