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

CCR4 antagonist 3 

Cat. No.: HY-131349
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CCR4 antagonist 3 is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity.

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

CCR4 antagonist 3 Chemical Structure

CCR4 antagonist 3 Chemical Structure

CAS No. : 2174938-70-4

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Description

CCR4 antagonist 3 is an orally active, potent and selective CCR4 antagonist. CCR4 antagonist 3, featuring a novel piperidinyl-azetidine motif, has IC50s of 22 nM and 50 nM in the calcium flux and CTX assay. CCR4 antagonist 3 has antitumor activity[1].

IC50 & Target[1]

CCR4

 

In Vitro

CCR4 antagonist 3 (compound 38) shows no activity in a CYP450 induction assay[1].
CCR4 antagonist 3 inhibits the migration of mouse iTreg cells with an IC50 of 39 nM, while the IC50 in human iTreg cells is 33 nM[1].

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

In Vivo

CCR4 antagonist 3 (compound 38; 50 mg/kg; PO; daily; for 40 days) significantly reduces the tumor growth[1].
CCR4 antagonist 3 (0.5 mg/kg; IV) has low clearance (CL=10.2 mL/min/kg), medium volume of distribution (Vss=5.2 L/kg), a T1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse[1].
CCR4 antagonist 3 has low clearance (CL=7.3 mL/min/kg), a half-life of 12.7 hr, and is 44% bioavailable in dog. CCR4 antagonist 3 has low clearance (CL=3.7 mL/min/kg), a long terminal half-life (10.7 hr), and good bioavailability (%F = 41) in cynomolgus monkey[1].

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

Animal Model: Six-to eight-week-old, female C57BL/6 mice with Pan02-OVA tumor[1]
Dosage: 50 mg/kg
Administration: PO; daily; for 40 days
Result: Significantly reduced the tumor growth.
Animal Model: Rat and mouse[1]
Dosage: 0.5 mg/kg of IV; 2 mg/kg of PO
Administration: IV or PO
Result: Possessed medium clearance (CL=47.6 mL/min/kg) and was 49% bioavailable upon oral dosing in rat.
Had low clearance (CL=10.2 mL/min/kg), medium volume of distribution (Vss=5.2 L/kg), a T1/2 of 6.9 h, and good bioavailability (%F = 29) of oral dosing in mouse.
Molecular Weight

500.42

Formula

C₂₄H₂₇Cl₂N₇O

CAS No.

2174938-70-4

SMILES

[H][[email protected]@]1(CCCN(C1)CCO)C2CN(C2)C3=CN=C(C4=N3)C(C#N)=NN4[[email protected]](C)C5=CC=C(C=C5Cl)Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

CCR4 antagonist 3CCRCC chemokine receptororallypiperidinyl-azetidinemotifantitumorCYP450Inhibitorinhibitorinhibit

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CCR4 antagonist 3
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