Rapacuronium bromide
Based on 1 Customer Validation
Rapacuronium bromide (Org 9487), a non-depolarizing neuromuscular blocker, is an allosteric modulator of muscarinic acetylcholine receptor (mAChR).
For research use only. We do not sell to patients.
- Purity: 98.0%
- CAS No.: 156137-99-4
- Formula: C37H61BrN2O4
- Molecular Weight:677.80
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Muscarinic receptor[1]
Rapacuronium binds to all muscarinic receptor subtypes at physiologically relevant concentrations and displays micromolar affinity and slight selectivity towards M2 receptor. Rapacuronium exhibits complex effects on the kinetics of ACh binding and subsequent receptor activation estimated from stimulation of [35S]GTPγS binding. Rapacuronium alone concentration dependently lowers [35S]GTPγS binding to membranes with a maximal effect of approximately 25% at odd-numbered subtypes and 15% at even-numbered subtypes, with EC50 ranging from 28 μM at M2 receptors to 76 μM at M3 receptors. While the EC50 values of Rapacuronium in inhibiting [35S]GTPγS binding at individual subtypes correlated with affinities measured in binding experiments with [3H]ACh (R2 = 0.76) they are lower (4- to 12-fold) at all subtypes. Measurements of ACh-stimulated [35S]GTPγS binding in the presence of 0.1, 1 and 10 μM Rapacuronium shows differential effects of Rapacuronium on receptor activation by an orthosteric agonist at individual receptor subtypes. At even-numbered subtypes 1 μM and 10 μM Rapacuronium significantly increases ACh EC50, with lowering of EMAX at 10 μM Rapacuronium. At this subtype 0.1 and 1 μM Rapacuronium causes a significant 2-fold decrease in ACh EC50 and approximately 60% and 35% increase in EMAX, respectively. Rapacuronium at 10 μM increases ACh EC50 by about 3-fold without a significant change in EMAX. Rapacuronium (0.1 - 10 μM) has no effect on ACh efficacy at the M1 and M5 subtypes but decreases the EC50 of ACh in stimulating [35S]GTPγS binding by 1.5- and 4-fold, respectively, at concentrations of 0.1 and 1 μM. However, this effect is not evident at 10 μM Rapacuronium[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 156137-99-4
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Appearance Solid
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Molecular Weight 677.80
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Formula C37H61BrN2O4
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Color Light yellow to yellow
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SMILES
C[C@@]12[C@](CC[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])C[C@H]([N+]5(CC=C)CCCCC5)[C@@H]4OC(CC)=O)([H])C[C@H](OC(C)=O)[C@@H](N6CCCCC6)C1.[Br-]
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Synonyms
Org 9487
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : ≥ 125 mg/mL (184.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
For determination of [35S]GTPγS binding to G-proteins in membranes a final concentration of 200 pM (M1, M3 and M5 receptors) or 500 pM (M2 and M4 receptors) of [35S]GTPγS is used. Incubation medium is supplemented with 5 μM (M1, M3 and M5 receptors) or 50 μM (M2 and M4 receptors) GDP. Nonspecific binding is determined in the presence of 1 μM unlabeled GTPγS. When effects of Rapacuronium on ACh-stimulated [35S]GTPγS binding is measured Rapacuronium is added to membranes 60 min prior to ACh and [35S]GTPγS. Incubation with [35S]GTPγS is carried out for 20 min and free ligand is removed by filtration as described above. Filtration and washing with ice-cold water lasted for 9 s (wash-aspirate button time). After filtration filters are dried in vacuum for 1 h while heated at 80°C and then solid scintillator Meltilex A is melted on filters (105°C, 90 s) using a hot plate. After cooling the filters are counted using a Wallac Microbeta scintillation counter[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (280 KB)
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SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
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Handling Instructions (2659 KB)
References
[1]. Jakubík J, et al. Divergence of allosteric effects of Rapacuronium on binding and function of muscarinic receptors. BMC Pharmacol. 2009 Dec 28;9:15. [Content Brief]
[2]. Vizi ES, et al. A new short-acting non-depolarizing muscle relaxant (SZ1677) without cardiovascular side-effects. Acta Anaesthesiol Scand. 2003 Mar;47(3):291-300. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.4754 mL | 7.3768 mL | 14.7536 mL | 36.8840 mL |
| 5 mM | 0.2951 mL | 1.4754 mL | 2.9507 mL | 7.3768 mL | |
| 10 mM | 0.1475 mL | 0.7377 mL | 1.4754 mL | 3.6884 mL | |
| 15 mM | 0.0984 mL | 0.4918 mL | 0.9836 mL | 2.4589 mL | |
| 20 mM | 0.0738 mL | 0.3688 mL | 0.7377 mL | 1.8442 mL | |
| 25 mM | 0.0590 mL | 0.2951 mL | 0.5901 mL | 1.4754 mL | |
| 30 mM | 0.0492 mL | 0.2459 mL | 0.4918 mL | 1.2295 mL | |
| 40 mM | 0.0369 mL | 0.1844 mL | 0.3688 mL | 0.9221 mL | |
| 50 mM | 0.0295 mL | 0.1475 mL | 0.2951 mL | 0.7377 mL | |
| 60 mM | 0.0246 mL | 0.1229 mL | 0.2459 mL | 0.6147 mL | |
| 80 mM | 0.0184 mL | 0.0922 mL | 0.1844 mL | 0.4611 mL | |
| 100 mM | 0.0148 mL | 0.0738 mL | 0.1475 mL | 0.3688 mL |
Rapacuronium bromide Related Classifications
HY-16423 Related Classifications
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