| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
beta1-Adrenergic and beta2-Adrenergic Receptors (beta1-AR and beta2-AR). Propranolol D7 HCl acts as a competitive and non-selective antagonist of beta1- and beta2-adrenergic receptors. It has high affinity for both receptors, with Ki values of 1.8 nM for beta1-AR and 0.8 nM for beta2-AR. By blocking the binding of endogenous catecholamines (epinephrine, norepinephrine), it reduces heart rate (negative chronotropy), decreases cardiac contractility (negative inotropy), lowers blood pressure, and suppresses renin release from the kidneys. It also has membrane-stabilizing (local anesthetic) activity at high concentrations and is highly lipophilic, facilitating CNS penetration.
|
|---|---|
| ln Vitro |
Propranolol HCl has Ki values of 1.8 nM for beta1-AR and 0.8 nM for beta2-AR. It inhibits isoprenaline (isoproterenol)-induced tachycardia in vitro with a pA2 of 8.5-9.0 in isolated guinea pig atria. The D7-labeled version is an internal standard and is not tested for activity in functional assays. It blocks norepinephrine-induced lipolysis in isolated rat adipocytes (beta3-AR, albeit with lower affinity) at higher concentrations.
|
| ln Vivo |
In animal models, propranolol (0.1-10 mg/kg i.v. or p.o.) inhibits isoprenaline-induced tachycardia, reduces mean arterial blood pressure (MAP) in hypertensive rats, and reduces cardiac output (negative inotropic/chronotropic effects). It crosses the blood-brain barrier (BBB) and produces CNS effects (e.g., reduced anxiety-like behavior, blockade of fear memory reconsolidation). The D7-labeled version is not administered in efficacy studies; it is used as an IS in bioanalysis.
|
| Enzyme Assay |
Radioligand binding assays for beta1- and beta2-AR: Membrane preparations from CHO cells expressing human beta1-AR or beta2-AR (20-50 microg protein) are incubated with [3H]CGP-12177 (a non-selective beta-antagonist) or [¹2⁵I]-cyanopindolol as the radioligand and varying concentrations of propranolol (unlabeled) (0.01-1000 nM) for 60 minutes at 25degC in 50 mM Tris-HCl buffer (pH 7.4). Nonspecific binding is determined with 10 microM propranolol. Bound and free radioligands are separated by filtration through GF/B filters. Bound radioactivity is measured by liquid scintillation or gamma counting. Ki values are calculated from IC50 using the Cheng-Prusoff equation.
|
| Cell Assay |
Not applicable (Propranolol D7 HCl is an internal standard, not used in cell-based functional assays for activity). For functional antagonism in vitro, isolated guinea pig right atria are mounted in organ baths containing Krebs-Henseleit buffer (37degC, 95% O2/5% CO2) with a resting tension of 0.5-1 g. Tissues are electrically paced at 1-3 Hz to measure contractile force and rate. Cumulative concentration-response curves to isoprenaline (0.1-1000 nM) are constructed in the absence or presence of propranolol (1-1000 nM, 30 min pre-incubation). The pA2 (negative logarithm of the antagonist dissociation constant) is calculated from the rightward shift of the isoprenaline concentration-response curve using Schild plot analysis.
|
| Animal Protocol |
Male Sprague-Dawley rats (200-300 g, n=6 per group) are anesthetized and instrumented with carotid artery catheters for blood pressure (MAP) and heart rate (HR) monitoring and jugular vein catheters for drug administration. Propranolol (0.1-10 mg/kg) or vehicle is administered intravenously (bolus or infusion). For oral studies, propranolol (5-20 mg/kg) is administered by gavage. Isoprenaline (0.1-1 microg/kg) is administered as a bolus before and after propranolol administration. The percent inhibition of isoprenaline-induced tachycardia is calculated. For PK studies, blood samples are collected at 0, 15, 30, 60, 120, 240, and 360 min post-dose. Plasma is processed and analyzed by LC-MS/MS using Propranolol D7 HCl as the internal standard.
|
| ADME/Pharmacokinetics |
Propranolol D7 HCl is a stable isotope internal standard with a mass shift of +7 Da. Propranolol is highly lipophilic (logP ~3.0), is completely absorbed after oral administration (>90%), but undergoes extensive first-pass metabolism, resulting in an absolute oral bioavailability of approximately 25-30% in humans. It is highly protein bound (>90%, primarily to albumin and alpha1-acid glycoprotein). The terminal half-life is 3-6 hours. It is metabolized primarily by CYP2D6 (major), CYP1A2, and CYP3A4.
|
| Toxicity/Toxicokinetics |
Propranolol D7 HCl is for research use only and not for human consumption. The parent drug propranolol is generally well tolerated. Common adverse effects include bradycardia, hypotension, fatigue, dizziness, cold extremities (Raynaud's phenomenon), and sleep disturbances (insomnia, vivid dreams). Propranolol is contraindicated in patients with asthma (beta2 blockade causes bronchospasm), bradycardia, heart block, and severe hypotension. Overdose can cause cardiac failure, severe bradycardia, and respiratory depression.
|
| References | |
| Additional Infomation |
Propranolol (Inderal®) was FDA-approved in 1967 as the first clinically successful beta-blocker. It is widely used for hypertension, angina pectoris, cardiac arrhythmias, myocardial infarction prevention, migraine prophylaxis, essential tremor, and anxiety disorders (stage fright). Propranolol D7 HCl is a research internal standard for LC-MS/MS bioanalysis. It is essential for accurate quantification of propranolol in clinical research, therapeutic drug monitoring (TDM), pharmacokinetic studies, and drug-drug interaction studies (especially with CYP2D6 substrates), as well as for forensic toxicology.
|
| Molecular Formula |
C16H14D7NO2.HCL
|
|---|---|
| Molecular Weight |
302.848
|
| Exact Mass |
266.201
|
| CAS # |
1613439-56-7
|
| Related CAS # |
Propranolol hydrochloride;318-98-9;(S)-(-)-Propranolol hydrochloride;4199-10-4;Propranolol-d7 (ring-d7);344298-99-3
|
| PubChem CID |
75125730
|
| Appearance |
White to off-white solid powder
|
| LogP |
2.968
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
20
|
| Complexity |
257
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
[2H]C([2H])([2H])C([2H])(C([2H])([2H])[2H])NCC(COC1=CC=CC2=CC=CC=C21)O.Cl
|
| InChi Key |
ZMRUPTIKESYGQW-ODLOEXKQSA-N
|
| InChi Code |
InChI=1S/C16H21NO2.ClH/c1-12(2)17-10-14(18)11-19-16-9-5-7-13-6-3-4-8-15(13)16;/h3-9,12,14,17-18H,10-11H2,1-2H3;1H/i1D3,2D3,12D;
|
| Chemical Name |
1-(1,1,1,2,3,3,3-heptadeuteriopropan-2-ylamino)-3-naphthalen-1-yloxypropan-2-ol;hydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 Vitro) |
DMSO : ~100 mg/mL (~330.20 mM)
|
|---|---|
| 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 | 3.3020 mL | 16.5098 mL | 33.0196 mL | |
| 5 mM | 0.6604 mL | 3.3020 mL | 6.6039 mL | |
| 10 mM | 0.3302 mL | 1.6510 mL | 3.3020 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
