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Forskolin

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Catalog No.
B1421
腺苷酸环化酶激活剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 550.00
现货
25mg
¥ 700.00
现货
50mg
¥ 1,050.00
现货
100mg
¥ 1,500.00
现货

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Background

Forskolin is a cell-permeable activator of adenylyl cyclase [1].

Adenylate cyclase is an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to 3',5'-cyclic AMP (cAMP) and pyrophosphate.

Forskolin is a cell-permeable activator of adenylyl cyclase. In rat cerebral cortical membranes, forskolin reversibly and rapidly activated adenylate cyclase with EC50 value of 5-10 μM. GTP and GDP increased the responses to forskolin. In rat cerebral cortical slices, forskolin rapidly increased cAMP by 35-fold with IC50 values of 25 μM [1]. Forskolin inhibited the inactivation of adenylate cyclases induced by N-ethylmaleimide with Kd values of 7.6 and 6.3 μM for the platelet and brain adenylate cyclases, respectively. Also, forskolin protected adenylate cyclases against thermal inactivation. Forskolin activated the platelet adenylate cyclase with IC50 and Kd values of 3-10 μM and 9-11 μM, respectively [2]. In pig epidermal cells, forskolin activated epidermal adenylate cyclase with Ka value of 2-3×10-5 M and induced cAMP accumulations, which then inhibited mitotic in a dose-dependent way [3].

References:
[1].  Seamon KB, Padgett W, Daly JW. Forskolin: unique diterpene activator of adenylate cyclase in membranes and in intact cells. Proc Natl Acad Sci U S A, 1981, 78(6): 3363-3367.
[2].  Awad JA, Johnson RA, Jakobs KH, et al. Interactions of forskolin and adenylate cyclase. Effects on substrate kinetics and protection against inactivation by heat and N-ethylmaleimide. J Biol Chem, 1983, 258(5): 2960-2965.
[3].  Takeda J, Adachi K, Halprin KM, et al. Forskolin activates adenylate cyclase activity and inhibits mitosis in in vitro in pig epidermis. J Invest Dermatol, 1983, 81(3): 236-240.

文献引用

1. Zhang H, Wen JJ, et al. "Forskolin reduces fat accumulation in Nile tilapia (Oreochromis niloticus) through stimulating lipolysis and beta-oxidation." Comp Biochem Physiol A Mol Integr Physiol. 2018 Dec 26;230:7-15. PMID:30593869
2. Morel JD, Paatero AO, et al. "Proteomics reveals scope of mycolactone-mediated Sec61 blockade and distinctive stress signature." Mol Cell Proteomics. 2018 Jun 18. pii: mcp.RA118.000824. PMID:29915147

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt410.5
Cas No.66575-29-9
FormulaC22H34O7
Solubility≥20.525mg/mL in DMSO
Chemical Name[(3R,4aR,5S,6S,6aS,10S,10aR,10bS)-3-ethenyl-6,10,10b-trihydroxy-3,4a,7,7,10a-pentamethyl-1-oxo-5,6,6a,8,9,10-hexahydro-2H-benzo[f]chromen-5-yl] acetate
SDFDownload SDF
Canonical SMILESCC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议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。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1, 2]:

细胞系

人源间充质干细胞

溶解方法

该化合物在DMSO中的溶解度> 10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应时间

0.075-0.2 mM 处理4天或7天; 或10μM

应用

使用不同浓度Forskolin处理人源间充质干细胞4天,抑制其增殖;同时,Forskolin以浓度相关的方式促进人源间充质干细胞表达碱性磷酸酶;除此之外,Forskolin (10 μM)显著地刺激大鼠下丘脑-垂体神经系统释放血管加压素和催产素。

动物实验 [1]:

动物模型

颗粒物植入雄性裸鼠皮下口袋模型

剂量

0.10 或0.15mM Forskolin

应用

Forskolin(0.10 mM)在体内促进人源间充质干细胞的骨形成。

注意事项

请于室内测试所有化合物的溶解度。实际溶解度和理论值可能略有不同,这是由实验系统的误差引起的,属于正常现象。

References:

1. Doorn, J., Siddappa, R., van Blitterswijk, C. A. and de Boer, J. (2012) Forskolin enhances in vivo bone formation by human mesenchymal stromal cells. Tissue Eng Part A. 18, 558-567

2. Roszczyk, M. and Juszczak, M. (2014) Forskolin-stimulated vasopressin and oxytocin release from the rat hypothalamo-neurohypophysial system in vitro is inhibited by melatonin. Endokrynol Pol. 65, 125-131

质量控制

化学结构

Forskolin

相关生物数据

Forskolin

相关生物数据

Forskolin