2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. Rapacuronium bromide

Rapacuronium bromide  (Synonyms: Org 9487)

Cat. No.: HY-16423 Purity: ≥98.0%
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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.

Rapacuronium bromide Chemical Structure

Rapacuronium bromide Chemical Structure

CAS No. : 156137-99-4

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Based on 1 publication(s) in Google Scholar

Rapacuronium bromide Related Antibodies

Top Publications Citing Use of Products

View All mAChR Isoform Specific Products:

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mAChR1 mAChR2 mAChR3 mAChR4 mAChR5

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Rapacuronium bromide (Org 9487), a non-depolarizing neuromuscular blocker, is an allosteric modulator of muscarinic acetylcholine receptor (mAChR)[1].

IC50 & Target

Muscarinic receptor[1]
In Vitro

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.

Rapacuronium bromide Related Antibodies
In Vivo

Time course of the neuromuscular effects of Rapacuronium following the administration of the 2×ED90 doses to rats and guinea-pigs with ED90 of 5953±199 and 187±16 µg/kg in rat and guinea pig, respectively[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

677.80

Formula

C37H61BrN2O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

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-]
Shipping

Room temperature in continental US; may vary elsewhere.
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
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4754 mL 7.3768 mL 14.7536 mL
5 mM 0.2951 mL 1.4754 mL 2.9507 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References
Kinase Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

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
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Rapacuronium bromide Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rapacuronium156137-99-4Org 9487Org9487Org-9487mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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