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Osthole/蛇床子素 {[allProObj[0].p_purity_real_show]}

货号:A141553 同义名: Osthol; NSC 31868

Osthole是一种 O-甲基化香豆素,是组胺 H1 受体抑制剂,具有免疫调节、抗氧化和抗炎活性。

Osthole/蛇床子素 化学结构 CAS号:484-12-8
Osthole/蛇床子素 化学结构
CAS号:484-12-8
Osthole/蛇床子素 3D分子结构
CAS号:484-12-8
Osthole/蛇床子素 化学结构 CAS号:484-12-8
Osthole/蛇床子素 3D分子结构 CAS号:484-12-8
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Osthole/蛇床子素 纯度/质量文件 产品仅供科研

货号:A141553 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine 2HCl 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

99%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

99%
Azelastine HCl 98%
Epinastine HCl 99%
Levodropropizine 97%
Cyproheptadine HCl 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin HCl 99+%
Buclizine 2HCl 95%
Latrepirdine 2HCl GluR 99%
Cetirizine 2HCl 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。

Osthole/蛇床子素 生物活性

描述 Osthole, a natural coumarin found in traditional Chinese medicinal herbs, has therapeutic potential in the treatment of various diseases. Mice were administered osthole (100 mg/kg/d, ip) for 3 d, then on the fourth day APAP (Acetaminophen) (300 mg/kg, ip) was co-administered with osthole. Compared with the mice treated with APAP alone, osthole pretreatment significantly reduced serum MDA levels and hepatic H2O2 levels, and improved liver GSH levels and the GSSG-to-GSH ratio. In cultured murine primary hepatocytes and Raw264.7 cells, however, osthole (40 μM) did not alleviate APAP-induced cell death, but it significantly suppressed APAP-caused elevation of inflammatory cytokines[3]. Mice were injected with osthole (100 mg/kg, ip) or vehicle, followed by TMX (Tamoxifen, 90 mg/kg, ip) 24 h later. Osthole prevents TMX hepatotoxicity by suppressing p38 activation and subsequently reducing TMX-induced oxidative damage[4]. Pretreatment with osthole (100 mg/kg/d, ip, 3d) significantly ameliorated the clinical scores, colon length shortening, colonic histopathological changes and the expression of inflammatory mediators in TNBS-induced colitis. In mouse peritoneal macrophages, pretreatment with osthole (50 μM) significantly attenuated the LPS-induced elevation of cytokines at the mRNA level[5]. Osthole can be considered as a potential component of the treatment of Osteoarthritis, for it possesses a cartilage protective effect, as well as anti-inflammation, analgesic, and movement improving effects[6].

Osthole/蛇床子素 参考文献

[1]Kuo PL, Hsu YL, et al. Osthole-mediated cell differentiation through bone morphogenetic protein-2/p38 and extracellular signal-regulated kinase 1/2 pathway in human osteoblast cells. J Pharmacol Exp Ther. 2005 Sep;314(3):1290-9.

[2]Ko FN, Wu TS, et al. Inhibition of platelet thromboxane formation and phosphoinositides breakdown by osthole from Angelica pubescens. Thromb Haemost. 1989 Nov 24;62(3):996-9.

[3]Cai Y, Sun W, Zhang XX, Lin YD, Chen H, Li H. Osthole prevents acetaminophen-induced liver injury in mice. Acta Pharmacol Sin. 2018 Jan;39(1):74-84

[4]Zhou WB, Zhang XX, Cai Y, Sun W, Li H. Osthole prevents tamoxifen-induced liver injury in mice. Acta Pharmacol Sin. 2019 May;40(5):608-619

[5]Sun W, Cai Y, Zhang XX, Chen H, Lin YD, Li H. Osthole pretreatment alleviates TNBS-induced colitis in mice via both cAMP/PKA-dependent and independent pathways. Acta Pharmacol Sin. 2017 Aug;38(8):1120-1128

[6]Chern CM, Zhou H, Wang YH, Chang CL, Chiou WF, Chang WT, Yao CH, Liou KT, Shen YC. Osthole ameliorates cartilage degradation by downregulation of NF-κB and HIF-2α pathways in an osteoarthritis murine model. Eur J Pharmacol. 2020 Jan 15;867:172799

Osthole/蛇床子素 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.09mL

0.82mL

0.41mL

20.47mL

4.09mL

2.05mL

40.93mL

8.19mL

4.09mL

Osthole/蛇床子素 技术信息

CAS号484-12-8
分子式C15H16O3
分子量 244.29
SMILES Code C1=CC(=C(C2=C1C=CC(O2)=O)CC=C(C)C)OC
MDL No. MFCD00076049
别名 Osthol; NSC 31868; Ostol; Ostole; 7-Methoxy-8-(3-methyl-2-butenyl)coumarin
运输蓝冰
InChI Key MBRLOUHOWLUMFF-UHFFFAOYSA-N
Pubchem ID 10228
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Sealed in dry,2-8°C

溶解方案

DMSO: 105 mg/mL(429.82 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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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