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编 号：F356806
分子式：C22H36N2O6
分子量：424.53
分子式：C22H36N2O6
分子量：424.53
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CAS No: 431077-35-9
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生物活性：
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research.
体内研究：
PPI-2458 (0-50 mg/kg，口服，隔日一次)逆转 PG-PS (25 mg/kg, i.p) 诱导的关节炎模型中的关节肿胀和炎症。PPI-2458 (0-3 mg/kg，鼻胃插管，隔日一次)可导致实验初代食蟹猴生发中心生发中心淋巴细胞减少。PPI-2458 (0-100 mg/kg，口服，隔日一次)以剂量依赖的方式显著抑制肿瘤生长在SR肿瘤异种移植的严重联合免疫缺陷小鼠中。Animal Model:Female Lewis rats (101–121 g, PG-PS (25 mg/kg, i.p.)-induced arthritis model)
Dosage:0.25, 1, 5, and 50 mg/kg
Administration:Orally (po), started at day 15 after the chronic destructive phase of the disease was established and terminated on day 31
Result:Significantly and dose-dependently attenuated the chronic inflammatory response. Markedly attenuated paw swelling in a dose-dependent manner with maximal protection at an orally administered dose of 50 mg/kg at day 31.
Animal Model:Forty-two experimentally naive cynomolgus monkeys
Dosage:0.1 mg/kg (three males and three females), 0.3 mg/kg (three males and three females), 1.0 mg/kg (five males and five females), and 3.0 mg/kg (five males and five females)
Administration:Nasogastric intubation every other day (QOD) for 13 days (total of seven treatments)
Result:Exhibited a marked decrease in germinal center lymphocytes.
Animal Model:60 female Fox Chase severe combined immunodeficient mice (SR lymphoma cells were injected s.c. above the right hind leg)
Dosage:10, 30, or 100 mg/kg
Administration:oral gavage, QOD
Result:Significantly suppressed tumor growth in a dose-dependent manner. PPI-2458 administered at 100 mg/kg produced the greatest degree of tumor growth inhibition, which was 57% (P < 0.001) at the end of the study.
体外研究：
PPI-2458 可有效抑制 HUVEC 增殖，GI50 为0.2 nM，在1 nM 时最大抑制率大于 95%。PPI-2458 (0-100 nM, 6天)抑制 SU-DHL-16 细胞的增殖和MetAP-2。
PPI-2458 is a potent, orally active, selective and irreversible inhibitor of methionine aminopeptidase-2 (MetAP-2). PPI-2458 can be used for arthritis and lymphoma research.
体内研究：
PPI-2458 (0-50 mg/kg，口服，隔日一次)逆转 PG-PS (25 mg/kg, i.p) 诱导的关节炎模型中的关节肿胀和炎症。PPI-2458 (0-3 mg/kg，鼻胃插管，隔日一次)可导致实验初代食蟹猴生发中心生发中心淋巴细胞减少。PPI-2458 (0-100 mg/kg，口服，隔日一次)以剂量依赖的方式显著抑制肿瘤生长在SR肿瘤异种移植的严重联合免疫缺陷小鼠中。Animal Model:Female Lewis rats (101–121 g, PG-PS (25 mg/kg, i.p.)-induced arthritis model)
Dosage:0.25, 1, 5, and 50 mg/kg
Administration:Orally (po), started at day 15 after the chronic destructive phase of the disease was established and terminated on day 31
Result:Significantly and dose-dependently attenuated the chronic inflammatory response. Markedly attenuated paw swelling in a dose-dependent manner with maximal protection at an orally administered dose of 50 mg/kg at day 31.
Animal Model:Forty-two experimentally naive cynomolgus monkeys
Dosage:0.1 mg/kg (three males and three females), 0.3 mg/kg (three males and three females), 1.0 mg/kg (five males and five females), and 3.0 mg/kg (five males and five females)
Administration:Nasogastric intubation every other day (QOD) for 13 days (total of seven treatments)
Result:Exhibited a marked decrease in germinal center lymphocytes.
Animal Model:60 female Fox Chase severe combined immunodeficient mice (SR lymphoma cells were injected s.c. above the right hind leg)
Dosage:10, 30, or 100 mg/kg
Administration:oral gavage, QOD
Result:Significantly suppressed tumor growth in a dose-dependent manner. PPI-2458 administered at 100 mg/kg produced the greatest degree of tumor growth inhibition, which was 57% (P < 0.001) at the end of the study.
体外研究：
PPI-2458 可有效抑制 HUVEC 增殖，GI50 为0.2 nM，在1 nM 时最大抑制率大于 95%。PPI-2458 (0-100 nM, 6天)抑制 SU-DHL-16 细胞的增殖和MetAP-2。
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