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  3. Kukoamine B mesylate

Kukoamine B mesylate  (Synonyms: 地骨皮乙素甲磺酸盐)

目录号: HY-N2393A
产品使用指南 技术支持

Kukoamine B 是一种精胺生物碱,是一种强效的双重 LPS 和 CpG DNA 抑制剂,其 Kd 值分别为 1.23 µM 和 0.66 µM。Kukoamine B 具有抗炎、抗糖尿病、抗氧化、抗骨质疏松和神经保护作用。Kukoamine B 具有用于脓毒症研究的潜力。

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Kukoamine B mesylate Chemical Structure

Kukoamine B mesylate Chemical Structure

CAS No. : 1375179-86-4

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Kukoamine B mesylate 的其他形式现货产品:

Other Forms of Kukoamine B mesylate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Kukoamine B, a spermine alkaloid, is a potent dual LPS and CpG DNA inhibitor with Kd values of 1.23 µM and 0.66 µM, respectively. Kukoamine B exerts anti-inflammatory, anti-diabetic, anti-oxidant, anti-osteoporotic and neuroprotective effects. Kukoamine B has the potential for the study of sepsis. [1][2][3][4].

体外研究
(In Vitro)

Kukoamine B (5-20 μM, 2 h) 可增强 SH-SY5Y 细胞活力并防止质膜受到损伤[2]
Kukoamine B (5-20 μM, 2 h) 减轻 H2O2 诱导的 SH-SY5Y 细胞凋亡 (Apoptosis) 和线粒体膜电位 (mitochondria membrane potential (MMP)) 损失[2]
Kukoamine B (5-20 μM, 2 h) 通过调节 SH-SY5Y 细胞的 MAPKs 和 PI3K-AKT 信号通路,展现出抗氧化应激作用[2]
Kukoamine B (10-20 μM, 3 days) 促进前成骨细胞 MC3T3-E1 的成骨分化及矿化结节形成[3]
Kukoamine B (50-200 μM, 12 h) 是一种双重抑制剂,能够抑制 LPS 和 CpG DNA 诱导的 RAW 264.7 细胞和小鼠腹腔巨噬细胞释放 TNF-α 和 IL-6[4]
Kukoamine B (50-200 μM, 12 h) 下调由 LPS 和 CpG DNA 在 RAW 264.7 细胞中上调的两种受体 (TLR4TLR9) 以及两种重要酶 (iNOSCOX-2) 的 mRNA 表达[4]
Kukoamine B (0-200 μM, 30min-2 h) 在 RAW 264.7 细胞中抑制由 LPS 和 CpG DNA 诱导的 IkB-α 和 p38 磷酸化以及 NF-kB 的激活[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[2]

Cell Line: SH-SY5Y cells
Concentration: 5, 10, 20 μM (H2O2, 100 μM, for another 12 h)
Incubation Time: 2 h
Result: Prevented cell death and improved cell viability dose-dependently.
Lowered the LDH release.
Increased the activity of CAT, SOD, and GSH-Px, and reduced the MDA production

Apoptosis Analysis[2]

Cell Line: SH-SY5Y cells
Concentration: 5, 10, 20 μM (H2O2, 100 μM, for another 12 h)
Incubation Time: 2 h
Result: Decreased total apoptotic cells and late apoptotic cells.

Immunofluorescence[2]

Cell Line: SH-SY5Y cells
Concentration: 5, 10, 20 μM (H2O2, 100 μM, for another 12 h)
Incubation Time: 2 h
Result: Increased the fluorescence intensity of Rho (Rhodamine) 123.
Decreased the ROS production.

Western Blot Analysis[2]

Cell Line: SH-SY5Y cells
Concentration: 5, 10, 20 μM (H2O2, 100 μM, for another 12 h)
Incubation Time: 2 h
Result: Restored the mitochondria function via inhibiting the ratio of Bcl-2/Bax.
Decreased cytochromec, caspase-3, caspase-9, p-p38, p-ERK and p-JNK expression.
Increased p-AKT expression.

RT-PCR[4]

Cell Line: RAW 264.7 cells
Concentration: 0, 100, 200 μM
Incubation Time: 12 h
Result: Down-regulated the mRNA expression of two receptors (TLR4 and TLR9) and two important enzymes (iNOS and COX-2).

Western Blot Analysis[4]

Cell Line: RAW 264.7 cells
Concentration: 0, 100, 200 μM
Incubation Time: 30 min-2 h
Result: Suppressed the IkB-a and p38 phosphorylation as well as the degradation of IkB-a.
体内研究
(In Vivo)

Kukoamine B (20, 50 mg/kg, i.g., 每日一次, 连续 9 周) 减轻炎症并降低血糖,且不会导致体重增加或肝脏质量增加[1]
Kukoamine B (2, 5 mg/kg, p.o., 每日一次, 连续 12 周) 在去卵巢小鼠模型中展现出抗骨质疏松作用[3]
Kukoamine B (1.25-60 mg/kg, i.v., 1 次或每隔 8 h 一次 (连续3 天)) 能够保护在脓毒症模型中受到 大肠杆菌 感染的小鼠,并降低循环中 LPS 和 TNF-α 的水平[4]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male, 4-week old db/db mice (BKS.Cgm+/+Leprdb/J) and wildtype (WT) mice (C57BLKS/J-m+/+ db). A spontaneous type 2 diabetic animal model[1].
Dosage: 20, 50 mg/kg
Administration: i.g., daily, 9 weeks
Result: Successfully controlled the augment of blood glucose with age increase.
Reduced levels of 29 inflammatory markers such as IL-2, IL-3, IL-4, IL-5, IL-6, IL-7 and IL8.
Animal Model: Seven-week-old female ddy mice underwent either an ovariectomy or sham-operated surgery[3].
Dosage: 2, 5 mg/kg
Administration: p.o., daily, 12 weeks
Result: Inhibited the OVX-induced BMD loss in the right femur bone and restored the impaired bone structural properties of BV/TV, Tb.Th, Tb.N, and Tb.Sp.
Animal Model: Kunming (KM) mice, 4–6 weeks old, 18–20 g, male and female in equal number. Mice were injected with heat-killed E. coli (EC, 1.0 * 1011 CFU•kg-1) in order to establish the sepsis model.[4].
Dosage: 1.25, 2.5, 5, 10, 15, 30, 60 mg/kg
Administration: 80 mice (15, 30, 60 mg/kg), i.v., only one injection; 100 mice (1.25, 2.5, 5 mg/kg), i.v., every 8 h for 3 days; 96 mice, (60 mg/kg), i.v., once at 0, 2, 4, 6, 8 h after injection of EC.
Result: Significantly decreased the mortality rate from 87.5% to 62.5%, 62.5%, or 37.5% (15, 30, 60 mg/kg).
Decreased the mortality rate from 95% to 65%, 60% and 45% (1.25, 2.5 and 5 mg/kg).
Decreased the circulatory LPS and TNF-a levels in a time-dependent manner.
分子量

626.76

Formula

C29H46N4O9S

CAS 号
中文名称

地骨皮乙素甲磺酸盐

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Kukoamine B mesylate
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HY-N2393A
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