2. GPCR/G Protein Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel
  3. CCR Calcium Channel Arrestin P-glycoprotein
  4. IDOR-1117-2520

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.

IDOR-1117-2520

IDOR-1117-2520 Chemical Structure

CAS No. : 2737274-49-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

Other Forms of IDOR-1117-2520:

IDOR-1117-2520 Related Antibodies

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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Arrestin-2/β-Arrestin 1 Arrestin-3/β-Arrestin 2

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Description

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[1][2].

IC50 & Target[1][2]

CCR6

 

In Vitro

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.

IDOR-1117-2520 Related Antibodies
In Vivo

IDOR-1117-2520 (10-100 mg/kg for rats, 3-10 mg/kg for dogs; p.o.) is rapidly absorbed in rats and dogs, with peak plasma concentrations of IDOR-1117-2520 reached within 0.3-0.8 h[1].
IDOR-1117-2520 (0.02-1  mg/mL; p.o. via drinking water; 8  days) reduces CCR6+ cell migration and ear thickness in the Aldara® mouse model of skin inflammation[2].

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

Animal Model: Aldara® mouse model of skin inflammation[2]
Dosage: 0.02, 0.1, 0.3, 0.5 and 1  mg/mL
Administration: p.o. via drinking water; 8  days
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).
Animal Model: Aldara® mouse model of skin inflammation[2]
Dosage: 50  mg/kg
Administration: Gavage; twice per day; started on day 0, 3 or 5 post Aldara® treatment until day 7.
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.
Molecular Weight

436.55

Formula

C25H32N4O3
CAS No.
Appearance

Solid

Color

White to off-white

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
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 : 25 mg/mL (57.27 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 2.2907 mL 11.4534 mL 22.9069 mL
5 mM 0.4581 mL 2.2907 mL 4.5814 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.

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In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 99.94%

SDS (251 KB)

COA (253 KB) HNMR (397 KB) RP-HPLC (233 KB) LCMS (94 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, 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
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IDOR-1117-2520 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:

IDOR-1117-25202737274-49-4CCRCalcium ChannelArrestinP-glycoproteinCC chemokine receptorCa2+ channelsCa channelsP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243lung inflammationautoimmune diseaseskin inflammationmiceInhibitorinhibitorinhibit

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