2. Membrane Transporter/Ion Channel Apoptosis MAPK/ERK Pathway Stem Cell/Wnt NF-κB Immunology/Inflammation Metabolic Enzyme/Protease
  3. P2X Receptor Apoptosis ERK p38 MAPK c-Myc NF-κB Reactive Oxygen Species (ROS)
  4. Bullatine A

Bullatine A  (Synonyms: 雪上一枝蒿甲素)

目录号: HY-N5025 纯度: ≥98.0%
COA 产品使用指南 技术支持

Bullatine A，一种二萜生物碱，是强效的 P2X7 拮抗剂。Bullatine A 具有抗风湿、抗炎和抗痛觉作用。Bullatine A 抑制 ATP 诱导的 BV-2 细胞死亡/凋亡 (apoptosis) 以及 P2X 受体介导的炎症反应。Bullatine A 通过靶向 SIRT6 抑制胶质瘤细胞生长。Bullatine A 特异性地减轻大鼠的痛觉过敏。Bullatine A 通过抑制小鼠中的 ROS/JNK/NF-κB 途径减轻 LPS (HY-D1056) 诱导的全身炎症反应。Bullatine A 改善慢性社交挫败应激 (CSDS) 小鼠的绝望行为。Bullatine A 可用于炎症、胶质母细胞瘤 (GBM) 和抑郁症研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

Bullatine A

Bullatine A Chemical Structure

CAS No. : 1354-84-3

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
1 mg ￥571
In-stock
5 mg ￥1500
In-stock
10 mg ￥2500
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

Bullatine A 相关抗体

Top Publications Citing Use of Products

查看 P2X Receptor 亚型特异性产品:

查看所有亚型
P2X1 Receptor P2X2 Receptor P2X3 Receptor P2X4 Receptor P2X7 Receptor

查看 ERK 亚型特异性产品:

查看所有亚型
ERK ERK1 ERK2 ERK5 ERK8

查看 p38 MAPK 亚型特异性产品:

查看所有亚型
p38 MAPK p38α p38β MAPK13 p38δ p38γ

查看 NF-κB 亚型特异性产品:

查看所有亚型
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bullatine A, a diterpenoid alkaloid, is a potent P2X7 antagonist. Bullatine A possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A inhibits ATP-induced BV-2 cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A suppresses glioma cell growth by targeting SIRT6. Bullatine A specifically attenuates pain hypersensitivity in rats. Bullatine A attenuates LPS (HY-D1056)-induced systemic inflammatory response by inhibiting the ROS/JNK/NF-κB pathway in mice. Bullatine A improves despair behavior in Chronic chronic social defeat stress (CSDS) mice. Bullatine A can be used for the study of inflammation, glioblastoma (GBM) and depression[1][2][3][4][5].

IC50 & Target[1]

P2X7 Receptor

 

体外研究
(In Vitro)

Bullatine A (1-50 μM，24 小时) 抑制 ATP 诱导的 BV-2 细胞死亡，下调 IL-6、IL-1β、iNOS 的 mRNA 水平，减少 NO 和 IL-6 的过量产生，并选择性地抑制 BV-2 细胞中 P2X7 受体 mRNA 的上调 (对 P2X4 mRNA 无影响)[1]。
Bullatine A (1-100 μM，6 小时) 以剂量依赖方式刺激原代小胶质细胞中前动力蛋白的表达，EC50 为 3.2 μM[2]。
Bullatine A (10-80 μM，6 小时) 显著抑制 LPS (HY-D1056) 诱导的 BV2 小胶质细胞和 iBMDMs 中 IL-1β、IL-6、iNOS 和 TNF-α 的 mRNA 表达[3]。
Bullatine A (80 μM) 抑制 LPS 诱导的 iBMDMs 中 IKKα/β、IκBα 的磷酸化和 NF-κB p65 的核转位，减少 JNK 磷酸化，但对 p38、ERK1/2 磷酸化无明显影响[3]。
Bullatine A (80 μM，24 小时) 减少 LPS 诱导的 iBMDMs 中细胞内 ROS 生成[3]。
Bullatine A (50-800 nM，7 天) 以剂量依赖方式降低 U87MG 和 U251 细胞的集落形成能力[4]。
Bullatine A (5-45 μM，24 小时) 以剂量依赖方式增加 U87MG 细胞的早期和晚期凋亡率，降低线粒体膜电位，并诱导 U87MG 和 U251 细胞的 G2/M 期细胞周期阻滞[4]。
Bullatine A (5-45 μM，24 小时) 在 U87MG 细胞中下调 p-ERK 和 Myc 的表达并以剂量依赖方式抑制 H3K9Ac、H3K56Ac 的表达，同时上调 SIRT6 的表达[4]。
Bullatine A (50 μM，24 小时) 抑制 eATP 诱导的 BV-2 细胞中线粒体钙超载、ER-线粒体共定位增加、PERK-elF-2α UPR 激活、溶酶体产生、NLRP3 炎症体蛋白表达升高以及细胞存活率降低[5]。

