2. Anti-infection
  3. Bacterial
  4. Pristimerin

Pristimerin  (Synonyms: 扁蒴藤素; Celastrol methyl ester)

目录号: HY-N1937 纯度: 99.22%
COA 产品使用指南

摩尔计算器

Pristimerin是高效可逆的单酰基甘油脂肪酶(MGL)抑制剂，IC50值为93 nM。

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Pristimerin Chemical Structure

Pristimerin Chemical Structure

CAS No. : 1258-84-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥787
In-stock
1 mg ￥316
In-stock
5 mg ￥748
In-stock
10 mg ￥1246
In-stock
25 mg ￥3000
In-stock
50 mg ￥4224
In-stock
100 mg ￥5913
In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Pristimerin:

Pristimerin 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM.

IC50 & Target

IC50: 93 nM (MGL)[1]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
1A9 ED50
0.1 μg/mL
Compound: 7
Cytotoxicity against human 1A9 cells after 3 days by SRB assay
Cytotoxicity against human 1A9 cells after 3 days by SRB assay
[PMID: 14640511]
1A9 ED50
0.11 μg/mL
Compound: 7
Cytotoxicity against human 1A9 cells after 6 days by SRB assay
Cytotoxicity against human 1A9 cells after 6 days by SRB assay
[PMID: 14640511]
1A9/ptx-10 ED50
0.076 μg/mL
Compound: 7
Cytotoxicity against human 1A9/PTX10 cells after 6 days by SRB assay
Cytotoxicity against human 1A9/PTX10 cells after 6 days by SRB assay
[PMID: 14640511]
1A9/ptx-10 ED50
0.11 μg/mL
Compound: 7
Cytotoxicity against human 1A9/PTX10 cells after 3 days by SRB assay
Cytotoxicity against human 1A9/PTX10 cells after 3 days by SRB assay
[PMID: 14640511]
A549 ED50
0.31 μg/mL
Compound: 7
Cytotoxicity against human A549 cells after 3 days by SRB assay
Cytotoxicity against human A549 cells after 3 days by SRB assay
[PMID: 14640511]
A549 IC50
1.03 μM
Compound: 1
Cytotoxic activity against human A549 cells incubated for 48 hrs by MTT assay
Cytotoxic activity against human A549 cells incubated for 48 hrs by MTT assay
[PMID: 28587825]
A549 IC50
1.1 μM
Compound: 1a
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
[PMID: 34170694]
A549 IC50
1.4 μM
Compound: CEL01
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 27647369]
Bel-7402 IC50
1.16 μM
Compound: 1
Cytotoxic activity against human Bel7402 cells incubated for 48 hrs by MTT assay
Cytotoxic activity against human Bel7402 cells incubated for 48 hrs by MTT assay
[PMID: 28587825]
HCT-8 ED50
0.15 μg/mL
Compound: 7
Cytotoxicity against human HCT8 cells after 3 days by SRB assay
Cytotoxicity against human HCT8 cells after 3 days by SRB assay
[PMID: 14640511]
HeLa IC50
0.32 μM
Compound: 1
Cytotoxic activity against human HeLa cells incubated for 48 hrs by MTT assay
Cytotoxic activity against human HeLa cells incubated for 48 hrs by MTT assay
[PMID: 28587825]
HeLa IC50
3.42 μM
Compound: B, triterpene quinine methide
Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 23395966]
HepG2 IC50
0.78 μM
Compound: 1
Cytotoxic activity against human HepG2 cells incubated for 48 hrs by MTT assay
Cytotoxic activity against human HepG2 cells incubated for 48 hrs by MTT assay
[PMID: 28587825]
HL-60 IC50
0.2 μM
Compound: 23
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
[PMID: 21090801]
HT-29 IC50
4600 ng/mL
Compound: 6
Cytotoxicity against human HT-29 cells after 72 hrs by Alamar blue assay
Cytotoxicity against human HT-29 cells after 72 hrs by Alamar blue assay
[PMID: 9644053]
KB ED50
0.1 μg/mL
Compound: 7
Cytotoxicity against human KB cells after 3 days by SRB assay
Cytotoxicity against human KB cells after 3 days by SRB assay
[PMID: 14640511]
KB IC50
0.55 μg/mL
Compound: 5
Cytotoxicity against human KB cells by MTT assay
Cytotoxicity against human KB cells by MTT assay
[PMID: 7714534]
KB IC50
0.9 μM
Compound: 1a
Antiproliferative activity against human KB cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
Antiproliferative activity against human KB cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
[PMID: 34170694]
L1210 IC50
0.36 μg/mL
Compound: 5
Cytotoxicity against mouse L1210 cells by MTT assay
Cytotoxicity against mouse L1210 cells by MTT assay
[PMID: 7714534]
MCF7 ED50
0.14 μg/mL
Compound: 7
Cytotoxicity against human MCF7 cells after 3 days by SRB assay
Cytotoxicity against human MCF7 cells after 3 days by SRB assay
[PMID: 14640511]
MCF7 IC50
0.4 μM
Compound: 23
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay
[PMID: 21090801]
MCF7 IC50
0.87 μM
Compound: B, triterpene quinine methide
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 23395966]
MCF7 IC50
0.9 μM
Compound: 1a
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
[PMID: 34170694]
MCF7 IC50
1.57 μM
Compound: CEL01
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 27647369]
MDA-MB-231 IC50
0.8 μM
Compound: 1a
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 48 hrs by MTT assay
[PMID: 34170694]
P388 IC50
0.12 μg/mL
Compound: 5
Cytotoxicity against mouse P388 cells by MTT assay
Cytotoxicity against mouse P388 cells by MTT assay
[PMID: 7714534]
PANC-1 IC50
1.49 μM
Compound: CEL01
Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay
Antiproliferative activity against human PANC1 cells assessed as reduction in cell viability after 48 hrs by MTT assay
[PMID: 27647369]
PC-3 ED50
0.23 μg/mL
Compound: 7
Cytotoxicity against human PC3 cells after 3 days by SRB assay
Cytotoxicity against human PC3 cells after 3 days by SRB assay
[PMID: 14640511]
SGC-7901 IC50
0.63 μM
Compound: 1
Cytotoxic activity against human SGC7901 cells incubated for 48 hrs by MTT assay
Cytotoxic activity against human SGC7901 cells incubated for 48 hrs by MTT assay
[PMID: 28587825]
SW982 IC50
1.28 μM
Compound: B, triterpene quinine methide
Cytotoxicity against human SW982 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human SW982 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 23395966]
T cell line IC50
1202 nM
Compound: 1a
Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay
Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay
[PMID: 32822186]
T cell line CC50
2.4 μM
Compound: 1a
Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay
Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay
[PMID: 32822186]
U-87MG ATCC ED50
0.17 μg/mL
Compound: 7
Cytotoxicity against human U87MG cells after 3 days by SRB assay
Cytotoxicity against human U87MG cells after 3 days by SRB assay
[PMID: 14640511]
体外研究
(In Vitro)

