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Forskolin

Forskolin

产品编号 T2939   CAS 66575-29-9
别名: 毛喉素, Coleonol, Colforsin

Forskolin (Coleonol) 是从毛喉鞘蕊花中提取的一种天然产物,是腺苷酸环化酶激活剂,可以增加 cAMP 水平。它诱导多种细胞类型的分化并激活孕烷 X 受体和FXR,也可诱导细胞自噬。它对心脏产生正性肌力作用,具有血小板抗凝集和降压作用。

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Forskolin Chemical Structure
Forskolin, CAS 66575-29-9
规格 价格/CNY 货期 数量
1 mg ¥ 218 现货
5 mg ¥ 496 现货
10 mg ¥ 672 现货
25 mg ¥ 972 现货
50 mg ¥ 1,230 现货
100 mg ¥ 1,960 现货
200 mg ¥ 3,160 现货
500 mg ¥ 4,970 现货
1 mL * 10 mM (in DMSO) ¥ 547 现货
产品目录号及名称: Forskolin (T2939)
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天然产物信息
生物活性
化学信息
存储 & 溶解度
参考文献
结构类型
产品描述 Forskolin (Coleonol), a potent activator of the adenylate cyclase (EC50: 0.5 μM), can increase the cAMP level. It is extracted from the plant Coleus forskohlii.
靶点活性 Adenylyl cyclase:0.5 μM (cell free)
体外活性 Forskolin (Fsk) treatment inhibited the proliferation of both Kit 225 and MT-2 cells in a dose-dependent manner with an IC50 equal to ~5 μM Forskolin. Fsk treatment (10–100 μM) increased cAMPi levels ~5- to 20-fold above basal levels, which reached maximum levels between 50–100 μM Fsk [2]. Forskolin binds to adenylyl cyclase in membranes from stably transfected Sf9 cells expressing type 1 adenylyl cyclase with an IC50 value of 41 nM and demonstrates an EC50 value of 0.5 μM in an activation assay assessing formation of cAMP from ATP [1]. 'VC6T' [VPA, CHIR99021 (CHIR), 616452, Tranylcypromine] plus Forskolin (VC6TF) induced some GFP-positive clusters expressing E-cadherin [3].
体内活性 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. In pups exposed to hyperoxia (75% oxygen) from P7 to P12, the Mrp4(-/-) mice showed a significant increase in the unvascularized retinal area [4]. Hepatic fibrosis induced by CCl4 was significantly reduced by forskolin, as indicated by decreased α-SMA expression and collagen deposition. Forskolin co-treatment significantly attenuated oxidative stress and inflammation, reduced TGF-β1 levels and down-regulated mRNA expression of Ptch-1, Smo and Gli-2 through cAMP-dependent PKA activation [5].
激酶实验 For Jak3 kinase assays, Fsk-treated MT-2 cells were lysed, clarified, and immunoprecipitated using Jak3 antibody as described above. Kinase reactions were carried out as described previously at 30 °C for 20 min. For PKA kinase assays, untreated MT-2 cells were lysed, and Jak3 was immunoprecipitated and bound to PAS beads as described previously. Immunoprecipitated Jak3 was washed with kinase buffer (50 mM Hepes-NaOH (pH 7.4), 10 mM MgCl2, 0.5 mM EGTA, 0.5 mM DTT, 20 μg/ml aprotinin, 10 μg/ml leupeptin, 1 μg/ml pepstatin A) and incubated with 200 μM ATP and purified protein kinase A catalytic subunit (PKAc) as indicated in the figure legends. Kinase reactions were carried out at 32 °C for 30 min followed by vigorous washing of the beads with cold kinase wash buffer as described previously. For [γ-32P]ATP radiolabeled kinase assays using recombinant Jak3, Hek293 cells were transfected with wild type (WT) Jak3 or kinase-dead Jak3 K855A using Lipofectamine 2000 according to the manufacturer's instructions. Cells were lysed and immunoprecipitated with Jak3 antibody. Jak3-bound PAS beads were washed three times in cold lysis buffer followed by kinase buffer. Kinase reactions were initiated by adding 10 μCi [γ-32P]ATP, 10 μm unlabeled ATP, and 1 μg of purified PKAc to Jak3-bound PAS bead reaction mixtures. Kinase reactions were performed at 32 °C for 30 min. Jak3-bound PAS beads were washed three times in radioimmunoassay buffer (10 mM Tris-HCl, pH 7.4, 75 mM NaCl, 20 mM EDTA, 10 mM EGTA, 20 mM Na4P2O7, 50 mM NaF, 20 mM 2-glycerolphosphate, 1 mM p-nitrophenyl phosphate, 0.1% Triton X-100) and one time in kinase wash buffer. The reactions were stopped by adding 2× SDS-PAGE sample buffer followed by SDS-PAGE. Coomassie stainable Jak3 bands were excised from the PVDF membrane and subjected to phosphoamino acid analysis [2].
细胞实验 Kit 225 or MT-2 cells were treated with 1, 5, 10, 20, 50, or 100 μM Forskolin for 20 min at 37 °C. Cells were lysed and clarified by centrifugation, and the concentration of cAMP was detected by direct cAMP ELISA. Optical density was measured at 405 nm, and the concentration of intracellular cAMP was calculated using a weighted four parameter logistic curve according to the manufactures instructions [2].
动物实验 Forskolin was dissolved in dimethyl sulfoxide (DMSO) and injected intraperitoneally into neonatal mice at postnatal days 4 (P4) and 5 (P5). Mice injected with DMSO served as the controls. The treated mice were euthanized at P6, and their retinas were isolated for whole-mount immunohistochemistry (IHC). We first tested the effect of different concentrations of forskolin on the survival rate and retinal vasculature and determined the optimal concentration, 1.0 μg/50 μL (0.3 mg/kg) at P4 and 1.5 μg/50 μL (0.5 mg/kg) at P5, used to compare the retinal vascular phenotypes between WT mice and Mrp4-deficient mice [4]. . After acclimatization for 2 weeks, animals were randomly divided into four groups of eight rats each and treated for six consecutive weeks as follows: The first group was treated with CCl4 (50% CCl4/corn oil; 0.5 mL·kg?1, i.p.) twice a week to induce liver fibrosis. The second group was given forskolin only at a dose of 10 mg·kg?1, i.p., dissolved in a DMSO/saline solution (1:49) five times a week. The third group was given both CCl4 and forskolin. The dose of forskolin used here was based on the results of our preliminary study. The fourth group served as the normal control, receiving vehicles only. At 24 h after the last injection, blood samples were collected from the retro‐orbital plexus after light anesthesia with sodium pentobarbital (50 mg·kg?1, i.p.). Serum was separated by centrifugation at 3000× g for 10 min and was used for the assessment of liver functions. Rats were killed by cervical dislocation, and livers were removed and weighed. A portion of liver tissue was washed and homogenized to obtain a 20% (w·v?1) homogenate, which was used for assessment of oxidative stress, inflammatory and fibrogenic markers. Another portion was placed in formalin for immunohistochemical and histopathological analyses. The remainder was stored at ?80°C, together with the 20% homogenate, until needed [5].
别名 毛喉素, Coleonol, Colforsin
化合物与蛋白结合的复合物

