Forskolin
(Synonyms: 毛喉素; Coleonol; Colforsin) 目录号 : GC11920
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 的 IC50 为 41 nM。
Cas No.:66575-29-9
Sample solution is provided at 25 µL, 10mM.
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].
References:
[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]。
| Cell experiment [1]: | |
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Cell lines |
PC cells |
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Preparation Method |
Cells were treated with Forskolin in FBS supplemented medium without exosomes and harvested at indicated times for subsequent analysis |
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Reaction Conditions |
10 uM Forskolin, 72 hours |
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Applications |
Forskolin is also a potent exosome biogenesis and/or secretion activator in prostate cancer (PC) cells. |
| Animal experiment [2]: | |
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Animal models |
Male Wistar rats, aged 10-14 weeks old, with a mean weight of 300 g ± 50 g |
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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. |
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Dosage form |
6 mg/kg per day of forskolin for 8 weeks |
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Applications |
Forskolin predominantly decreased basal glucose in healthy rats and attenuated the severity of hyperglycemia in diabetic rats. |
|
References: [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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| Cas No. | 66575-29-9 | SDF | |
| 别名 | 毛喉素; Coleonol; Colforsin | ||
| 化学名 | [(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 | ||
| Canonical SMILES | CC(=O)OC1C(C2C(CCC(C2(C3(C1(OC(CC3=O)(C)C=C)C)O)C)O)(C)C)O | ||
| 分子式 | C22H34O7 | 分子量 | 410.5 |
| 溶解度 | ≥ 20.525mg/mL in DMSO | 储存条件 | -20°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4361 mL | 12.1803 mL | 24.3605 mL |
| 5 mM | 0.4872 mL | 2.4361 mL | 4.8721 mL |
| 10 mM | 0.2436 mL | 1.218 mL | 2.4361 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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