标签归档：guggulsterone

Guggulsterone(Synonyms: 香胶甾酮; Z/E-Guggulsterone)

发表于由

上海金畔生物科技有限公司提供天然产物萜类及其苷类Terpenoids and Glycosides。

Guggulsterone (Synonyms: 香胶甾酮; Z/E-Guggulsterone) 纯度: 99.83%

Guggulsterone 是一种植物甾醇，来自 Commiphora wightii 树的树胶脂。 Guggulsterone 通过下调抗细胞凋亡 (apoptosis) 基因产物 (IAP1，xIAP，Bfl-1/A1，Bcl-2，cFLIP，survivin)，调节细胞周期蛋白 (cyclin D1，c-Myc)，激活 caspases，JNK，抑制 Akt，抑制多种肿瘤细胞的生长并诱导细胞凋亡。Guggulsterone 通过调节几种转录因子介导基因表达，包括 NF-κB，STAT3，C /EBPα，雄激素受体 (androgen receptor) 和糖皮质激素受体(glucocorticoid receptors)。Guggulsterone，一种法尼醇 X 受体 (FXR) 拮抗剂，可降低 CDCA 诱导的 FXR 活化，Z- 和 E-Guggulsterone 的 IC50 分别为 17 和 15 μM。

Guggulsterone(Synonyms: 香胶甾酮; Z/E-Guggulsterone)

Guggulsterone Chemical Structure

CAS No. : 95975-55-6

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥770 In-stock
5 mg ￥700 In-stock
10 mg ￥1300 In-stock
20 mg ￥2100 In-stock
50 mg ￥4000 In-stock
100 mg ￥7000 In-stock
200 mg   询价  
500 mg   询价  

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生物活性

Guggulsterone is a plant sterol derived from the gum resin of the tree Commiphora wightii. Guggulsterone inhibits the growth of a wide variety of tumor cells and induces apoptosis through down regulation of antiapoptotic gene products (IAP1, xIAP, Bfl-1/A1, Bcl-2, cFLIP and survivin), modulation of cell cycle proteins (cyclin D1 and c-Myc), activation of caspases and JNK, inhibition of Akt[1]. Guggulsterone, a farnesoid X receptor (FXR) antagonist, decreases CDCA-induced FXR activation with IC50s of 17 and 15 μM for Z- and E-Guggulsterone, respectively[2].

IC50 & Target[1]

JNK

 

Akt

 

Caspase

 

体外研究
(In Vitro)

Guggulsterone (0.5-20 μM; 24 hours) suppresses TREM-1, TLR4 and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: RAW 264.7 murine macrophage cells
Concentration: 0.5, 5, 10, 20 μM
Incubation Time: 24 hours
Result: Suppressed TREM-1, TLR4, and TNF-α expression as well as the phosphorylation of IκBα and NF-κB p65 by LPS.

体内研究
(In Vivo)

Guggulsterone (orally; 100 mg/kg once per day for 8 days) significantly improved the survival rates of wild-type mice with TNBS-induced colitis[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wild-type mice with TNBS-induced colitis[2]
Dosage: 100 mg/kg
Administration: Orally; once per day; for 8 days
Result: Improved the survival rates of wild-type mice with TNBS-induced colitis.

分子量

312.45

Formula

C21H28O2
CAS 号

95975-55-6
中文名称

香胶甾酮；咕咕草
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
In Vitro: 

DMSO : 20.83 mg/mL (66.67 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2005 mL 16.0026 mL 32.0051 mL
5 mM 0.6401 mL 3.2005 mL 6.4010 mL
10 mM 0.3201 mL 1.6003 mL 3.2005 mL

*

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。

In Vivo:

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

  • 1.

    请依序添加每种溶剂： 50% PEG300    50% saline

    Solubility: 10 mg/mL (32.01 mM); Suspended solution; Need ultrasonic

  • 2.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.66 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 3.

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.66 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 4.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (6.66 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (6.66 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 Shanghai Jinpan Biotech Co Ltd 网站选购。
参考文献

  • [1]. Shishodia S, et al. Guggulsterone for Chemoprevention of Cancer. Curr Pharm Des. 2016;22(3):294-306.

    [2]. Che X, et al. Protective effects of guggulsterone against colitis are associated with the suppression of TREM-1 and modulation of macrophages. Am J Physiol Gastrointest Liver Physiol. 2018 Jul 1;315(1):G128-G139.