IDOR-1117-2520
Based on 1 Customer Validation
IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC50 = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC50 = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation.
For research use only. We do not sell to patients.
- Purity: 99.94%
- CAS No.: 2737274-49-4
- Formula: C25H32N4O3
- Molecular Weight:436.55
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Storage:Powder -20°C, 3 years , 4°C, 2 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
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CCR6 |
IDOR-1117-2520 (100 μM) has no effect at in HepaRG cells[1].
IDOR-1117-2520 antagonizes CCL20-mediated calcium influx in cells expressing recombinant human CCR6 (IC50 = 63 nM) and inhibits CCL20-induced β-arrestin recruitment to human CCR6 (IC50 = 30 nM)[1].
IDOR-1117-2520 (50 nM) inhibits the migration of B cells and T cells towards CCL20, with inhibition rates of 40% and 50% of the maximum migration, respectively[1].
IDOR-1117-2520 is found to be a substrate of P-gp/MDR1 but not of BCRP and also not of the uptake transporters OATP1B1 and OATP1B3[1].
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:Aldara® mouse model of skin inflammation[2]
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Dosage:0.02, 0.1, 0.3, 0.5 and 1 mg/mL
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Administration:p.o. via drinking water; 8 days
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Result:Reduced ear thickness in animals treated over a period of 8 days in a dose-dependent manner with a maximal observed efficacy achieved with 0.5 mg/mL.
Showed a significant reduction of infiltrating CCR6+ T cells at the end of the study (day 8).
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Animal Model:Aldara® mouse model of skin inflammation[2]
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Dosage:50 mg/kg
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Administration:Gavage; twice per day; started on day 0, 3 or 5 post Aldara® treatment until day 7.
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Result:Significantly reduced the degree of swelling, and this reduction continued until the end of the study on day 8.
Reduced the amount of CD3+ CCR6+ cells at day 8.
Chemical Information
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CAS No. 2737274-49-4
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Appearance Solid
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Molecular Weight 436.55
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Formula C25H32N4O3
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Color White to off-white
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SMILES
CC(C1=CC=C([C@@](C2=CC(C3=NOC(C(C)(O)C)=N3)=CN=C2)(O)C4(CN(C4)C)C)C=C1)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (57.27 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)
Purity & Documentation
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Data Sheet (277 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
[1]. Meyer EA, et al. Discovery of the Clinical Candidate IDOR-1117-2520: A Potent and Selective Antagonist of CCR6 for Autoimmune Diseases. J Med Chem. 2024 May 10. [Content Brief]
[2]. Kulig P, et al. Efficacy of IDOR-1117-2520, a novel, orally available CCR6 antagonist in preclinical models of skin dermatitis. Br J Pharmacol. 2025 Aug;182(15):3452-3475. [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 | 2.2907 mL | 11.4534 mL | 22.9069 mL | 57.2672 mL |
| 5 mM | 0.4581 mL | 2.2907 mL | 4.5814 mL | 11.4534 mL | |
| 10 mM | 0.2291 mL | 1.1453 mL | 2.2907 mL | 5.7267 mL | |
| 15 mM | 0.1527 mL | 0.7636 mL | 1.5271 mL | 3.8178 mL | |
| 20 mM | 0.1145 mL | 0.5727 mL | 1.1453 mL | 2.8634 mL | |
| 25 mM | 0.0916 mL | 0.4581 mL | 0.9163 mL | 2.2907 mL | |
| 30 mM | 0.0764 mL | 0.3818 mL | 0.7636 mL | 1.9089 mL | |
| 40 mM | 0.0573 mL | 0.2863 mL | 0.5727 mL | 1.4317 mL | |
| 50 mM | 0.0458 mL | 0.2291 mL | 0.4581 mL | 1.1453 mL |
IDOR-1117-2520 Related Classifications
HY-162495 Related Classifications
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