864289-85-0
864289-85-0 structure
- Name: C-021
- Chemical Name: 2-([1,4'-bipiperidin]-1'-yl)-N-cycloheptyl-6,7-dimethoxyquinazolin-4-amine
- CAS Number: 864289-85-0
- Molecular Formula: C27H41N5O2
- Molecular Weight: 467.65
- Catalog: Signaling Pathways GPCR/G Protein CCR
- Create Date: 2017-02-16 00:13:21
- Modify Date: 2024-01-21 23:57:41
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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].
| Name | 2-([1,4'-bipiperidin]-1'-yl)-N-cycloheptyl-6,7-dimethoxyquinazolin-4-amine |
|---|---|
| Synonyms |
2-(1,4'-BIPIPERIDIN)-1'-YL-N-CYCLOHEPTYL-6,7-DIMETHOXY-4-QUINAZOLINAMINE
C 021 dihydrochloride |
| 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 |
| Molecular Formula | C27H41N5O2 |
|---|---|
| Molecular Weight | 467.65 |
| Exact Mass | 467.32600 |
| PSA | 62.75000 |
| LogP | 5.31230 |