IBMX-3-Isobutyl-1-methylxanthine-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIBMXCat. No.: HY-12318CAS No.: 28822-58-4Synonyms: 3-Isobutyl-1-methylxanthine; Isobutylmethylxanthine分式: CHNO分量: 222.24作靶点: Phosphodiesterase (PDE)作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C

2、6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (449.96 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.4996 mL 22.4982 mL 44.9964 mL5 mM 0.8999 mL 4.4996 mL 8.9993 mL10 mM 0.4500 mL 2.2498 mL 4.4996 mL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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请

3、先配制澄的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (11.25 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (11.25 mM); Clear solution3. 请依

4、序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (11.25 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 IBMX种谱的磷酸酯酶 (PDE) 抑制剂，抑制 PDE3，PDE4 和 PDE5，IC50 分别为 6.5，26.3 和 31.7 M。IC50 & Target IC50: 6.51.2 M(PDE3), 26.33.9 M (PDE4), 31.75.3 M (PDE5) 1体外研究 At 1

5、00 M, KMUP-1 (a xanthine derivative) and IBMX are the most effective at inducing tracheal relaxation;the magnitude of the relaxation responses induced by KMUP-1 and IBMX are not significantly different 1.IBMX (100 M) activates renal outer medullary K+ (ROMK) channels (n=6, P+ (HK)-fed rats with IBMX

6、 (100M) for 20 min leads to a significant increase in tubular cAMP content to 1.430.35 pg/mm tubule length(n=14) compare with that measured in vehicle-treated controls (0.610.13 pg/mm tubule length, n=12, P 2.体内研究 IBMX, a non-selective PDE inhibitor significantly decreases the liver glycogen storage

7、 (mg/g, IBMX 221.5P0.05) also mc2 does not change plasma glucose (control=1413 and mc2=1455). IBMX has the highestefficacy on increasing plasma glucose 3. Treatments with IBMX and Apocynin significantly decrease cold-induced elevation of right ventricular (RV) systolic pressure (23.51.8 and 24.20.6

8、mmHg, respectively)although they do not decrease RV pressure to the warm control levels. IBMX or Apocynin significantlyreduces medial layer thickness (19.00.9, and 16.90.8 m, respectively) and increases lumen diameter(62.74.2, and 59.54.3 m, respectively) of small PAs in cold-exposed rats 4.PROTOCOL

9、Cell Assay 2 Cells are grown in 24-well plates 105 cells per well. At confluence, monolayer cells are washed withphosphate buffer solution (PBS) and then incubated with KMUP-1 (0.1-100 M) in the presence of 100 MIBMX for 20 min. Incubation is terminated by the addition of 10% trichloroacetic acid (T

10、CA). Cell suspensionsare sonicated and then centrifuged at 2500 g for 15 min at 4C. To remove TCA, the supernatants areextracted three times with 5 volumes of water-saturated diethyl ether. Then, the supernatants are lyophilizedand the cyclic GMP or AMP of each sample is determined by using commerci

11、ally availableradioimmunoassay kits 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 34 Male mice (25-35 g) are used. For the experiment, the test compound (IBMX, milrinone, MCPIP, mc1, mc2,mc5 or mc6) or solvent (control) i

12、s injected subcutaneously to mice at 1 mg/kg dosage twice a day (8:00 a.m.and 8:00 p.m.) for 7 days. On day 8, animals are anesthetized with intraperitoneal injection of thiopental (80mg/kg) and blood samples are obtained from their hearts and then the liver is dissected. Each sample iscentrifuged f

13、or 5 min and its serum is separated. The serum and the liver of each animal are kept frozen inless than -18 oC for the following measurements.Rats 42/3 Master of Small Molecules 您边的抑制剂师www.MedChemESix groups of male Sprague-Dawley rats are used (150-180g, 6 rats/group). Three groups of rats areexpos

14、ed to a climate-controlled walk-in chamber maintained at moderate cold (5.01C). The remaininggroups are kept in an identical chamber maintained at room temperature (23.51C, warm) and served ascontrols. After eight weeks of exposure to cold, 3 groups in each temperature condition received continuousI

15、V infusion of IBMX (PDE-1 inhibitor, 8.5 mg/kg/day), Apocynin (NADPH oxidase inhibitor, 25 mg/kg/day) andvehicle (DMSO, 50%), respectively. The doses of drugs have been validated for effective inhibition of PDE-1and NADPH oxidase activity, respectively. Body weight is measured weekly. After one week

16、 of drug infusion,the animals right ventricular systolic blood pressure (RVBP) is measured under anesthesia. The RVP is areliable indicator of pulmonary arterial blood pressure (PAP) and has been used by numerous investigatorsfor evaluating PH.MCE has not independently confirmed the accuracy of thes

17、e methods. They are for reference only. Carbohydr Polym. 2019 Apr 1;209:363-371. Free Radic Biol Med. 2018 Jun;121:215-230. J Cell Biochem. 2019 Jan;120(1):321-331. Patent. US20180263995A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Wu BN, et al. KMUP-1, a xanthine derivati

18、ve, induces relaxation of guinea-pig isolated trachea: the role of the epithelium, cyclicnucleotides and K+ channels. Br J Pharmacol. 2004 Aug;142(7):1105-142. Wei Y, et al. Angiotensin II type 2 receptor regulates ROMK-like K+ channel activity in the renal cortical collecting duct during highdietary K+ adaptat