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IP2
MCE 国际站:IP2
产品活性:IP2 是一种免疫调节剂。IP2 增加癌细胞中 PTP 衍生的抗原呈递。IP2 对癌细胞无细胞毒性。IP2 在小鼠体内诱导肿瘤生长缺陷。
研究领域:Others
作用靶点:Others
In Vitro: IP2 (35 µM) shows immunomodulatory activity in murine MCA205 fibrosarcoma cells.
IP2 (35 µM) increases in the intron-derived SL8 antigen presentation.
IP2 (10 µM; 72 h) shows non-cytotoxic for cancer cells.
IP2 (10 µM) shows selectivity against three G-protein coupled receptor ADRB1 (35%), HRH2 (40%), and OPRD1 (53%), and inhibits the three enzymes of COX1 (52.8%), PDE3A (84.8%), and PDE4D2 (87.2%).
IP2 (10 µM) dose not induce immunogenic cell death hallmarks in human osteosarcoma U2OS cells.
In Vivo: IP2 (0.711 mg/kg for i.p. for mice; 9.103 mg/kg for i.v. for nice; 26.76 mg/kg for i.v. for dog) shows a high bioavailability in mice.
IP2 (50, 100, 250, 500 mg/kg; i.p.) shows very well toleration in C57BL/6 mice.
IP2 (2.5 mg/kg; i.v.) induces tumor growth defects in C57BL/6 mice.
IP2 (5 mg/kg; intratumor injection; three times per week for 2 weeks) induces tumor growth defects in C57BL/6 mice.
Pharmacokinetic Parameters of IP2 in Male C57BL/6J mice and male beagle dog.
| Dose (mg/kg) | Cmax (ng/mL) | Tmax (h) | T1/2 (h) | CL (mL/min/kg) | F % | MRT0-t (h) | AUCtot (ng/mL·h) | AUCextra (%) | |
| ip mice | 9.103 | 2078 | 0.0833 | 0.8 | 154 | 86 | 0.7 | 982.3 | 1.3 |
| iv mice | 0.711 | 322.7 | 0.0833 | 1.1 | 133 | 0.9 | 88.8 | 15.2 | |
| iv dog | 26.76 | 272 (µg/mL) | 0.0833 | 3.8 | 0.69 | 3.8 | 654.7 (µg/mL·h) | 0.9 |
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