1. GPCR/G Protein
    Immunology/Inflammation
  2. CCR
  3. C-021

C-021 

Cat. No.: HY-103364
Handling Instructions

C-021 is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM.

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

C-021 Chemical Structure

C-021 Chemical Structure

CAS No. : 864289-85-0

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Description

C-021 is a potent CC chemokine receptor-4 (CCR4) antagonist. C-021 potently inhibits functional chemotaxis in human and mouse with IC50s of 140 nM and 39 nM, respectively. C-021 effectively prevents human CCL22-derived [35S]GTPγS from binding to the receptor with an IC50 of 18 nM[1].

IC50 & Target[1]

CCR4

 

In Vitro

The in vitro oxidative metabolic stability of C-021 (Compound 1b) is evaluated by measuring the rate of drug consumption in human liver microsomes (HML), thus providing intrinsic clearance values (CLint). C-021 exhibits CLint value of 17,377 mL/h/kg[1].

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

In Vivo

The potency of C-021 (Compound 1b) is evident after subcutaneous administration in the murine oxazolone-induced contact hypersensitivity test, a known model of acute skin inflammation. When C-021 is administered orally, however, very little inhibition is observed[1].
C-021 (1 mg/kg; i.p.; daily; for 3 days) significantly less microgliosis in acute liver failuremice[2].

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

Animal Model: Male C57Bl/6 mice (20-25 g) with acute liver failure[2]
Dosage: 1 mg/kg
Administration: i.p.; daily; for 3 days
Result: Significantly less microgliosis, and significantly reduced the pERK1/2 to tERK1/2 ratio.
Molecular Weight

467.65

Formula

C₂₇H₄₁N₅O₂

CAS No.
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Storage

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

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C-021
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HY-103364
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