AUNP-12 acetate
作者：齐岳
发布时间：2023-09-13
16:37:29
点击数：
产品名称：AUNP-12 acetate
产品描述：
| 产品描述 | AUNP-12 acetate is a polypeptide inhibitor of PD-1 that is equivalent to PD-1 and PD-2 in inhibiting lymphocyte proliferation and effector fuction, in addition to immune activation and antitumor activity. |
| 体外活性 | In vitro, AUNP-12 displayed equipotent antagonism toward PD-L1 and PD-L2 in the rescue of lymphocyte proliferation and effector functions. In human PBMC cells, AUNP-12 was also able to significantly rescue recombinant human PD-L1 and PD-L2 mediated inhibition in vitro, with average EC50 values of 63.3 nM and 44.1 nM against PD-L1 and PD-L2 respectively. [1] |
| 体内活性 | AUNP-12 acetaterescued the proliferation in the mouse splenocyte assay system, with average EC50 values of 17 nM and 16.6 nM against rmPD-L1 and rmPD-L2 respectively. AUNP-12 (6 hours) showed a Plasma protein binding of 93.9% with plasma stability of more than 60%. AUNP-12 exhibited a half-life of 90 minutes in mouse liver microsomes. In male Balb/c mice, AUNP-12 subcutaneous injection or intravenous injection as a concentration of 3 mg/kg for its PK study. As a result, AUNP-12 shows a low volume of distribution, and the peak plasma levels reach at 0.2-0.4 hours. The absolute bioavailability of AUNP-12 is about 77% in mice. [1] |
| 别名 | AUNP-12 acetate (1353563-85-5 Free base) |
| 分子量 | 3321.61 |
| 分子式 | C144H230N40O50 |
存储
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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