Isoprenaline hydrochloride NEW
| Price | $33 |
| Package | 1g |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-16 |
Product Details
| Product Name: Isoprenaline hydrochloride | CAS No.: 51-30-9 |
| Purity: 98% | Supply Ability: 10g |
| Release date: 2024/11/16 |
Product Introduction
Bioactivity
| 名稱 | Isoprenaline hydrochloride |
| 描述 | Isoprenaline hydrochloride (NCI-c55630) is a potent beta-adrenergic agonist with the peripheral vasodilator, bronchodilator, and cardiac stimulating properties. |
| 細(xì)胞實驗 | Cells are seeded in 24-well culture dishes at a density of 2 to 5×10^4 cells per well. Experiments are performed after 3 to 5 days in culture when cells has reached confluence. Culture medium is aspirated and replaced by 0.5 mL of PBS containing the pharmacological agents. Treatments are performed in quadruplicate at 37°C. The type 3, 4 and 5 PDE inhibitors cilostamide (10 gM), rolipram (10 pM) and DMPPO (10 gM), respectively, are incubated with cells for 30 min before addition of adenylate or guanylate cyclase activators. Cyclic GMP and cyclic AMP are respectively increased in RASMC by stimulation of particulate guanylate cyclase with ANF (50 nM for 10 min) or fl-adrenoceptors with isoprenaline (5 nm for 5 min). At the end of the incubation period, the medium is removed and intracellular cyclic nucleotides are extracted by two ethanolic (65%) ishes at 4°C for 5 min. Ethanolic extracts are pooled, evaporated to dryness by a Speed-Vac system. The dried extract is dissolved in a suitable amount of assay buffer and cyclic nucleotide levels are measured by scintillation proximity assay [3]. |
| 體外活性 | Incubation of intact rat fat cells with isoprenaline (300 nM, 3 min) increased particulate cGMP- and cilostamide-inhibited, low-Km cAMP phosphodiesterase (cAMP-PDE) activity by about 50% and 100%, respectively [1]. Relaxation induced by isoprenaline was also potentiated by the cyclic GMP-inhibited PDE (PDE 3) inhibitor cilostamide (100 nM). Isoprenaline (5 nM and 10 microM) increased cyclic AMP levels and this effect was potentiated by cilostamide (10 microM), by rolipram, a cyclic AMP-specific PDE (PDE 4) inhibitor (10 microM) and by cyclic GMP-elevating agents (50 nM ANF or 30 nM SNP plus 100 nM DMPPO) [2]. Isoprenaline increased the phosphorylation levels of Akt, and the downstream FoxO1, FoxO3a, and CREB. When catecholamine binding to β-adrenoceptors, the G protein–coupled receptor kinase-2 (GRK2) mediates the translocation of PI3K to β-adrenoceptors and then enhances the recruitment of β-arrestin and AP-2, which finally results in the internalization and downregulation of β-adrenoceptors. It has reported that disrupts the interaction between PI3K and GRK2 by displacing class I PI3K isoforms blocks agonist-stimulated β-adrenoceptors internalization [3]. |
| 體內(nèi)活性 | METHODS: To induce a model of pathological cardiac remodeling, Isoprenaline hydrochloride (1.5 mg/kg in NaCl 0.9%) was injected subcutaneously into C57BL/6 mice once a day for ten days. RESULTS: Cardiac structural abnormalities (increased IVSTd and LVPWd), impaired cardiac function (EF and CO), and elevated heart weight/body weight ratios (HW/BW) were seen in Isoprenaline-administered mice. [3] |
| 存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | H2O : 201.8 mM DMSO : 60 mg/mL (242.21 mM) |
| 關(guān)鍵字 | peripheral vasodilator | Isoprenaline | Beta Receptor | cardiac stimulating activities | Inhibitor | Isoproterenol | Isoprenaline Hydrochloride | inhibit | Adrenergic Receptor | Isoprenaline hydrochloride | bronchodilator | Endogenous Metabolite | Isoproterenol Hydrochloride |
| 相關(guān)產(chǎn)品 | Sucrose | Daidzein | Guanidine hydrochloride | Fumaric acid | Ferulic Acid | Formamide | Oleamide | Glycerol | Thymidine | Naringin |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 神經(jīng)退行性疾病化合物庫 | 膜蛋白靶向化合物庫 | 激酶抑制劑庫 | 藥物功能重定位化合物庫 | FDA 上市藥物庫 | 抗癌上市藥物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | GPCR靶點分子庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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