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

Bullatine A 相关抗体:

Real Time qPCR[1]

Cell Line: ATP-induced BV-2 cells
Concentration: 1, 10, 50 μM
Incubation Time: 24 h
Result: Up-regulated the ratio of Bcl-2/Bax mRNA.
Down-regulated ATP-induced mRNA levels of IL-6, IL-1β and iNOS in BV-2 cells.
Inhibited ATP-induced up-regulation of P2X7 receptor mRNA without obvious effect on P2X4 mRNA in BV-2 cells.

Real Time qPCR[3]

Cell Line: LPS-induced BV2 microglia and iBMDMs
Concentration: 10, 20, 40, 80 μM
Incubation Time: 6 h
Result: Inhibited LPS (HY-D1056)-induced mRNA expression of IL-1β, IL-6, iNOS and TNF-α in BV2 microglia and iBMDMs.

Cell Cycle Analysis[4]

Cell Line: U87MG and U251 cells
Concentration: 5, 15, 45 μM
Incubation Time: 24 h
Result: Induced G2/M phase cell cycle arrest in U87MG and U251 cells.

Apoptosis Analysis[4]

Cell Line: U87MG cells
Concentration: 5, 15, 45 μM
Incubation Time: 24 h
Result: Increased the early and late apoptosis rates of U87MG cells.
Upregulated the expression of cleaved caspase-9, cleaved caspase-3 and Bax.
Downregulated the expression of Bcl-2.

Western Blot Analysis[4]

Cell Line: U87MG cells
Concentration: 5, 15, 45 μM
Incubation Time: 24 h
Result: Downregulated the expression of p-ERK and Myc proteins in U87MG cells.
Inhibitd the expression of H3K9Ac and H3K56Ac in U87MG cells.
Upregulated the expression of SIRT6.
体内研究
(In Vivo)

Bullatine A (0.3-30 mg/kg，皮下注射，累计剂量每隔 1 小时给药) 以剂量依赖方式减轻脊神经结扎诱导的神经病理性疼痛大鼠和完全弗氏佐剂 (CFA) 诱导的炎性疼痛大鼠的机械性痛觉过敏和热痛觉过敏[2]。
Bullatine A (0.3-30 mg/kg，皮下注射，累计剂量每隔 1 小时给药) 缓解 Walker 256 诱导的骨癌疼痛大鼠和 Streptozotocin (HY-13753) 诱导的神经病理性疼痛大鼠的机械性痛觉过敏[2]。
Bullatine A (0.3-30 μg (10 μL)，鞘内注射，单次剂量) 抑制神经病理性疼痛大鼠的机械性痛觉过敏[2]。
Bullatine A (5-20 mg/kg，腹腔注射，在 LPS 注射前 12 小时和 1 小时各给药一次) 减轻小鼠中 LPS 诱导的全身炎症反应[3]。
Bullatine A (10 μg/kg，灌胃给药，每日一次，2 周) 改善 CSDS 小鼠的绝望行为[5]。
Bullatine A (10 μg，海马内微注射，每两天一次，10 天) 部分改善海马 MAMs 中 CSDS 诱导的抑郁样行为[5]。

