C-021

Modify Date: 2024-01-21 23:57:41

C-021 Structure
C-021 structure
Common Name C-021
CAS Number 864289-85-0 Molecular Weight 467.65
Density N/A Boiling Point N/A
Molecular Formula C27H41N5O2 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of C-021


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].

 Names

Name 2-([1,4'-bipiperidin]-1'-yl)-N-cycloheptyl-6,7-dimethoxyquinazolin-4-amine
Synonym More Synonyms

 C-021 Biological Activity

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].
Related Catalog
Target

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].
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]. 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.
References

[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.

[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.

 Chemical & Physical Properties

Molecular Formula C27H41N5O2
Molecular Weight 467.65
Exact Mass 467.32600
PSA 62.75000
LogP 5.31230

 Synonyms

2-(1,4'-BIPIPERIDIN)-1'-YL-N-CYCLOHEPTYL-6,7-DIMETHOXY-4-QUINAZOLINAMINE
C 021 dihydrochloride