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Cyclopamine

Cyclopamine

产品编号 T2825   CAS 4449-51-8
别名: 环巴胺, 11-Deoxojervine

Cyclopamine (11-Deoxojervine) 是Hedgehog 通路的拮抗剂,细胞实验中IC50=46 nM。它还是选择性Smo 抑制剂。

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Cyclopamine Chemical Structure
Cyclopamine, CAS 4449-51-8
规格 价格/CNY 货期 数量
5 mg ¥ 484 现货
10 mg ¥ 753 现货
25 mg ¥ 1,380 现货
50 mg ¥ 2,263 现货
100 mg ¥ 3,598 现货
1 mL * 10 mM (in DMSO) ¥ 548 现货
产品目录号及名称: Cyclopamine (T2825)
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选择批次  
纯度: 99.66%
纯度: 98.55%
纯度: 98.31%
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天然产物信息
生物活性
化学信息
存储 & 溶解度
TCMIP信息
参考文献
结构类型
产品描述 Cyclopamine (11-Deoxojervine), a Smoothened (Smo) antagonist (IC50: 46 nM in TM3Hh12 cells), belongs to the group of steroidal jerveratrum alkaloids.
靶点活性 Smoothened:46 nM (TM3Hh12 cells)
体外活性 The Chicken embryos Exposure to cyclopamine resulted in visible external defects, including cyclopia, microphthalmia, proboscis formation, amelia, thoracic lordosis, and decreased body size [2]. cyclopamine treatment reduced the growth of tumor cell lines from the oesophagus, stomach, biliary tract and pancreas by 75–95% compared with tomatidine controls [3]. In pancreatic cancer cell lines, Hh inhibition with cyclopamine resulted in down-regulation of snail and up-regulation of E-cadherin, consistent with inhibition of epithelial-to-mesenchymal transition, and was mirrored by a striking reduction of in vitro invasive capacity (P < 0.0001) [4].
体内活性 To examine the effects of cyclopamine treatment in vivo, subcutaneous xenografts from HUCCT1 cells, a metastatic cholangiocarcinoma cell line, were established in athymic mice. Tumours in cyclopamine-treated animals regressed completely by 12 days [3]. In the delayed treatment model, no difference in weight was noted between control and cyclopamine (1.2 mg) treated BxPC3-SMOlow tumours. By contrast, a 50–60% decrease in tumour mass was observed in Panc 05.04- and L3.6sl-derived tumours, respectively (Fig. 5b, c)—an even more marked effect was noted in the concurrent treatment model, which revealed an 84% reduction in tumour mass of L3.6sl-derived tumours [5].
激酶实验 This assay measures the end stage of the Hh signaling pathway, that is, the transcriptional modulation of Gli, using Luciferase as readout (Gli-Luc assay). Cyclopamine is prepared for assay by serial dilution in DMSO and then added to empty assay plates. TM3Hh12 cells (TM3 cells containing Hh-responsive reporter gene construct pTA-8xGli-Luc) are resuspended in F12 Ham's/DMEM (1:1) containing 5% FBS and 15 mM Hepes pH 7.3, added to assay plates and incubated with Cyclopamine for approximately 30 minutes at 37 °C in 5% CO2. 1 nM Hh-Ag 1.5 is then added to assay plates and incubated at 37 °C in the presence of 5% CO2. After 48 hours, either Bright-Glo or MTS reagent is added to the assay plates and luminescence or absorbance at 492 nm is determined. IC50 value, defined as the inflection point of the logistic curve, is determined by non-linear regression of the Gli-driven luciferase luminescence or absorbance signal from MTS assay vs log10 (concentration) of Cyclopamine using the R statistical software pack [1].
细胞实验 Cells were cultured in triplicate in 96-well plates in assay media to which 5E1 monoclonal antibody, ShhNp and/or cyclopamine were added at 0 h at concentrations indicated in the main text. Viable cell mass was determined by optical density measurements at 490 nm (OD490) at 2 and 4 days using the CellTiter96 colorimetric assay. Relative growth was calculated as OD (day 4) 2 OD (day 2)/OD (day 2) [3].
动物实验 A total of 0.1 ml Hanks' balanced salt solution and matrigel (1:1) containing 2 × 10^6 cells were injected subcutaneously into CD-1 nude mice. Tumours were grown for 4 days to a minimum volume of 125 mm3; treatment was initiated simultaneously for all subjects. Mice were injected subcutaneously with vector alone (triolein:ethanol 4:1 v/v) or a cyclopamine suspension (1.2 mg per mouse in triolein: ethanol 4:1 v/v) daily for 7 days. At the end of the treatment period, tumours were excised from mice, weighed and then fixed for 3 h at 4 °C with 4% paraformaldehyde, embedded in paraffin wax and sectioned (6 μm). Apoptotic cells were identified by TUNEL using recombinant Tdt as previously described29. Sections were then counterstained with eosin. Eight ×20-magnified fields from regions corresponding to the exterior, middle and interior of two control and two cyclopamine-treated tumours were chosen at random [5].
别名 环巴胺, 11-Deoxojervine
分子量 411.62
分子式 C27H41NO2
CAS No. 4449-51-8

