盐酸异丙肾上腺素 T1056

Product Introduction
Bioactivity


英文名: Isoprenaline hydrochloride

描述: Isoprenaline hydrochloride (NCI-c55630) 是非选择性的β-肾上腺素能受体激动剂，有支气管扩张剂，外周血管扩张剂和心脏刺激活性。

细胞实验: 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].

体外活性: 用 Isoprenaline （300 nM，3 分钟）诱导完整的大鼠脂肪细胞，可使微粒 cGMP 和西洛他胺抑制的低 Km cAMP 磷酸二酯酶（cAMP-PDE）活性分别提高约 50%和 100%[1]。环 GMP PDE（PDE 3）抑制剂西洛他胺（100 nM）可增强 Isoprenaline 诱导的松弛。 Isoprenaline （5 nM 和 10 microM）可增加环 AMP 水平，西洛他胺（10 microM）、环 AMP PDE（PDE 4）抑制剂罗利普仑（10 microM）和环 GMP 诱导剂（50 nM ANF 或 30 nM SNP 加 100 nM DMPPO）可增强这种效应[2]。 Isoprenaline 增加了 Akt 以及下游 FoxO1、FoxO3a 和 CREB 的磷酸化水平。当儿茶酚胺与β肾上腺素受体结合时，G蛋白偶联受体激酶-2（GRK2）介导PI3K向β肾上腺素受体转位，然后增强β-arrestin和AP-2的招募，最终导致β肾上腺素受体的内化和下调。有报道称，通过置换 I 类 PI3K 同工酶来破坏 PI3K 和 GRK2 之间的相互作用可阻止激动剂刺激的 β 肾上腺素受体内化 [3]。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: H2O : 201.8 mM
DMSO : 60 mg/mL (242.21 mM)


关键字: peripheral vasodilator | Isoprenaline | Beta Receptor | cardiac stimulating activities | Inhibitor | Isoproterenol | Isoprenaline Hydrochloride | inhibit | Adrenergic Receptor | Isoprenaline hydrochloride | bronchodilator | Endogenous Metabolite | Isoproterenol Hydrochloride

相关产品: PI3Kdelta inhibitor 1 | BQR-695 | δ-Tocotrienol | Umbralisib | PI3K-IN-10 | PI3K/Akt/mTOR-IN-2 | YM-201636 | Autophinib | Apilimod | Taselisib

相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Breast Cancer Compound Library | FDA-Approved Kinase Inhibitor Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | Kinase Inhibitor Library | GPCR Compound Library | Anti-Cancer Approved Drug Library

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