| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg |
| ln Vitro |
For three minutes, isoproterenol hemisulfate (300 nM) boosts the activity of low-Km cAMP phosphodiesterase (cAMP-PDE) in intact rat adipocytes by roughly 100% and increases granular cGMP [1]. In rat adipocytes, insulin-stimulated glucose transport activity is inhibited by isoproterenol. Isoproterenol, in the absence of adenosine, promotes a time-dependent (t1/2 ~2 min) >50% decrease in GLUT4 accessibility on the surface of insulin-stimulated cells, which is directly correlated with the observed suppression of transport activity [2]. Cyclic AMP levels are raised by isoproterenol (5 nM and 10 μM), cilopamide (10 mM), rolipram, a cyclic GMP elevator, and a cyclic PDE (PDE 4) inhibitor (10 mM). This action can be amplified by 50 nM ANF or 30 nM SNP + 100 nM DMPPO [3]. While Gs α gene-specific hybridization stays unaltered, isoproterenol raises the transcriptional activity of the Gi α-2 gene to 140% of control levels [4]. The iK activation curve shifts negatively by around 10 mV when isoproterenol (20 nM) is added, regardless of whether 300 nM nisoldipine inhibits L-type Ca2+ currents or not [5]. Isoproterenol (20 nM) improved the spontaneous pacing rate of sinoatrial node pacemaker cells in isolated rabbit pacemaker cells by 16% [5].
|
|---|---|
| ln Vivo |
Isoproterenol hemisulfate (oral, 0.27-0. 64 μg/kg) is extensively metabolized in dogs by relatively few reactions [6].
|
| Animal Protocol |
Animal/Disease Models: Dog[1]
Doses: 0.27-0. 64 μg/kg Route of Administration: Oral Experimental Results:Most of the radioactivity is excreted unchanged through the urine, and only one-third of the radioactivity in the urine exists in the form of O-methyl metabolites. It shows that almost all plasma radioactivity is bound to isoprenaline, and this metabolite accounts for more than 80% of urine radioactivity. . Indicates that heart rate returns to baseline values when plasma concentrations are high. |
| References |
[1]. Degerman E, et al. Evidence that insulin and isoprenaline activate the cGMP-inhibited low-Km cAMP phosphodiesterase in rat fat cells by phosphorylation. Proc Natl Acad Sci U S A. 1990 Jan;87(2):533-7.
[2]. Vannucci SJ, et al. Cell surface accessibility of GLUT4 glucose transporters in insulin-stimulated rat adipose cells. Modulation by isoprenaline and adenosine. 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 aortic smooth muscle: role of phosphodiesterase 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. [6]. M E Conolly, et al. Metabolism of isoprenaline in dog and man. Br J Pharmacol |
| Molecular Formula |
C22H36N2O10S
|
|---|---|
| Molecular Weight |
520.59
|
| CAS # |
299-95-6
|
| Related CAS # |
Isoprenaline hydrochloride;51-30-9;Isoprenaline;7683-59-2
|
| SMILES |
S(=O)(=O)(O[H])O[H].O([H])C([H])(C1C([H])=C([H])C(=C(C=1[H])O[H])O[H])C([H])([H])N([H])C([H])(C([H])([H])[H])C([H])([H])[H].O([H])C([H])(C1C([H])=C([H])C(=C(C=1[H])O[H])O[H])C([H])([H])N([H])C([H])(C([H])([H])[H])C([H])([H])[H]
|
| Synonyms |
Norisodrine; dl-Isoproterenol sulfate; Isoproterenol sulfate anhydrous
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9209 mL | 9.6045 mL | 19.2090 mL | |
| 5 mM | 0.3842 mL | 1.9209 mL | 3.8418 mL | |
| 10 mM | 0.1921 mL | 0.9604 mL | 1.9209 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