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 4.12 mg/mL (10 mM), Sonification is recommended

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4294 mL 12.1471 mL 24.2943 mL 60.7356 mL
5 mM 0.4859 mL 2.4294 mL 4.8589 mL 12.1471 mL
10 mM 0.2429 mL 1.2147 mL 2.4294 mL 6.0736 mL
TCMIP相关数据
中药材来源及性味归经
所属中成药
所属中药方剂

中药材来源及性味归经

中药材名称 中药材拉丁名 归经
白藜芦 Veratrum nigrum L. 苦, 辛 肺, 胃, 肝
杜仲叶 Eucommia ulmoides Oliv. 微辛 肝, 肾
藜芦 Veratrum nigrum L., Veratrum schindleri Loes.f., Veratrum maackii Regel, Veratrum dahuricum(Turcz.)Loes.f.及Veratrum grandiflorum(Maxim.)Loes.f. 辛, 苦 肝, 肺, 胃

所属中成药

中成药名称 处方组成 主治疾病 中成药类型
首乌强身片 制何首乌,墨旱莲,杜仲叶,豨莶草,牛膝,桑叶,女贞子,桑椹,金樱子,覆盆子 口服,一次3片。 补益药
杜仲颗粒 杜仲,杜仲叶 开水冲服,一次1袋,一日2次。 扶正药
绍兴大补酒 党参,山药,白术,熟地黄,川芎,杜仲叶,茯苓,当归,炙黄芪,玉竹,白芍,炙甘草 口服,一次15~30毫升,一日2次。 补益药
益寿强身膏 党参,人参,茯苓,炙黄芪,白术,山药,制何首乌,当归,熟地黄,川芎,泽泻,牡丹皮,牛膝,白芍,杜仲叶,续断,阿胶,红花,三七,炙甘草,黄精,陈皮 口服,一次15g,一日2次。 补益药
杜仲双降袋泡剂 杜仲叶,苦丁茶 开水泡服,一次1袋,一日2~3次。 清热药
骨刺片 昆布,骨碎补,党参,桂枝,威灵仙,牡蛎,杜仲叶,鸡血藤,附子,制川乌,制草乌,延胡索,白芍,三七,马钱子 N/A N/A
长春益寿膏 天冬,麦冬,熟地黄,山药,牛膝,地黄,杜仲叶,制何首乌,茯苓,人参,木香,柏子仁,五味子,狗脊,花椒,泽泻,石菖蒲,远志,菟丝子,金樱子,枸杞子,覆盆子,地骨皮 开水冲服,一次30克,一日2次,早晚各1次。 补益药
神州跌打丸 红茴香,大血藤,山橿根,蛇葡萄,刘寄奴,紫金牛,络石藤,制川乌,制草乌,地耳草,一支黄花,半边莲,南藤,牛尾菜,藜芦,山药 口服,小蜜丸一次9g,大蜜丸一次2丸,一日2~3次。 祛风药
强力定眩片 天麻,杜仲,野菊花,杜仲叶,川芎 口服,一次4~6片,一日3次。 祛风药
腰痛片 杜仲叶,补骨脂,续断,当归,白术,牛膝,肉桂,乳香,狗脊,赤芍,泽泻,土鳖虫 N/A 和血药
益寿大补酒 党参,茯苓,白芍,续断,当归,三七,杜仲叶,制何首乌,红花,黄芪,牛膝,山药,牡丹皮,泽泻,白术,熟地黄,人参 口服,一次20~30ml,一日1~2次。 补益药
