Isoprenaline hydrochloride

SKU: orb1309921

Description

Isoprenaline hydrochloride (NCI-c55630) is a potent β-adrenergic receptor agonist. It is widely used in research to study cardiac stimulation, bronchodilation, and peripheral vasodilation in both in vitro and in vivo experimental models.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	51-30-9
MW	247.719
Purity	99.65%
Formula	C₁₁H₁₈ClNO₃
SMILES	Cl.CC(C)NCC(O)c1ccc(O)c(O)c1
Target	Endogenous Metabolite,PDE,Adrenergic Receptor,PI3K
Solubility	DMSO:250 mg/mL (1009.21 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (20.18 mM);H2O:50 mg/mL (201.84 mM)

Bioactivity

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Target IC50	CLL cells:2.6 μM\|β-adrenoceptor:0.08 μM\|CML cells:5.6 μM\|AML cells:8.6 μM\|ALL cells:12.4 μM
In Vivo	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. Read more...
In Vitro	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 . 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) . 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 . Read more...
Cell Research	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 . Read more...

Storage & Handling

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Storage	store at low temperature \| Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Beta Receptor, bronchodilator, cAMP PDE, cardiac stimulating activities, Adrenergic Receptor, AdrenergicReceptor, NCI-c55630, Isoprenaline, Isoprenaline HCl, Isoprenaline Hydrochloride, Isoprenaline hydrochloride, Isoproterenol, Isoproterenol hydrochloride, Isoproterenol Hydrochloride, inhibit, Inhibitor, EndogenousMetabolite, Endogenous Metabolite, PI3K, peripheral vasodilator

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Compound Identifiers

PubChem CID

5807 ↗

Key Properties

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No computed properties available.

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