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  • Forskolin
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Forskolin

A tool for increasing cAMP formation

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¥637-1412
价格
510-1130
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  • 货号: ajci8082
  • CAS: 66575-29-9
  • 别名: 毛喉素; Coleonol; Colforsin
  • 分子式: C22H34O7
  • 分子量: 410.5
  • 纯度: >98%
  • 溶解度: ≥ 20.525mg/mL in DMSO
  • 储存: -20°C, protect from light
  • 库存: 现货

Background

Forskolin is a potent adenylyl cyclase activator with IC50 of 41 nM for type I adenylyl cyclase [1]. Forskolin, with EC50 of 0.5 μM, is also an inducer of intracellular cAMP formation [2] Forskolin induces the differentiation of a variety of cells, activates progesterone X receptor (PXR) and FXR[3] Forskolin has contractile effects on the heart, and has anti-platelet aggregation and antihypertensive effectsForskolin also induces autophagy [4][5].


Forskolin (Coleonol) is also a potent exosome biogenesis and/or secretion activator in prostate cancer (PC) cells[7]. Modulation of free radical stress in human red blood cell membrane by forskolin and the prospects for treatment of cardiovascular disease and Diabetes[8].The increase in cAMP by forskolin attenuated cytotoxicity and apoptosis.


In vivo studies,forskolin predominantly decreased basal glucose in healthy rats and attenuated the severity of hyperglycemia in diabetic rats[6]. The Mrp4(-/-) mice exhibited no overt abnormalities in the development of the retinal vasculature, but retinal vascular development in the Mrp4(-/-) mice was suppressed in response to forskolin administration.The forskolin-treated Mrp4(-/-) mice showed an increased number of Ki67-positive and cleaved caspase 3-positive ECs, a significant decrease in the amount of pericyte coverage, and a reduced number of empty sleeves[2].

参考文献:
[1]: Robbins JD, Boring DL, et,al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J Med Chem. 1996 Jul 5;39(14):2745-52. doi: 10.1021/jm960191+. PMID: 8709105.
[2]: Matsumiya W, Kusuhara S, et,al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec 7;53(13):8029-35. doi: 10.1167/iovs.12-10781. PMID: 23154460; PMCID: PMC3517270.
[3]: Mayati A, Moreau A, et,al. Functional polarization of human hepatoma HepaRG cells in response to forskolin. Sci Rep. 2018 Oct 31;8(1):16115. doi: 10.1038/s41598-018-34421-8. PMID: 30382126; PMCID: PMC6208432.
[4]: Awad JA, Johnson RA, 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 Mar 10;258(5):2960-5. PMID: 6681815.
[5]: Seamon KB, Daly JW, et,al. Structure-activity relationships for activation of adenylate cyclase by the diterpene forskolin and its derivatives. J Med Chem. 1983 Mar;26(3):436-9. doi: 10.1021/jm00357a021. PMID: 6681845.
[6]: Ríos-Silva M, Trujillo X, et,al. Effect of chronic administration of forskolin on glycemia and oxidative stress in rats with and without experimental diabetes. Int J Med Sci. 2014 Mar 11;11(5):448-52. doi: 10.7150/ijms.8034. PMID: 24688307; PMCID: PMC3970096.
[7]: Datta A, Kim H, et,al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. doi: 10.1038/s41598-018-26411-7. PMID: 29802284; PMCID: PMC5970137.
[8]:Niaz MA, Singh RB. Modulation of free radical stress in human red blood cell membrane by forskolin and the prospects for treatment of cardiovascular disease and diabetes. Cell Mol Biol (Noisy-le-grand). 1999 Dec;45(8):1203-7. PMID: 10643969.


Forskolin 是一种有效的腺苷酸环化酶激活剂,对 I 型腺苷酸环化酶 [1] 的 IC50 为 41 nM。 Forskolin,EC50 为 0.5 μM,也是细胞内 cAMP 形成的诱导剂 [2] Forskolin 诱导多种细胞分化,激活黄体酮 X 受体 (PXR) 和 FXR[3] Forskolin 具有对心脏有收缩作用,并具有抗血小板聚集和降压作用毛喉素还诱导自噬[4][5]


毛喉素 (Coleonol) 也是前列腺癌 (PC) 细胞中有效的外泌体生物发生和/或分泌激活剂[7]。毛喉素对人红细胞膜自由基应激的调控及其治疗心血管疾病和糖尿病的前景[8]。毛喉素通过增加cAMP减弱细胞毒性和细胞凋亡。


体内研究表明,毛喉素主要降低健康大鼠的基础葡萄糖,并减轻糖尿病大鼠的高血糖症的严重程度[6]。 Mrp4(-/-) 小鼠在视网膜血管发育方面没有表现出明显的异常,但 Mrp4(-/-) 小鼠的视网膜血管发育在毛喉素给药后受到抑制。经毛喉素处理的 Mrp4(-/- ) 小鼠显示 Ki67 阳性和裂解半胱天冬酶 3 阳性 EC 数量增加,周细胞覆盖量显着减少,空袖数量减少[2]

Protocol

Cell experiment [1]:

Cell lines

PC cells

Preparation Method

Cells were treated with Forskolin in FBS supplemented medium without exosomes and harvested at indicated times for subsequent analysis

Reaction Conditions

10 uM Forskolin, 72 hours

Applications

Forskolin is also a potent exosome biogenesis and/or secretion activator in prostate cancer (PC) cells.

Animal experiment [2]:

Animal models

Male Wistar rats, aged 10-14 weeks old, with a mean weight of 300 g ± 50 g

Preparation Method

Forskolin (10 mg capsules) was administered orally for 8 weeks by catheter. The administered doses 6 mg/kg per day was equivalent to the 1 mg/kg per day in humans doses. Forskolin was diluted in plain water to 60 mg/100.

Dosage form

6 mg/kg per day of forskolin for 8 weeks

Applications

Forskolin predominantly decreased basal glucose in healthy rats and attenuated the severity of hyperglycemia in diabetic rats.

参考文献:

[1]. Datta A, Kim H,et,al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161. doi: 10.1038/s41598-018-26411-7. PMID: 29802284; PMCID: PMC5970137.


[2]. Ríos-Silva M, Trujillo X, et,al. Effect of chronic administration of forskolin on glycemia and oxidative stress in rats with and without experimental diabetes. Int J Med Sci. 2014 Mar 11;11(5):448-52. doi: 10.7150/ijms.8034. PMID: 24688307; PMCID: PMC3970096.

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