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Ipratropium-d7 bromide (Sch 1000-d7 (bromide))

Cat No.:V76884 Purity: ≥98%
Ipratropium-d7 (bromide)e is the deuterated form of Ipratropium bromide.
Ipratropium-d7 bromide (Sch 1000-d7 (bromide))
Ipratropium-d7 bromide (Sch 1000-d7 (bromide)) Chemical Structure Product category: mAChR
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
1mg
Other Sizes

Other Forms of Ipratropium-d7 bromide (Sch 1000-d7 (bromide)):

  • Ipratropium Bromide (Sch 1000)
  • Ipratropium bromide hydrate
  • Ipratropium Bromide
Official Supplier of:
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Top Publications Citing lnvivochem Products
Product Description
Ipratropium-d7 (bromide)e is the deuterated form of Ipratropium bromide. Ipratropium bromide (Sch 1000) is an antagonist of muscarinic receptors, with IC50s of 2.9 nM, 2 nM and 1.7 nM for binding to M1, M2 and M3 receptors respectively. Ipratropium bromide may be used in research on COPD and asthma, among others.
Ipratropium-d7 bromide (Sch 1000-d7 bromide) is a deuterium-labeled form of ipratropium bromide, a muscarinic acetylcholine receptor antagonist used as a bronchodilator in chronic obstructive pulmonary disease (COPD) and asthma. The d7 label (seven deuterium atoms) serves as an internal standard for LC-MS/MS quantification in bioanalytical studies.
Biological Activity I Assay Protocols (From Reference)
Targets
Ipratropium-d7 bromide targets muscarinic acetylcholine receptors (M1, M2, M3 subtypes) in the airways. It acts as a competitive antagonist, blocking the action of acetylcholine and reducing bronchial smooth muscle tone. The d7 label does not alter receptor binding, but the labeled compound is used primarily as an analytical standard, not for activity studies.
ln Vitro
Drug compounds have included stable heavy isotopes of carbon, hydrogen, and other elements, mostly as tracers for quantification throughout the drug development process. Due to its potential to alter the pharmacokinetic and metabolic characteristics of medications, deuteration has drawn attention[1].
Unlabeled ipratropium bromide inhibits carbachol-induced contraction of isolated guinea pig tracheal rings (cell-free tissue bath assay) with an IC50 in the low nanomolar range. It also displaces [3H]-N-methylscopolamine from M3 receptors in membrane preparations (Kd ~0.2 nM). Ipratropium-d7 is not used in these assays; it is used for quantification.
ln Vivo
In cell-based assays (e.g., human bronchial epithelial cells or smooth muscle cells), unlabeled ipratropium (0.1-100 nM) inhibits methacholine-induced calcium flux and ERK phosphorylation. It also blocks acetylcholine-induced bronchoconstriction in isolated perfused lungs. Ipratropium-d7 is used as an internal standard to measure drug concentrations in cell lysates or culture media by LC-MS/MS.
Enzyme Assay
For analytical method development, Ipratropium-d7 bromide is used as an internal standard. A calibration curve is prepared by spiking unlabeled ipratropium bromide into blank plasma or buffer with a fixed concentration of the d7 standard. Samples are extracted by protein precipitation or solid-phase extraction and analyzed by LC-MS/MS. The peak area ratio (unlabeled/d7) is used for quantification. No receptor binding assay is performed with the labeled standard.
Cell Assay
Bronchial epithelial cells or lung slices are treated with unlabeled ipratropium bromide (0.1-100 nM) for 15-60 minutes. At the end of the experiment, cells are lysed, and ipratropium concentrations are quantified by LC-MS/MS using Ipratropium-d7 as the internal standard. This allows measurement of cellular accumulation. Parallel functional assays (e.g., calcium flux) are performed to correlate concentration with effect.
Animal Protocol
In animal studies, Ipratropium-d7 can be co-administered with unlabeled ipratropium as a tracer, or used as an internal standard in bioanalysis. Rats or guinea pigs are dosed with ipratropium bromide via inhalation or intravenous injection (e.g., 1-10 ug/kg). Blood and lung tissue are collected at multiple time points. Samples are analyzed by LC-MS/MS with Ipratropium-d7 as the internal standard to determine pharmacokinetic parameters (Cmax, AUC, half-life).
ADME/Pharmacokinetics
Ipratropium-d7 has identical PK properties to unlabeled ipratropium. Ipratropium bromide is poorly absorbed after oral administration; it is administered by inhalation. The systemic bioavailability is low (2-5%). After inhalation, the drug acts locally in the lungs and is rapidly cleared from plasma (half-life 2-4 hours). It is metabolized by esterases and excreted in urine and feces. The d7 label does not affect these properties.
Toxicity/Toxicokinetics
Ipratropium-d7 is used in trace amounts and does not contribute to toxicity. The unlabeled ipratropium is well-tolerated at therapeutic doses. Common adverse effects include dry mouth, cough, and throat irritation. Systemic side effects (e.g., tachycardia, urinary retention) are rare due to low bioavailability. The deuterium label does not alter the safety profile. No additional toxicity is expected.
References

[1]. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

[2]. Fryer, A.D. and J. Maclagan, Ipratropium bromide potentiates bronchoconstriction induced by vagal nerve stimulation in the guinea-pig. Eur J Pharmacol, 1987. 139(2): p. 187-91.

[3]. Harvey, K.L., A. Hussain, and H.L. Maddock, Ipratropium Bromide-Mediated Myocardial Injury in In Vitro Models of Myocardial Ischaemia/Reperfusion. Toxicol Sci, 2014.

[4]. Discovery of novel quaternary ammonium derivatives of (3R)-quinuclidinyl amides as potent and long acting muscarinic antagonists. Bioorg Med Chem Lett. 2015 Apr 15;25(8):1736-1741.

[5]. Anti-inflammatory effects of formoterol and ipratropium bromide against acute cadmium-induced pulmonary inflammation in rats. Eur J Pharmacol. 2010 Feb 25;628(1-3):171-8.

Additional Infomation
Ipratropium bromide (Atrovent®) is an FDA-approved anticholinergic bronchodilator for COPD and asthma. Ipratropium-d7 is a research-grade stable isotope-labeled internal standard intended for non-clinical analytical use only. It is not for human therapeutic use. The compound is supplied as a powder, stored at -20degC. The d7 label has high isotopic purity (≥98%). It is commonly used in pharmacokinetic and bioequivalence studies.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C22H27D7BRNO3
Molecular Weight
447.46
Related CAS #
Ipratropium bromide;22254-24-6;Ipratropium bromide hydrate;66985-17-9
Appearance
Typically exists as solid at room temperature
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

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 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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2348 mL 11.1742 mL 22.3484 mL
5 mM 0.4470 mL 2.2348 mL 4.4697 mL
10 mM 0.2235 mL 1.1174 mL 2.2348 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

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

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:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
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  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
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.

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