化合物ONO-8430506 T38759

Product Introduction
Bioactivity


英文名: ONO-8430506

描述: ONO-8430506 是一种可口服的、具有有效性的 autotaxin (ATX)/ENPP2 抑制剂（ IC90 ：100 nM），能够抑制小鼠血浆中 ATX 活性。

体外活性: The IC50 values of ONO-8430506 against the lysophospholipase D (LysoPLD) activity of recombinant human ATX/ENPP2 are 5.1 nM and 4.5 nM, determined using synthetic fluorescent substrate (FS-3) and a natural substrate (16:0-LPC) assay, respectively.[2] ONO-8430506 exhibits effective inhibition of lysophosphatidic acid (LPA) formation, demonstrating IC50 values of approximately 10 nM with both recombinant and plasma-derived ATX/ENPP2 derived from diverse animal species.[2]

体内活性: ONO-8430506 (10 mg/kg/day; gavage; for 21 days). Tumor growth in ONO-8430506-treated mice caught up to the vehicle group by day 13; thereafter, primary tumor size was not significantly different from the vehicle-treated mice. It can slows initial tumor growth and limits lung metastasis. ONO-8430506 decreases the initial phase of breast tumor growth and subsequent lung metastases by ~60% in a syngeneic orthotopic mouse model.[1] ONO-8430506 (oral; 30 mg/kg) demonstrates good pharmacokinetics and persistently inhibits plasma lysophosphatidic acid formation in rats.[2] ONO-8430506 (30 or 100 mg/kg) enhances the antitumor effect of Paclitaxel in a breast cancer model.[3] ONO-8430506 exhibits moderate oral bioavailability (rat 51.6%, dog 71.1%, and monkey 30.8%) and C max (rat 261, dog 1670, and monkey 63 ng/mL) following oral administration (rat 1, dog 1, and monkey 1 mg/kg).[3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 90.0 mg/mL (195.0 mM)


关键字: ONO-8430506 | ONO 8430506 | ONO8430506

相关产品: Ginkgolide J | CP671305 | PDE5-IN-2 | Zardaverine | Trapidil | Pumafentrine | GEBR-7b | Mirodenafil | Glaucine | Autotaxin-IN-3

相关库: Bioactive Compounds Library Max | Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途