CID 2745687
Based on 1 Customer Validation
CID 2745687 acts as a specific, reversible and competitive GPR35 antagonist with a Ki of 12.8 nM.
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- Pureté: 99.35%
- CAS No.: 264233-05-8
- Formule: C17H19F2N5O2S
- Masse moléculaire:395.43
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.574 μM
Compound: 13, CID 2745687
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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
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[PMID: 23888932] |
| HT-29 | IC50 |
10.4 μM
Compound: 13, CID 2745687
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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
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[PMID: 23888932] |
| U2OS | IC50 |
0.2 μM
Compound: 13, CID 2745687
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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
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[PMID: 23888932] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Six-week-old male C57BL/6 mice[3]
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Dosage:1 mg/kg
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Administration:Oral administration, every day for 4 weeks
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Result:Inhibited Lodoxamide-mediated protective effects.
Chemical Information
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CAS No. 264233-05-8
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Appearance Solid
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Masse moléculaire 395.43
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Formule C17H19F2N5O2S
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Color Off-white to light yellow
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SMILES
O=C(C1=C(/C=N/NC(NC(C)(C)C)=S)N(C2=CC=C(C=C2F)F)N=C1)OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
DMSO : 125 mg/mL (316.11 mM; ultrasonic and warming and heat to 60°C; 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)
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 5 mg/mL (12.64 mM); Suspended solution; Need ultrasonic
Pureté et documentation
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Fiche technique (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Pingwei Zhao, et al. Targeting of the orphan receptor GPR35 by pamoic acid: a potent activator of extracellular signal-regulated kinase and β-arrestin2 with antinociceptive activity. Mol Pharmacol. 2010 Oct;78(4):560-8. [Content Brief]
[2]. Laura Jenkins, et al. Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. J Pharmacol Exp Ther. 2012 Dec;343(3):683-95. [Content Brief]
[3]. Mi-Jeong Kim, et al. Lodoxamide Attenuates Hepatic Fibrosis in Mice: Involvement of GPR35. Biomol Ther (Seoul). 2019 Jun 13;28(1):92-97. [Content Brief]
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 |
CID 2745687 Related Classifications
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