T2939_1

RAT TYPE II ADENYLYL CYCLASE C2 DOMAIN/FORSKOLIN COMPLEX

分子量 410.5
分子式 C22H34O7
CAS No. 66575-29-9

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

H2O: Insoluble

DMSO: 30 mg/mL (73 mM)

Ethanol: 15 mg/mL (36.5 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.4361 mL 12.1803 mL 24.3605 mL 60.9013 mL
5 mM 0.4872 mL 2.4361 mL 4.8721 mL 12.1803 mL
10 mM 0.2436 mL 1.218 mL 2.4361 mL 6.0901 mL
20 mM 0.1218 mL 0.609 mL 1.218 mL 3.0451 mL
DMSO 50 mM 0.0487 mL 0.2436 mL 0.4872 mL 1.218 mL

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参考文献

1. Robbins JD, et al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J Med Chem. 1996 Jul 5;39(14):2745-52. 2. Rodriguez G, et al. Forskolin-inducible cAMP pathway negatively regulates T-cell proliferation by uncoupling the interleukin-2 receptor complex. J Biol Chem. 2013 Mar 8;288(10):7137-46. 3. Hou P, et al. Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds. Science. 2013 Aug 9;341(6146):651-4. 4. Matsumiya W, et al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec 7;53(13):8029-35. 5. El-Agroudy NN, et al. Forskolin, a hedgehog signalling inhibitor, attenuates carbon tetrachloride-induced liver fibrosis in rats. Br J Pharmacol. 2016 Nov;173(22):3248-3260. 6. Lu J, Dou F, Yu Z. The potassium channel KCa3. 1 represents a valid pharmacological target for microgliosis-induced neuronal impairment in a mouse model of Parkinson’s disease[J]. Journal of Neuroinflammation. 2019, 16(1): 1-14. 7. Lin J Y, Cheng J, Du Y Q, et al. In vitro expansion of pancreatic islet clusters facilitated by hormones and chemicals[J]. Cell Discovery. 2020, 6(1): 1-12. 8. Lin J Y, Cheng J, Du Y Q, et al. In vitro pancreatic islet cluster expansion facilitated by hormones and chemicals[J]. Cell Discovery. 2020, 6(1): 1-12. 9. Wu L, Dong A, Dong L, et al. PARIS, an optogenetic method for functionally mapping gap junctions[J]. eLife. 2019 Jan 14;8. pii: e43366. 10. Xiaoli F, Yaqing Z, Ruhui L, et al. Graphene oxide disrupted mitochondrial homeostasis through inducing intracellular redox deviation and autophagy-lysosomal network dysfunction in SH-SY5Y cells[J]. Journal of Hazardous Materials. 2021: 126158.