杜仲冲剂 杜仲,杜仲叶 N/A 补益药
强力定眩胶囊 天麻,杜仲,野菊花,杜仲叶,川芎 口服。一次4~6粒,一日3次。 扶正药
杜仲平压片 杜仲叶 一次2片,一日2~3次,或遵医嘱。 补益药
骨刺胶囊 昆布,骨碎补,党参,桂枝,威灵仙,牡蛎(煅),杜仲叶,鸡血藤,附片,制川乌,制草乌,延胡索(制),白芍,三七,马钱子粉 口服,一次3粒,一日3次,或遵医嘱。 补肾壮骨药
杜仲平压分散片 杜仲叶 吞服,或用水分散后口服。一次2片,一日2~3次。 扶正药
杜仲绞股蓝口服液 杜仲叶,菟丝子,淫羊,胶股蓝 口服,一日2~3次,一次10毫升。 扶正药
腰痛丸 杜仲叶,补骨脂,狗脊,续断,当归,赤芍,白术,牛膝,泽泻,肉桂,乳香,土鳖虫 用盐开水送服,一次9g,一日2次。 和血药
杜仲平压胶囊 杜仲叶 口服,一次2粒,一日2~3次。 扶正药
妇宝颗粒 地黄,忍冬藤,续断,杜仲叶,麦冬,莲房,川楝子,白芍,延胡索,甘草,侧柏叶,大血藤 用开水冲服,每袋10克规格:一次20克,一日2次;每袋5克规格:一次10克,一日2次。 清热药

所属中药方剂

方剂名称 处方组成 剂型 处方来源
龙骨散54 黄柏,藜芦,石膏,铜绿,白矾,麝香,龙骨 散剂 《济阳纲目》卷一○七。
白矾丸6 白矾,羊踯躅,细辛,半夏,藜芦,朱砂,巴豆,苦参,雄黄,大黄,芒硝,大戟,川乌,狼毒 丸剂 《圣惠》卷五十四。
生姜丸2 生姜,半夏,附子,藜芦 丸剂 《普济方》卷二一二。
太一散1 川芎,石膏,藜芦,甘草 散剂 《普济方》卷四十五。
巴豆丸1 巴豆,杏仁,藜芦,皂荚,桔梗 丸剂 《圣惠》卷四十八。
木香汤18 木香,沉香,鳖甲,升麻,熏陆香,藜芦,雄黄,吴茱萸,甘草 汤剂 《圣济总录》卷一三五。
瓜蒂牙消散 藜芦,瓜蒂,芒硝,脑,麝 散剂 《伤寒总病论》卷六。
二圣散15 常山,葱白,藜芦 散剂 《济阳纲目》卷一。
白矾煮散 白矾,防风,细辛,附子,干姜,白术,甘草,蛇床子,藜芦,椒 散剂 《圣济总录》卷一七二。
夺命散3 蜈蚣,瓜蒂,藜芦,葱白 散剂 《普济方》卷三七四引《保生集》。
太一流金大道散 羊踯躅,桂枝,干姜,附子,细辛,朱砂,皂角,藜芦,牡丹皮 散剂 《幼幼新书》卷十三引《灵苑》。
四神散9 地龙,蟾蜍,藜芦,冰片 散剂 《圣济总录》卷十六。
天麻散1 藜芦,天麻,狼毒,白芷,草,钓苓根,草乌,贯众,细辛,雄黄,轻粉 散剂 《外科精义》卷下。
白矾汤 白矾,干姜,藜芦,蛇床子,甘草,细辛,防风,川椒 汤剂 《圣济总录》卷一二○。
白蔹散4 白蔹,白矾,远志,雄黄,藜芦,麝香,白芷 散剂 《魏氏家藏方》卷九。
生姜丸3 生姜,藜芦,乌头,肉桂,黄连,云实,代赭石 丸剂 《普济方》卷二一三。
太上五蛊丸 雄黄,花椒,巴豆,莽草,芫花,朱砂,鬼臼,白矾,藜芦,斑蝥,蜈蚣,獭肝,附子 丸剂 《千金》卷二十四。
二神散1 常山,葱白,藜芦 散剂 《丹溪心法附余》卷二十四。
夺命散8 蜈蚣,瓜蒂,藜芦 散剂 《幼幼新书》卷八引毛彬方。
太乙备急散 雄黄,桂心,芫花,朱砂,川椒,藜芦,巴豆,野葛,附子 散剂 《千金》卷十七。

