产品
编 号：F755829
分子式：C25H28FN7O3
分子量：493.53
分子式：C25H28FN7O3
分子量：493.53
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CAS No: 2767206-20-0
产品详情
生物活性：
A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM.
体内研究：
A2A receptor antagonist 2 (Compound 57) shows reasonable intravenous (IV) exposure and low bioavailabilities of intraperitoneal (IP) and per os (PO).Animal Model:C57BL/6 mice
Dosage:2 or 10 mg/kg
Administration:Intraperitoneal, intravenous or oral administration (Pharmacokinetic Analysis)
Result:PK profiles of A2A receptor antagonist 2 (n = 3)Parameters
Dosing RouteIV (2 mg/kg)PO (10 mg/kg)IP (10mg/kg)
Cmax (ng/mL)1091 ± 129a106 ± 33.041.8 ± 2.75
AUC0-last (ng/mL*h)767 ± 107145 ± 25.9812 ± 12.0
AUC0-t (ng/mL*h)764 ± 107139 ± 25.9444 ± 13.3
T1/2 (h)2.05 ± 0.942.55 ± 2.3917.6 ± 0.68
F (%)/3.78%11.6%
a This value means C0 = 1091 ± 129 ng/mL
体外研究：
A2A receptor antagonist 2 (Compound 57) shows potent antagonistic activity in the presence of a high level of NECA (5′-N-ethylcarboxamidoadenosine, an A2AR agonist) .A2A receptor antagonist 2 enhances the activation and effector function of T cells, with no obvious cytotoxicity toward the HCT116 cells and MC38 cells.
A2A receptor antagonist 2 (Compound 57) is a potent, highly selective adenosine A2A receptor (A2AR) antagonist with an IC50 of 8.3 nM.
体内研究：
A2A receptor antagonist 2 (Compound 57) shows reasonable intravenous (IV) exposure and low bioavailabilities of intraperitoneal (IP) and per os (PO).Animal Model:C57BL/6 mice
Dosage:2 or 10 mg/kg
Administration:Intraperitoneal, intravenous or oral administration (Pharmacokinetic Analysis)
Result:PK profiles of A2A receptor antagonist 2 (n = 3)Parameters
Dosing RouteIV (2 mg/kg)PO (10 mg/kg)IP (10mg/kg)
Cmax (ng/mL)1091 ± 129a106 ± 33.041.8 ± 2.75
AUC0-last (ng/mL*h)767 ± 107145 ± 25.9812 ± 12.0
AUC0-t (ng/mL*h)764 ± 107139 ± 25.9444 ± 13.3
T1/2 (h)2.05 ± 0.942.55 ± 2.3917.6 ± 0.68
F (%)/3.78%11.6%
a This value means C0 = 1091 ± 129 ng/mL
体外研究：
A2A receptor antagonist 2 (Compound 57) shows potent antagonistic activity in the presence of a high level of NECA (5′-N-ethylcarboxamidoadenosine, an A2AR agonist) .A2A receptor antagonist 2 enhances the activation and effector function of T cells, with no obvious cytotoxicity toward the HCT116 cells and MC38 cells.
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