Pristimerin 抑制纯化 MGL 的活性，IC50 为 93±8 nM，未纯化 MGL (MGL 转染的 HeLa 细胞的细胞裂解物) 的 IC50 > 398±68 nM。Pristimerin 通过一种快速、可逆和非竞争性的机制抑制 MGL。与调节性半胱氨酸 (可能是 Cys208[1]) 形成极性相互作用可能会加强 pristimerin 与 MGL 的结合。Pristimerin 以剂量和时间依赖性方式抑制 HFLS-RA 和 HUVEC 细胞活力。Pristimerin 降低 VEGF 诱导的 VEGFR2 自磷酸化并减弱 VEGF 诱导的 VEGFR2 介导的信号通路的激活[2]。

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

Pristimerin 相关抗体:
体内研究
(In Vivo)

Pristimerin 抑制炎症和肿瘤血管生成。Pristimerin 显著降低发炎关节滑膜组织中的血管密度，并降低血清中促血管生成因子的表达，包括 TNF-α、Ang-1 和 MMP-9[2]。

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

464.64

Formula

C30H40O4
CAS 号
性状

固体

颜色

Orange to reddish brown

中文名称

扁蒴藤素
结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验： 

DMF 中的溶解度 : 25 mg/mL (53.81 mM; 超声助溶)

DMSO 中的溶解度 : 20 mg/mL (43.04 mM; 超声助溶; 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 2.1522 mL 10.7610 mL 21.5220 mL
5 mM 0.4304 mL 2.1522 mL 4.3044 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 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

动物实验：

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 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，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制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

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (4.30 mM); 澄清溶液

    此方案可获得 ≥ 2 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.22%

COA (291 KB) LCMS (95 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

HFLS-RA (5 × 103 cells/mL) or HUVECs (1 × 104 cells/well) are seeded in 96-well plates and cultured in normal growth medium for 24 h. The cells are then incubated with different Pristimerin concentrations (0, 0.125, 0.25, 0.5 μM). The effects of Pristimerin on HUVECs viability are determined under VEGF-induced conditions. Cell viability is quantified by MTT assay. At 4 h before the end of the culture period, 30 μL of MTT solution (5.0 mg/mL) is added to each well. Cells without Pristimerin or VEGF served as a vehicle control[2].

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

Rat: Pristimerin is dissolved in DMSO (0.4%) and intraperitoneally injected daily into Male Sprague-Dawley rats in the experimental group (low-dose group, 0.40 mg/kg of body weight; high-dose group, 0.80 mg/kg of body weight) from day 11 to day 24 of immunization. The model group received vehicle (DMSO, 0.4%), and the normal control group received normal saline (NS). Methotrexate (positive control) is suspended in NS and orally administered in the autoimmune phase at an interval of 5 days[2].

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

Pristimerin 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / DMF 1 mM 2.1522 mL 10.7610 mL 21.5220 mL 53.8051 mL
5 mM 0.4304 mL 2.1522 mL 4.3044 mL 10.7610 mL
10 mM 0.2152 mL 1.0761 mL 2.1522 mL 5.3805 mL
15 mM 0.1435 mL 0.7174 mL 1.4348 mL 3.5870 mL
20 mM 0.1076 mL 0.5381 mL 1.0761 mL 2.6903 mL
25 mM 0.0861 mL 0.4304 mL 0.8609 mL 2.1522 mL
30 mM 0.0717 mL 0.3587 mL 0.7174 mL 1.7935 mL
40 mM 0.0538 mL 0.2690 mL 0.5381 mL 1.3451 mL
DMF 50 mM 0.0430 mL 0.2152 mL 0.4304 mL 1.0761 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:

Pristimerin1258-84-0Celastrol methyl ester扁蒴藤素BacterialInhibitorinhibitorinhibit

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