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Peukert S, et al. Identification and structure-activity relationships of ortho-biphenyl carboxamides as potent Smoothened antagonists inhibiting the Hedgehog signaling pathway. Bioorg Med Chem Lett. 2009 Jan 15;19(2):328-31. 2. Kim SK, et al. Pancreas development is promoted by cyclopamine, a hedgehog signaling inhibitor. Proc Natl Acad Sci U S A. 1998 Oct 27;95(22):13036-41. 3. Berman DM, et al. Widespread requirement for Hedgehog ligand stimulation in growth of digestive tract tumours. Nature. 2003 Oct 23;425(6960):846-51. 4. Feldmann G, et al. Blockade of hedgehog signaling inhibits pancreatic cancer invasion and metastases: a new paradigm for combination therapy in solid cancers. Cancer Res. 2007 Mar 1;67(5):2187-96. 5. Thayer SP, et al. Hedgehog is an early and late mediator of pancreatic cancer tumorigenesis. Nature. 2003 Oct 23;425(6960):851-6. 6. Ma W, et al. Reduced Smoothened level rescued Aβ-induced memory deficits and neuronal inflammation in animal models of Alzheimer's disease. J Genet Genomics. 2018 May 20;45(5):237-246. 7. Zheng H T, Fu T, Zhang H Y, et al. Progesterone-regulated Hsd11b2 as a barrier to balance mouse uterine corticosterone[J]. Journal of Endocrinology. 2020, 244(1): 177-187.

文献引用

1. Zheng H T, Fu T, Zhang H Y, et al. Progesterone-regulated Hsd11b2 as a barrier to balance mouse uterine corticosterone. Journal of Endocrinology. 2020, 244(1): 177-187 2. Li B, Yan Y P, He Y Y, et al.IHH, SHH, and primary cilia mediate epithelial-stromal cross-talk during decidualization in mice.Science Signaling.2023, 16(774): eadd0645. 3. Zhang Y, Wu T, Wang Y, et al.Reciprocal FGF19-GLI2 signaling induces epithelial-to-mesenchymal transition to promote lung squamous cell carcinoma metastasis.Cellular Oncology.2023: 1-14.
20(S)-Hydroxycholesterol LEQ506 Purmorphamine Jervine MRT-83 Glasdegib JNJ-1289 HhAntag

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 Wnt/Hedgehog/Notch 通路化合物库 蒙药化合物库 经典已知活性库 抗前列腺癌化合物库 生物碱类天然产物库 中药单体化合物库 NO PAINS 化合物库 抗癌天然产物库 细胞重编程化合物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
% Tween 80
% ddH2O
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技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Cyclopamine 4449-51-8 GPCR/G Protein Metabolism Stem Cells Endogenous Metabolite Hedgehog/Smoothened Smo 环巴胺 Hedgehog Smoothened 11-Deoxojervine inhibit Inhibitor inhibitor

 

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