盐酸异丙肾上腺素作用机制 - Medchemexpress - MCE中国

1、Product Data SheetIsoprenaline hydrochlorideCat. No.: HY-B0468CAS No.: 51-30-9分式: CHClNO分量: 247.72作靶点: Adrenergic Receptor; Endogenous Metabolite作通路: GPCR/G Protein; Neuronal Signaling; Metabolic Enzyme/Protease储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from lig

2、ht)溶解性数据体外实验 DMSO : 80 mg/mL (322.95 mM; Need ultrasonic)H2O : 50 mg/mL (201.84 mM)* means soluble, but saturation unknown.SolventMass1 mg 5 mg 10 mgConcentration制备储备液1 mM 4.0368 mL 20.1841 mL 40.3682 mL5 mM 0.8074 mL 4.0368 mL 8.0736 mL10 mM 0.4037 mL 2.0184 mL 4.0368 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；

3、旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。BIOLOGICAL ACTIVITY物活性 Isoprenaline hydrochloride脏刺激活性。种选择性的-肾上腺素能受体激动剂，具有有效的外周 管扩张剂，管扩张剂和IC & Target Human Endogenous Metabolite体外研究Isoprenaline (300 nM, 3 min) increases part

4、iculate cGMP- and cilostamide-inhibited, low-Km cAMP phosphodiesterase(cAMP-PDE) activity by about 100% in intact rat fat cells1. Isoprenaline inhibits insulin-stimulated glucose transportactivity in rat adipocytes. Isoprenaline, in the absence of adenosine, promotes a time-dependent (t1/2 approxima

5、tely2 min) decrease in the accessibility of insulin-stimulated cell surface GLUT4 of 50%, which directly correlated withthe observed inhibition of transport activity2. Isoprenaline (5 nM and 10 mM) increases cyclic AMP levels and thiseffect is potentiated by cilostamide (10 mM), by rolipram, a cycli

6、c AMP-specific PDE (PDE 4) inhibitor (10 mM) and bycyclic GMP-elevating agents (50 nM ANF or 30 nM SNP plus 100 nM DMPPO)3. Isoprenaline increases thePage 1 of 2 www.MedChemEtranscriptional activity of Gi alpha-2 gene to 140% of the control value, whereas gene specific hybridization for Gsalpha rema

7、ins unchanged4. Isoprenaline (20 nM) increases the amplitude of total iK and causes a negative shift ofapproximately 10 mV in the activation curve for iK, both in the absence and in the presence of 300 nM nisoldipine toblock the L-type Ca2+ current. Isoprenaline (20 nM) increases the spontaneous pac

8、emaker rate of sino-atrial nodepacemaker cells by 16% in rabbit isolated pacemaker cells5.PROTOCOLCell Assay 3 Cells are seeded in 24-well culture dishes at a density of 2 to 5104 cells per well. Experiments are performed after 3to 5 days in culture when cells has reached confluence. Culture medium

9、is aspirated and replaced by 0.5 mL of PBScontaining the pharmacological agents. Treatments are performed in quadruplicate at 37C. The type 3, 4 and 5 PDEinhibitors cilostamide (10 gM), rolipram (10 pM) and DMPPO (10 gM), respectively, are incubated with cells for 30 minbefore addition of adenylate

10、or guanylate cyclase activators. Cyclic GMP and cyclic AMP are respectively increased inRASMC by stimulation of particulate guanylate cyclase with ANF (50 nM for 10 min) or fl-adrenoceptors withisoprenaline (5 nm for 5 min). At the end of the incubation period, the medium is removed and intracellula

11、r cyclicnucleotides are extracted by two ethanolic (65%) ishes at 4C for 5 min. Ethanolic extracts are pooled, evaporated todryness by a Speed-Vac system. The dried extract is dissolved in a suitable amount of assay buffer and cyclicnucleotide levels are measured by scintillation proximity assay.MCE

12、 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 Circulation. 2018 Jun 5;137(23):2497-2513. Cell Rep. 2019 Dec 3;29(10):2929-2935.e4 J Exp Clin Cancer Res. 2019 Apr 25;38(1):174. Food Funct. 2018 Nov 14;9(11):5528-5535. J Funct Foods. 2020 Feb.S

13、ee more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Degerman E, et al. Evidence that insulin and isoprenaline activate the cGMP-inhibited low-Km cAMP phosphodiesterase in rat fat cells byphosphorylation. Proc Natl Acad Sci U S A. 1990 Jan;87(2):533-72. Vannucci SJ, et al.

14、 Cell surface accessibility of GLUT4 glucose transporters in insulin-stimulated rat adipose cells. Modulation by isoprenaline andadenosine. Biochem J. 1992 Nov 15;288 (Pt 1):325-30.3. Delpy E, et al. Effects of cyclic GMP elevation on isoprenaline-induced increase in cyclic AMP and relaxation in rat

15、 aortic smooth muscle: role ofphosphodiesterase 3. Br J Pharmacol. 1996 Oct;119(3):471-8.4. Muller FU, et al. Isoprenaline stimulates gene transcription of the inhibitory G protein alpha-subunit Gi alpha-2 in rat heart. Circ Res. 1993 Mar;72(3):696-700.5. Lei M, et al. Modulation of delayed rectifier potassium current, iK, by isoprenaline in rabbit isolated pacemaker cells. Exp Physiol. 2000 Jan;85(1):27-35.McePdfHeightPa