Isoprenaline HCl (Isoproterenol HCl)

Alias: NCI-c55630; Isoprenaline hydrochloride; NCIc55630; NCI c55630; Isoproterenol
Cat No.:V1119 Purity: ≥98%
Isoprenaline HCL (NCIc55630; NCI c55630; Isoproterenol), the hydrochloride salt of Isoprenaline, is a non-selective beta-adrenergic receptor agonist that has been used for the treatment of bradycardia and heart block.
Isoprenaline HCl (Isoproterenol HCl) Chemical Structure CAS No.: 51-30-9
Product category: Adrenergic Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
10g
Other Sizes

Other Forms of Isoprenaline HCl (Isoproterenol HCl):

  • Isoproterenol
  • Isoproterenol sulfate anhydrous
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Isoprenaline HCL (NCIc55630; NCI c55630; Isoproterenol), the hydrochloride salt of Isoprenaline, is a non-selective beta-adrenergic receptor agonist that has been used for the treatment of bradycardia and heart block.

Biological Activity I Assay Protocols (From Reference)
Targets
β adrenergic receptor
ln Vitro

In vitro activity: Isoprenaline (Isoproterenol) hydrochloride (300 nM, 3 min) increases in intact rat fat cells the low-Km cAMP phosphodiesterase (cAMP-PDE) activity that is inhibited by particulate cGMP and cilostamide by approximately 100%[1].
Isoprenaline suppresses insulin-stimulated glucose transport activity in rat adipocytes. In the absence of adenosine, isoprenaline causes a time-dependent (t1/2 of about 2 min) decrease in the accessibility of GLUT4 on the cell surface that is stimulated by insulin that is greater than 50%. This decrease is directly correlated with the observed inhibition of transport activity[2].
Isoprenaline (5 nM and 10 μM) raises the levels of cyclic AMP; this effect is enhanced by cyclic GMP-elevating agents (50 nM ANF or 30 nM SNP plus 100 nM DMPPO), cilostamide (10 mM), and rolipram, a cyclic AMP-specific PDE (PDE 4) inhibitor (10 mM)[3].
Isoprenaline causes the Gi alpha-2 gene's transcriptional activity to rise to 140% of the control value, while Gs alpha gene specific hybridization stays the same[4].
Isoprenaline (20 nM) raises the total iK amplitude and, both in the absence and in the presence of 300 nM nisoldipine to block the L-type Ca2+ current, results in a negative shift of roughly 10 mV in the iK activation curve[5].
Isoprenaline (20 nM) raises the rate of spontaneous pacemaker occurrence of sino-atrial node pacemaker cells in isolated rabbit pacemaker cells by sixteen percent[5].

ln Vivo
Isoprenaline (also known as isoproterenol) hydrochloride (oral, 0.27–0.64 μg/kg) is extensively metabolized through a limited number of reactions in dogs[6].
Animal Protocol
Dogs
0.27-0. 64 μg/kg
oral
References

[1]. 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]. 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]. 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]. 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]. Modulation of delayed rectifier potassium current, iK, by isoprenaline in rabbit isolated pacemaker cells. Exp Physiol. 2000 Jan;85(1):27-35.

[6]. Metabolism of isoprenaline in dog and man. Br J Pharmacol . 1972 Nov;46(3):458-72.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C11H18CLNO3
Molecular Weight
247.72
Exact Mass
247.1
Elemental Analysis
C, 53.34; H, 7.32; Cl, 14.31; N, 5.65; O, 19.38
CAS #
51-30-9
Related CAS #
Isoprenaline; 7683-59-2; Isoprenaline hemisulfate; 299-95-6
Appearance
Solid powder
SMILES
CC(C)NCC(C1=CC(=C(C=C1)O)O)O.Cl
InChi Key
IROWCYIEJAOFOW-UHFFFAOYSA-N
InChi Code
InChI=1S/C11H17NO3.ClH/c1-7(2)12-6-11(15)8-3-4-9(13)10(14)5-8;/h3-5,7,11-15H,6H2,1-2H3;1H
Chemical Name
4-[1-hydroxy-2-(propan-2-ylamino)ethyl]benzene-1,2-diol;hydrochloride
Synonyms
NCI-c55630; Isoprenaline hydrochloride; NCIc55630; NCI c55630; Isoproterenol
HS Tariff Code
2934.99.03.00
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 Data
Solubility (In Vitro)
DMSO: 50~80 mg/mL (201.8~323 mM)
Water: ~50 mg/mL (~201.8 mM)
Ethanol: <1 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.08 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (8.40 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


Solubility in Formulation 4: ~2.1 mg/mL or 8.40 mM in 10% DMSO: 40% PEG300: 5% Tween-80: 45% Saline
~2.1 mg/mL or 8.40 mM in 10% DMSO: 90% (20% SBE-β-CD in Saline)


Solubility in Formulation 5: 100 mg/mL (403.68 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 4.0368 mL 20.1841 mL 40.3682 mL
5 mM 0.8074 mL 4.0368 mL 8.0736 mL
10 mM 0.4037 mL 2.0184 mL 4.0368 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.

Calculator

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What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05219799 Recruiting Drug: Propranolol Hydrochloride
Drug: Isoproterenol
Obesity
Vasodilation
Healthy
University of Missouri-Columbia March 14, 2023 Early Phase 1
NCT05997732 Recruiting Drug: Phenylephrine Hydrochloride
Drug: Isoproterenol Hydrochloride
Vasoconstriction
Vasodilation
University of Alberta October 31, 2023 Phase 4
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