A2A receptor antagonist 2 (Compound 57) 是一个有效的、高选择性的adenosine A2Areceptor拮抗剂，IC50值为8.3 nM。
| 生物活性 | A2A receptor antagonist 2 (Compound 57) is a potent, highly selectiveadenosine A2Areceptor(A2AR) antagonist with anIC50of 8.3 nM[1]. |
| IC50& Target | |
体外研究
(In Vitro) | 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)[1].
A2A receptor antagonist 2 enhances the activation and effector function of T cells, with no obvious cytotoxicity toward the HCT116 cells and MC38 cells[1].
Western Blot Analysis[1] | Cell Line: | Jurkat T cells | | Concentration: | 10 μM | | Incubation Time: | Overnight | | Result: | Increased IL-2 production in the presence of NECA |
Cell Cytotoxicity Assay[1] | Cell Line: | HCT116 and Jurkat T cells | | Concentration: | 10 μM | | Incubation Time: | 48 h | | Result: | Completely reversed NECA’s suppression of the cytotoxic function of Jurkat T cells. |
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体内研究
(In Vivo) | A2A receptor antagonist 2 (Compound 57) shows reasonable intravenous (IV) exposure and low bioavailabilities of intraperitoneal (IP) andper os(PO)[1].
| Animal Model: | C57BL/6 mice[1] | | Dosage: | 2 or 10 mg/kg | | Administration: | Intraperitoneal, intravenous or oral administration (Pharmacokinetic Analysis) | | Result: | PK profiles of A2A receptor antagonist 2 (n = 3)[1]
| Parameters | | | | | Dosing Route | IV (2 mg/kg) | PO (10 mg/kg) | IP (10mg/kg) | | Cmax(ng/mL) | 1091 ± 129a | 106 ± 33.0 | 41.8 ± 2.75 | | AUC0-last(ng/mL*h) | 767 ± 107 | 145 ± 25.9 | 812 ± 12.0 | | AUC0-t(ng/mL*h) | 764 ± 107 | 139 ± 25.9 | 444 ± 13.3 | | T1/2(h) | 2.05 ± 0.94 | 2.55 ± 2.39 | 17.6 ± 0.68 | | F (%) | / | 3.78% | 11.6% |
aThis value means C0= 1091 ± 129 ng/mL |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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