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C 021 dihydrochloride

Catalog No.
B5457
Potent CCR4 antagonist
Grouped product items
SizePriceStock Qty
1mg
$85.00
Ship with 5-10 days
5mg
$277.00
Ship with 5-10 days
For scientific research use only and should not be used for diagnostic or medical purposes.

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

C 021 dihydrochloride is a potent antagonist of CCR4 with IC50 values of 0.039 and 0.14 μM for inhibition of chemotaxis in mouse and human, respectively [1].

CC chemokine receptor 4 (CCR4) is a G protein-coupled receptor and is a receptor for the CC chemokines, which play an important role in the development and function of the immune system.

C 021 dihydrochloride is a potent CCR4 antagonist. C 021 dihydrochloride potently inhibited functional chemotaxis in mice and human with IC50 values of 0.039 and 0.14 μM, respectively. In the GTPγS-binding assay, C 021 dihydrochloride was active with IC50 value of 0.018 μM [1].

Treatment mice with azoxymethane (AOM), which induced hepatic encephalopathy, AOM significantly increased microglia activation and the concentrations of CCL2 in the liver, serum, and cortex. C 021 dihydrochloride reduced liver damage and significantly improved the neurological outcomes. Also, C 021 dihydrochloride reduced microglia activation and phosphorylation of ERK1/2, and inhibited AOM-induced cytokine upregulation [2].

References:
[1].  Yokoyama K, Ishikawa N, Igarashi S, et al. Potent and orally bioavailable CCR4 antagonists: Synthesis and structure-activity relationship study of 2-aminoquinazolines. Bioorg Med Chem, 2009, 17(1): 64-73.
[2].  McMillin M, Frampton G, Thompson M, et al. Neuronal CCL2 is upregulated during hepatic encephalopathy and contributes to microglia activation and neurological decline. J Neuroinflammation, 2014, 11: 121.

Chemical Properties

Physical AppearancePale yellow solid
StorageStore at -20°C
M.Wt540.57
Cas No.864289-85-0
FormulaC27H41N5O2·2HCl
SolubilitySoluble in DMSO
Chemical Name2-([1,4'-bipiperidin]-1'-yl)-N-cycloheptyl-6,7-dimethoxyquinazolin-4-amine dihydrochloride
SDFDownload SDF
Canonical SMILESCOC1=CC2=C(N=C(N=C2N(C3CCCCCC3)[H])N4CCC(CC4)N5CCCCC5)C=C1OC.Cl.Cl
Shipping ConditionSmall Molecules with Blue Ice, Modified Nucleotides with Dry Ice.
General tips We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Quality Control & MSDS

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Chemical structure

C 021 dihydrochloride