Forskolin-Coleonol-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEForskolinCat. No.: HY-15371CAS No.: 66575-29-9Synonyms: Coleonol; Colforsin分式: CHO分量: 410.5作靶点: Adenylate Cyclase; Autophagy作通路: GPCR/G Protein; Autophagy储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数

2、据体外实验 DMSO : 100 mg/mL (243.61 mM; Need ultrasonic)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.09 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.09 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Forskolin

3、种有效的 腺苷酸环化酶 激活剂，结合到 I 型腺苷酸环化酶 IC50 为 41 nM，激活 I 型腺苷酸环化酶 EC50 为 0.5 M。IC50 & Target IC50: 41 nM (Adenylyl cyclase) 1EC50: 0.5 M (Adenylyl cyclase) 1体外研究 Forskolin (Fsk) is a naturally occurring diterpene isolated from Coleus forskholii, directly activates adenylylcyclase (AC) through its catalytic su

4、bunit to increase intracellular levels of cyclic adenosine monophosphate(cAMP) 1. Forskolin (Fsk) affects the proliferation of the human T-cell lines such as Kit 225 and MT-2.Forskolin treatment inhibits the proliferation of both Kit 225 and MT-2 cells in a dose-dependent manner withan IC50 equal to

5、 5 M Fsk. Forskolin treatment (10-100 M) increases cAMPi levels 5- to 20-fold abovebasal levels, which reache maximum levels between 50-100 M Forskolin 2.体内研究 The Forskolin (Fsk)-treated Mrp4-/- mice shows an increased number of Ki67-positive and cleaved caspase3-positive ECs, a significant decrease

6、 in the amount of pericyte coverage, and a reduced number of emptysleeves. In pups exposed to hyperoxia (75% oxygen) from P7 to P12, the Mrp4-/- mice shows a significantincrease in the unvascularized retinal area 3. The average blood glucose in the healthy rat group is102.121.94 mg/dL, 101.253.56 fo

7、r control group and 1032.08 in forskolin group. The data shows thatglucose levels at the end of the study are lower in forskolin group, with a significant difference according tothe statistical tests applied (p=0.03) 4.PROTOCOLCell Assay 2 Quiescent Kit 225 or MT-2 cells are seeded into 96-well plat

8、es at 5104 cells per well. Cells are thenpretreated for 1 h with 1% DMSO (vehicle) or Forskolin at 1, 5, 10, 25, 50, and 100 Mconcentrations. Thecells are stimulated with IL-2 and cultured for an additional 20 h at 37C. Control cells are treated with 1%DMSO for 20 h. During the final 4 h of incubati

9、on, the cells are pulsed with 3Hthymidine at a concentrationof 0.5 Ci/200 L. Cells are harvested onto fiberglass filters and analyzed using liquid scintillation counting2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 34 C57

10、BL/6J mice are used. Mrp4-knockout mice, which are established and repeatedly backcrossed to theC57BL/6J mice. Forskolin is injected intraperitoneally into neonatal mice at postnatal days 4 (P4) and 5 (P5).Mice injected with DMSO serve as the controls. The treated mice are euthanized at P6, and thei

11、r retinas areisolated for whole-mount immunohistochemistry (IHC). The effect of different concentrations of Forskolin onthe survival rate and retinal vasculature is first tested, and the optimal concentration is determined, 1.0 g/50L (0.3 mg/kg) at P4 and 1.5 g/50 L (0.5 mg/kg) at P5, used to compar

12、e the retinal vascular phenotypesbetween WT mice and Mrp4-deficient mice.Rats 42/3 Master of Small Molecules 您边的抑制剂师www.MedChemEMale Wistar rats, aged 10-14 weeks old, with a mean weight of 300 g50 g, are divided into four groups; 19are experimentally induced to develop diabetes, and 8 are maintaine

13、d in a healthy condition. Both diabeticand healthy rats receive no Forskolin (control), or 6 mg/kg per day of Forskolin, administered orally for 8weeks. Blood glucose levels are determined in each group before and after Forskolin treatment. The diabeticrats are tested two weeks after confirming the

14、presence of diabetes (three weeks after the induction) andafter eight weeks of the designated treatment.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Biomaterials. 2018 Dec 6;193:30-46. Br J Pharmacol. 2019 Aug;176(16):2962-2976. Int J Bio

15、l Macromol. 2018 Oct 1;117:42-50. J Lipid Res. 2018 Feb;59(2):330-338. ACS Chem Neurosci. 2018 Dec 19;9(12):3175-3185.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Robbins JD, et al. Forskolin carbamates: binding and activation studies with type I adenylyl cyclase. J Med Chem

16、. 1996 Jul5;39(14):2745-52.2. Rodriguez G, et al. Forskolin-inducible cAMP pathway negatively regulates T-cell proliferation by uncoupling the interleukin-2 receptorcomplex. J Biol Chem. 2013 Mar 8;288(10):7137-46.3. Matsumiya W, et al. Forskolin modifies retinal vascular development in Mrp4-knockout mice. Invest Ophthalmol Vis Sci. 2012 Dec7;53(13):8029-35.4. Ros-Silva M, et al. Effect of chronic administration of forskolin on glycemia and oxidative stress in rats with and without experimenta