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

Animal Model: Spinal nerve ligation-induced neuropathic pain model: adult male Wistar rats were subjected to tight ligation of left L5 and L6 spinal nerves under isoflurane anesthesia[2]
Dosage: 0.3, 1, 3, 10, 30 mg/kg
Administration: s.c. cumulative doses at 1 h intervals
Result: Attenuated mechanical allodynia and thermal hyperalgesia in spinal nerve ligation-induced neuropathic pain rats, with ED50 of 1.9 mg/kg and 0.7 mg/kg, Emax of 56.6% MPE and 66.1% MPE respectively.
Animal Model: Diabetic neuropathic pain model: adult male Wistar rats were fasted for 16 h, then received a single intravenous injection of Streptozotocin (40 mg/kg)[2]
Dosage: 0.3, 1, 3, 10, 30 mg/kg
Administration: s.c. cumulative doses at 1 h intervals
Result: Alleviated mechanical allodynia in streptozotocin-induced diabetic neuropathic pain rats, with ED50 of 1.2 mg/kg and Emax of 65.5% MPE.
Animal Model: Complete Freund’s adjuvant (CFA)-induced inflammatory pain model: 100 μL of CFA was injected into the tibiotarsal joint of the left hindpaw of adult male Wistar rats under mild isoflurane anesthesia[2]
Dosage: 0.3, 1, 3, 10, 30 mg/kg
Administration: s.c. cumulative doses at 1 h intervals
Result: Reduced mechanical allodynia and thermal hyperalgesia in CFA-induced inflammatory pain rats, with ED50 of 1.4 mg/kg and 0.6 mg/kg, Emax of 50.2% MPE and 60.2% MPE respectively.
Animal Model: Bone cancer pain model: Adult female Wistar rats were anesthetized with intraperitoneal pentobarbital (50 mg/kg), and 4 × 1050 Walker 256 carcinoma cells in 10 μL phosphate buffer solution were injected into the medullary cavity of the left tibia[2]
Dosage: 0.3, 1, 3, 10, 30 mg/kg
Administration: s.c. cumulative doses at 1 h intervals
Result: Mitigated mechanical allodynia in bone cancer pain rats induced by tibial implantation of Walker 256 carcinoma cells, with ED50 of 0.9 mg/kg and Emax of 45.6% MPE.
Animal Model: Spinal nerve ligation-induced neuropathic pain model: adult male Wistar rats were subjected to tight ligation of left L5 and L6 spinal nerves under isoflurane anesthesia[2]
Dosage: 0.3, 1, 3, 10, 30 μg (10 μL)
Administration: i.t. for a single dose
Result: Inhibited mechanical allodynia in neuropathic pain rats, with ED50 of 1.1 μg and Emax of 55.5% MPE.
Animal Model: C57BL/6 mice (8-10 weeks old, male, 20-25 g) were intraperitoneally injected with 5 mg/kg LPS to induce systemic inflammatory response[3]
Dosage: 5, 10, 20 mg/kg
Administration: i.p., twice at 12 h and 1 h prior to LPS injection
Result: Alleviated LPS-induced liver and lung tissue damage with reduced pathological scores.
Reduced serum IL-6 levels in LPS-treated mice.
Down-regulated mRNA expression of IL-1β, IL-6, iNOS and TNF-α in liver and showed similar trend in lung.
Attenuated immune cell infiltration and structural disruption in liver and lung tissues.
Animal Model: 8-week-old C57BL/6J mice were subjected to chronic social defeat stress (CSDS) for 10 days[5]
Dosage: 10 μg/kg
Administration: i.g. once daily for 2 weeks
Result: Shortened immobility time in forced swimming test (FST) at 10 μg/kg dose, improving despair behavior.
Showed no significant effects on social interaction ratio (SIT), total travel distance in open field test (OFT), or sucrose preference rate (SPT).
Failed to inhibit hippocampal microglia activation induced by CSDS.
Animal Model: 8-week-old C57BL/6J mice underwent hippocampal catheterization surgery, recovered, then were subjected to 10-day CSDS[5]
Dosage: 10 μg
Administration: Intra-hippocampal microinjection every two days for 10 days
Result: Increased social interaction ratio (SIT) and shortened immobility time in FST at 10 μg dose, partially ameliorating depressive-like behaviors.
Showed no significant changes in total travel distance in OFT.
Inhibited the increase of Facl-4 protein in hippocampal mitochondrial-associated ER membranes (MAMs) .
Had no significant effect on other MAMs-related proteins (Sigma-1, VDAC, Mfn2).
分子量

343.50

Formula

C22H33NO2
CAS 号
性状

固体

颜色

White to off-white

中文名称

雪上一枝蒿甲素
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 12.5 mg/mL (36.39 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9112 mL 14.5560 mL 29.1121 mL
5 mM 0.5822 mL 2.9112 mL 5.8224 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Bullatine A 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.9112 mL 14.5560 mL 29.1121 mL 72.7802 mL
5 mM 0.5822 mL 2.9112 mL 5.8224 mL 14.5560 mL
10 mM 0.2911 mL 1.4556 mL 2.9112 mL 7.2780 mL
15 mM 0.1941 mL 0.9704 mL 1.9408 mL 4.8520 mL
20 mM 0.1456 mL 0.7278 mL 1.4556 mL 3.6390 mL
25 mM 0.1164 mL 0.5822 mL 1.1645 mL 2.9112 mL
30 mM 0.0970 mL 0.4852 mL 0.9704 mL 2.4260 mL
Help & FAQs
  • 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.

Keywords:

Bullatine A1354-84-3雪上一枝蒿甲素P2X ReceptorApoptosisERKp38 MAPKc-MycNF-κBReactive Oxygen Species (ROS)P2XRsExtracellular signal regulated kinasesMycNuclear factor-κBNuclear factor-kappaBBV-2P2X receptorAnti-inflammationPainGlioma Cell proliferationSIRT6depressionInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
Bullatine A
目录号：
HY-N5025
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z