文献引用

1. Li J, Bai Y, Liu Y, et al.Transcriptome-based chemical screens identify CDK8 as a common barrier in multiple cell reprogramming systems.Cell Reports.2023, 42(6). 2. Han L, Song B, Zhang P, et al.PC3T: a signature-driven predictor of chemical compounds for cellular transition.Communications Biology.2023, 6(1): 989. 3. Chen S, Zhou X, Li W, et al.Development of a novel peptide targeting GPR81 to suppress adipocyte-mediated tumor progression.Biochemical Pharmacology.2023: 115800. 4. Ma X, Lu Y, Zhou Z, Human expandable pancreatic progenitor–derived β cells ameliorate diabetes. Science Advances. 2022, 8(8): eabk1826. 5. Fu J, Jiang L, Yu B, et al. Generation of a Human iPSC Line CIBi010-A with a Reporter for ASGR1 Using CRISPR/Cas9. Stem Cell Research. 2022: 102800 6. Zhao C, Sun C, Yuan J, et al. Hericium caput-medusae (Bull.: Fr.) Pers. fermentation concentrate polysaccharides improves intestinal bacteria by activating chloride channels and mucus secretion. Journal of Ethnopharmacology. 2022: 115721. 7. Xiaoli F, Yaqing Z, Ruhui L, et al. Graphene oxide disrupted mitochondrial homeostasis through inducing intracellular redox deviation and autophagy-lysosomal network dysfunction in SH-SY5Y cells. Journal of Hazardous Materials. 2021: 126158. 8. Wu L, Dong A, Dong L, et al. PARIS, an optogenetic method for functionally mapping gap junctions. ELife. 2019 Jan 14;8. pii: e43366 9. Lin J Y, Cheng J, Du Y Q, et al. In vitro pancreatic islet cluster expansion facilitated by hormones and chemicals. Cell Discovery. 2020, 6(1): 1-12 10. Wang W, Ren S, Lu Y, et al. Inhibition of Syk promotes chemical reprogramming of fibroblasts via metabolic rewiring and H2S production. The EMBO Journal. 2021 Jun 1;40(11):e106771. doi: 10.15252/embj.2020106771. Epub 2021 Apr 28.
11. Zhang X, Ke P X, Yuan X, et al. Forskolin Protected against Streptozotocin-Induced Diabetic Cardiomyopathy via Inhibition of Oxidative Stress and Cardiac Fibrosis in Mice. BioMed Research International. 2021, 2021 12. Jin C, Zhao S, Xie H. Forskolin enhanced the osteogenic differentiation of human dental pulp stem cells in vitro and in vivo. Journal of Dental Sciences. 2022 13. Wang H, Liang N, Huang D, et al. The effects of high-density lipoprotein and oxidized high-density lipoprotein on forskolin-induced syncytialization of BeWo cells. Placenta. 2021, 103: 199-205 14. Miao Y, Zhang Y, Qiao S, et al. Oral administration of curcumin ameliorates pulmonary fibrosis in mice through 15d-PGJ2-mediated induction of hepatocyte growth factor in the colon. Acta Pharmacologica Sinica. 2020: 1-14 15. Lin J Y, Cheng J, Du Y Q, et al. In vitro expansion of pancreatic islet clusters facilitated by hormones and chemicals. Cell Discovery. 2020, 6(1): 1-12 16. Hu Z, Lu Y, Cao J, et al.N-acetyltransferase NAT10 controls cell fates via connecting mRNA cytidine acetylation to chromatin signaling.Science Advances.2024, 10(2): eadh9871. 17. Zhao X, Cai X, Zhu H, et al.27-Hydroxycholesterol inhibits trophoblast fusion during placenta development by activating PI3K/AKT/mTOR signaling pathway.Archives of Toxicology.2024: 1-15. 18. Mendonça L S, Henriques D, Fernandes V, et al.Graft-derived neurons and bystander effects are maintained for six months after human iPSC-derived NESC transplantation in mice’s cerebella.Scientific Reports.2024, 14(1): 3236. 19. Dang Q, Zhu Y, Zhang Y, et al.Nuclear Binding Protein 2/Nesfatin-1 Affects Trophoblast Cell Fusion during Placental Development via the EGFR-PLCG1-CAMK4 Pathway.International Journal of Molecular Sciences.2024, 25(3): 1925.
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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 神经递质受体化合物库 抗癌天然产物库 NO PAINS 化合物库 抗代谢疾病化合物库 脂代谢化合物库 核受体化合物库 中药单体化合物库 干细胞分化化合物库 GPCR靶点分子库

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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
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mg/kg
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Keywords

Forskolin 66575-29-9 Autophagy Metabolism Neuroscience FXR Adenylyl cyclase AChR notropic pregnane Inhibitor exosome cancer antihypertensive 毛喉素 antiaggregatory X receptor prostate NR1H4 Adenylate Cyclase PXR Coleonol Colforsin cAMP inhibit inhibitor

 

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