ONO-0300302
目录号: PL06752 纯度: ≥99%
CAS No. :856689-51-5
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中文名称
ONO-0300302
英文名称
ONO-0300302
英文别名
3-(1-((2S,3S)-2-((2,3-dihydro-1H-inden-2-yl)methyl)-3-(3,5-dimethoxy-4-methylphenyl)-3-hydroxypropyl)-1H-pyrrol-3-yl)propanoic acid;BDBM50285779;J3.590.937K;3-[1-[(2S,3S)-2-(2,3-dihydro-1H-inden-2-ylmethyl)-3-(3,5-dimethoxy-4-methylphenyl)-3-hydroxypropyl]pyrrol-3-yl]propanoic acid;Chembl4165205
Cas No.
856689-51-5
分子式
C29H35NO5
分子量
477.59
包装储存
-20°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
产品详情
ONO-0300302 是一种口服有效的 LPA1 (溶血磷脂酸受体 1) 拮抗剂,其 IC50 为0.086 μM。ONO-0300302 是一种缓慢的紧密结合抑制剂,其结合亲和力随时间增加,其 Kd 为0.34 nM (37°C, 2 h)。ONO-0300302 可用于良性前列腺增生 (BPH) 的研究。
生物活性
ONO-0300302 is an orally active and potent LPA1 (lysophosphatidic acid receptor 1) antagonist, with an IC 50 of 0.086 μM. ONO-0300302 is a slow tight binding inhibitor, and its binding affinity increases with time, with K d of 0.34 nM (37 °C, 2 h). ONO-0300302 can be used for benign prostatic hyperplasia (BPH) research.
性状
Solid
IC50 & Target[1][2]
LPA1 Receptor 0.086 μM (IC50)
体外研究(In Vitro)
ONO-0300302 shows moderate stability against rat microsomes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ONO-0300302 inhibits significantly an LPA (lysophosphatidic acid receptor)-induced increase of intraurethral pressure (IUP) in rat (3 mg/kg, p.o.) and dog (1 mg/kg, p.o.) over 12 h. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[1]. Terakado M, et al. Discovery of a Slow Tight Binding LPA1 Antagonist (ONO-0300302) for the Treatment of Benign Prostatic Hyperplasia. ACS Med Chem Lett. 2017 Nov 20;8(12):1281-1286.
溶解度数据
In Vitro: DMSO : 220 mg/mL (460.65 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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