2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. CCR4 antagonist 3

CCR4 antagonist 3 is a potent chemokine receptor 4 (CCR4) antagonist with an IC50 value of 1.7 μM for [125I]TARC (thymus and activation regulated chemokine). CCR4 antagonist 3 inhibits binding of radiolabeled TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on the surface of CEM cells. CCR4 antagonist 3 also inhibits the in vitro migration of CEM cells mediated by TARC (IC50 = 6.4 μM).

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CCR4 antagonist 3

CCR4 antagonist 3 Chemische Struktur

CAS. Nr. : 1957-01-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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CCR4 antagonist 3 Related Antibodies

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Alle CCR Isoform-spezifische Produkte anzeigen:

Alle Isoformen anzeigen
CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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Beschreibung

CCR4 antagonist 3 is a potent chemokine receptor 4 (CCR4) antagonist with an IC50 value of 1.7 μM for [125I]TARC (thymus and activation regulated chemokine). CCR4 antagonist 3 inhibits binding of radiolabeled TARC and macrophage-derived chemokine (MDC) to CCR4 receptors on the surface of CEM cells. CCR4 antagonist 3 also inhibits the in vitro migration of CEM cells mediated by TARC (IC50 = 6.4 μM)[1].

IC50 & Target[1]

[125I]-TARC-CCR4

1.7 μM (IC50)

Cellular Effect
Cell Line Type Value Description References
CCRF-CEM IC50
3 3
Compound: 1
Displacement of [125I]MDC from CCR4 expressed in human CEM cell line
Displacement of [125I]MDC from CCR4 expressed in human CEM cell line
[PMID: 16497499]
CCRF-CEM IC50
1.7 3
Compound: 1
Displacement of [125I]TARC from CCR4 expressed in human CEM cell line
Displacement of [125I]TARC from CCR4 expressed in human CEM cell line
[PMID: 16497499]
CCRF-CEM IC50
1.7 3
Compound: 1
Displacement of [125I]TARC from CCR4 expressed in human CEM cell line
Displacement of [125I]TARC from CCR4 expressed in human CEM cell line
[PMID: 16497499]
CCRF-CEM IC50
3 3
Compound: 1
Displacement of [125I]MDC from CCR4 expressed in human CEM cell line
Displacement of [125I]MDC from CCR4 expressed in human CEM cell line
[PMID: 16497499]
CCRF-CEM IC50
6.4 3
Compound: 1
Inhibition of TARC-mediated CEM cell migration
Inhibition of TARC-mediated CEM cell migration
[PMID: 16497499]
CCRF-CEM IC50
6.4 3
Compound: 1
Inhibition of TARC-mediated CEM cell migration
Inhibition of TARC-mediated CEM cell migration
[PMID: 16497499]
In Vivo

CCR4 antagonist 3 (compound 1) (0.5 mg/kg for IV; 2 mg/kg for PO; single dosage) exhibits a high clearance, short half-life and low oral bioavailability[1].

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

Animal Model: Rats[1]
Dosage: 0.5 mg/kg for IV; 2 mg/kg for PO
Administration: IV and PO; single dosage
Result: Exhibited a high clearance of 4.2 L/h/kg and a short half-life of 0.4 h, and the oral bioavailability of 2%.
Molekulargewicht

240.32

Formel

C14H12N2S
CAS. Nr.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC1=CSC(NC2=C3C=CC=CC3=CC=C2)=N1
Versand

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

DMSO : 62.5 mg/mL (260.07 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 4.1611 mL 20.8056 mL 41.6112 mL
5 mM 0.8322 mL 4.1611 mL 8.3222 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.

  • Molaritätsrechner

  • Verdünnungsrechner

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.
Calculation results:
Working solution concentration: mg/mL
Reinheit & Dokumentation
Verweise

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 4.1611 mL 20.8056 mL 41.6112 mL 104.0280 mL
5 mM 0.8322 mL 4.1611 mL 8.3222 mL 20.8056 mL
10 mM 0.4161 mL 2.0806 mL 4.1611 mL 10.4028 mL
15 mM 0.2774 mL 1.3870 mL 2.7741 mL 6.9352 mL
20 mM 0.2081 mL 1.0403 mL 2.0806 mL 5.2014 mL
25 mM 0.1664 mL 0.8322 mL 1.6644 mL 4.1611 mL
30 mM 0.1387 mL 0.6935 mL 1.3870 mL 3.4676 mL
40 mM 0.1040 mL 0.5201 mL 1.0403 mL 2.6007 mL
50 mM 0.0832 mL 0.4161 mL 0.8322 mL 2.0806 mL
60 mM 0.0694 mL 0.3468 mL 0.6935 mL 1.7338 mL
80 mM 0.0520 mL 0.2601 mL 0.5201 mL 1.3003 mL
100 mM 0.0416 mL 0.2081 mL 0.4161 mL 1.0403 mL
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CCR4 antagonist 3 Related Classifications

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  • 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:

CCR4 antagonist 31957-01-3CCRCC chemokine receptorTARCthymuschemokinemacrophageMDCCEM cellsInhibitorinhibitorinhibit

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