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ONO-8430506 {[allProObj[0].p_purity_real_show]}

货号:A1554598

ONO-8430506 化学结构 CAS号:1354805-08-5
ONO-8430506 化学结构
CAS号:1354805-08-5
ONO-8430506 3D分子结构
CAS号:1354805-08-5
ONO-8430506 化学结构 CAS号:1354805-08-5
ONO-8430506 3D分子结构 CAS号:1354805-08-5
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ONO-8430506 纯度/质量文件 产品仅供科研

货号:A1554598 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PDE PDE1 PDE10A PDE2 PDE3 PDE4 PDE5 PDE6 其他靶点 纯度
Doxofylline 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

96%
7-(2,3-Dihydroxypropyl)theophylline 98%
Aminophylline +

PDE, IC50: 0.12 mM

98+%
Anagrelide HCl 99%+
Irsogladine AChR,mAChR 99%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

99%+
Dipyridamole 98%
Luteolin +

PDE1, Ki: 15.0 μM

++

PDE2, Ki: 6.4 μM

+

PDE3, Ki: 13.9 μM

+

PDE4, Ki: 11.1 μM

+

PDE5, Ki: 9.5 μM

98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

97%
Milrinone ++

PDE2, IC50: 5.2 μM

++

PDE3, IC50: 2.1 μM

ATPase 99%
Pimobendan ++

PDE3, IC50: 0.32 μM

98%
Cilostazol ++

PDE3, IC50: 0.2 μM

98%
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

99% (HPLC)
Apremilast +++

PDE4, IC50: 74 nM

98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

98+%
Roflumilast ++++

PDE4A4, IC50: 4.3 nM

PDE4A1, IC50: 0.7 nM

99%
Rolipram +++

PDE4B, IC50: 130 nM

99%+
Cilomilast +++

HPDE4, IC50: 120 nM

LPDE4, IC50: 100 nM

99%
Fenspiride HCl +

PDE3, pIC50: 3.44

+

PDE4, pIC50: 4.16

99% (HPLC)
Avanafil ++++

PDE5, IC50: 1 nM

98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

98%
Icariin ++

PDE5, IC50: 0.432 μM

98%
Sildenafil +++

PDE6, IC50: 33 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

ONO-8430506 生物活性

描述 ONO-8430506 is an orally bioavailable and potent inhibitor of autotaxin (ATX)/ENPP2, displaying an IC90 of 100 nM for inhibiting ATX activity in mouse plasma[1][2][3].

ONO-8430506 动物研究

Animal study ONO-8430506, administered at 10 mg/kg/day via gavage for 21 days, slows the initial growth of tumors and curtails lung metastasis[1].ONO-8430506 reduces the initial phase of breast tumor growth and lung metastases by approximately 60% in a syngeneic orthotopic mouse model[1].ONO-8430506, given orally at 30 mg/kg, shows favorable pharmacokinetics and consistently inhibits the formation of plasma lysophosphatidic acid in rats[2].ONO-8430506 at doses of 30 or 100 mg/kg enhances the anticancer efficacy of Paclitaxel in a breast cancer model[3].ONO-8430506 demonstrates moderate oral bioavailability and peak plasma concentrations (Cmax) in rats (51.6%, 261 ng/mL), dogs (71.1%, 1670 ng/mL), and monkeys (30.8%, 63 ng/mL) at a dose of 1 mg/kg orally[3].ONO-8430506 exhibits terminal elimination half-lives of 3.4 hours in rats, 8.9 hours in dogs, and 7.9 hours in monkeys, with low plasma clearance rates (8.2 mL/min/kg in rats, 4.7 mL/min/kg in dogs, and 5.8 mL/min/kg in monkeys) and large volumes of distribution (1474 mL/kg in rats, 1863 mL/kg in dogs, and 2275 mL/kg in monkeys) following intravenous administration at 0.3 mg/kg[3].

ONO-8430506 参考文献

[1]Matthew G K Benesch, et al. Inhibition of autotaxin delays breast tumor growth and lung metastasis in mice. FASEB J. 2014 Jun;28(6):2655-66.

[2]Hiroshi Saga, et al. A novel highly potent autotaxin/ENPP2 inhibitor produces prolonged decreases in plasma lysophosphatidic acid formation in vivo and regulates urethral tension. PLoS One. 2014 Apr 18;9(4):e93230.

[3]Yuzo Iwaki, et al. ONO-8430506: A Novel Autotaxin Inhibitor That Enhances the Antitumor Effect of Paclitaxel in a Breast Cancer Model. ACS Med Chem Lett. 2020 May 14;11(6):1335-1341.

ONO-8430506 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.67mL

4.33mL

2.17mL

ONO-8430506 技术信息

CAS号1354805-08-5
分子式C27H28FN3O3
分子量 461.53
SMILES Code O=C(C1(C2)CCC2(CC(N3CCC(C4=CC=CN=C4N5CC6=CC=C(F)C=C6)=C5C3)=O)CC1)O
MDL No. MFCD34604003
别名
运输蓝冰
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry, store in freezer, under -20°C

溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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