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Triptonide (Synonyms: 雷公藤内酯酮; NSC 165677; PG 492)
目录号: PC14804 纯度: ≥98%
CAS No. :38647-11-9
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中文名称
Triptonide
中文别名
雷公藤内酯酮;雷藤酮;★雷公藤内酯酮;雷公藤内酯酮(P);雷公藤内酯酮(标准品);雷公藤内酯酮(雷藤酮 );雷公藤内酯酮,Triptonide,植物提取物,标准品,对照品;雷公藤内酯酮(雷藤酮 ,雷公藤羰内酯);雷公藤内酯酮,雷藤酮;雷公藤羰内酯
英文名称
Triptonide
英文别名
Triptonide;(3bS,4aS,5aS,6aS,7aS,7bS,8aS,8bS)-6a-Isopropyl-8b-methyl-3b,4,4a,7a,7b,8b,9,10-octahydrotrisoxireno[4b,5:6,7:8a,9]phenanthro[1,2-c]furan-1,6(3H,6aH)-dione;TRIPTONIDE(P) PrintBack;14-Deoxy-14-oxotriptolide;l-triptonide;NSC 165677;PG 492;Triptolide,14-deoxy-14-oxo;14-deoxy-14-oxo-triptolide;(-)-triptonide;Spectrum_001724;SpecPlus_000568;Spectrum2_000477;Spectrum5_001806;KBioSS_002204;DivK1c_006664;SPBio_000614;Triptonide, >=98% (HPLC);KBio2_007340;KBio2_004772;KBio2_002204;KBio1_001608;BCP26007;NSC165677;NCI60_001273;AB0035809;ST24050308;N2;s9416;Y0208;N2407
Cas No.
38647-11-9
分子式
C20H22O6
分子量
358.39
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
生物活性

Triptonide (NSC 165677) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC50 of appropriately 0.3?nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects.

性状

Solid

IC50 & Target[1][2]

IC50: 0.3?nM (Wnt)

体外研究(In Vitro)

Triptonide blocks Wnt/β-catenin signaling via C-terminal transactivation domain of β-catenin, and promots apoptosis in Wnt-dependent cancer cells.
Triptonide potently inhibits the proliferation of human B-lymphoma Raji and T-lymphoma Jurkat cells with IC50 of 5.7 nM and 4.8 nM, respectively.
Triptonide (2.5-10 nM; 6 days) significantly suppresses B-lymphoma cell colony-forming capability.
Triptonide (20 nM; 3 days) promotes apoptosis through activation of PARP and caspase 3, but reduction of BCL2 protein levels in the lymphoma cells.
Triptonide (5-10 nM; 72 hours) markedly reduces both total and phosphorylated Lyn proteins, and diminishes Lyn downstream ERK and ATK signal pathways.

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

Cell Proliferation Assay

Cell Line: B-lymphoma Raji cells, T-lymphoma Jurkat cells
Concentration: 0-80 nM
Incubation Time: 3 days, 6 days
Result: Inhibited lymphoma cell tumorigenic capability in a dose-dependent manner.

Apoptosis Analysis

Cell Line: Raji cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 3 days
Result: Did not significantly induce apoptosis at the effective tumor growth-inhibitory (2.5-10 nM); moderately induced lymphoma cell apoptosis (20 nM).

Western Blot Analysis

Cell Line: Raji cells
Concentration: 5 nM, 10 nM, 20 nM
Incubation Time: 3 days
Result: Did not vigorously activated pro-apoptotic proteins PARP and caspase 3 in lymphoma cells (5-10 nM); significantly activated PARP and caspase 3 (20 nM); significantly reduced anti-apoptotic BCL2 levels.

RT-PCR

Cell Line: Raji cells
Concentration: 5 nM, 10 nM
Incubation Time: 72 hours
Result: Significantly diminished Lyn mRNA levels in the lymphoma cells.
体内研究(In Vivo)

Triptonide (5 mg/kg; i.p.; daily; for 34 days) exerts a strong anti-lymphoma effect in mice.

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

Animal Model: Eight-week-old female NOD/SCID mice (18-22 g), with 3 x 10 Raji cells xenograft
Dosage: 5 mg/kg
Administration: Intraperitoneal injection, daily, for 34 days
Result: Potently inhibited lymphoma cell growth and tumorigenic capability.
运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
结构分类
来源
参考文献
溶解度数据
体外研究: 

DMSO : 100 mg/mL (279.03 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.7903 mL 13.9513 mL 27.9026 mL
5 mM 0.5581 mL 2.7903 mL 5.5805 mL
10 mM 0.2790 mL 1.3951 mL 2.7903 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.98 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (6.98 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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