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Supplier NameMedChemExpress (MCE)
Contactsales
Tel609-228-6898
Mobile609-228-6898
QQ
Emailsales@medchemexpress.com; tech@medchemexpress.com
Websitehttps://www.medchemexpress.com/
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Product NameCCR4 Antagonist
SynonymsCCR4 Antagonist
CAS864289-85-0
EINECS
Chemical FormulaC27H41N5O2
Molecular Weight467.7
inchi
Package10 mM * 1 mL;5 mg;10 mg;25 mg
PriceEmail to quote
DescriptionsC-021

C-021

MedChemExpress (MCE)

HY-103364

864289-85-0

99.95%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Room temperature in continental US

Descriptions

C-021

C-021

MedChemExpress (MCE)

HY-103364

864289-85-0

99.95%

Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

Room temperature in continental US
may vary elsewhere.

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.

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].

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].

CCR4

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[1]. Yokoyama K, et al. Potent and orally bioavailable CCR4 antagonists: Synthesis and structure-activity relationship study of 2-aminoquinazolines. Bioorg Med Chem. 2009 Jan 1
17(1):64-73.
[Content Brief]

[2]. Matthew McMillin, et al. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation. 2014 Jul 10
11:121.
[Content Brief]

Supplier Websitehttps://www.medchemexpress.com/c-021.html
Last Update2025-05-21 16:50:25
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