Etripamil
Based on 1 Customer Validation
Etripamil (MSP-2017) is a short-acting, L-type calcium-channel antagonist. Etripamil inhibits calcium influx through slow calcium channels, thereby slowing AV node conduction and prolonging the AV node refractory period. Etripamil increases heart rate and decreases systolic blood pressure. Etripamil can be used in the study of paroxysmal supraventricular tachycardia (PSVT).
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- Reinheit: 98.10%
- CAS. Nr.: 1593673-23-4
- Formel: C27H36N2O4
- Molecular Weight:452.59
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Speicherung:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Alle Calcium Channel Isoform-spezifische Produkte anzeigen
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Biologische Aktivität
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L-type calcium channel |
Etripamil (1.9-5.7 mg/kg; intranasal administration; weekly; 26 doses) does not cause macroscopic or systemic microscopic abnormalities in cynomolgus monkeys[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Chinese-origin cynomolgus monkeys (20 males and 20 females, body weights ranged from 2.5-3.1 kg for males and 2.3-2.9 kg for females, age ranged from 2.5-4.0 years at dosing onset)[4]
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Dosage:1.9 mg/kg, 3.8 mg/kg, 5.7 mg/kg.
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Administration:Intranasal administration using a single-use nasal spray device, weekly for 26 doses
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Result:Showed no mortality.
Induced transient runny nose, sneezing, salivation, and vomiting (≥1.9 mg/kg/dose).
Did not cause histological changes in the nasal cavity, larynx, and pharynx at ≥1.9 mg/kg/dose.
Caused microscopic changes limited to the left nasal cavity and nasopharynx after a 28-day recovery period.
Showed a systemic NOAEL of 5.7 mg/kg/dose and local toxicity NOAEL of 1.9 mg/kg/dose.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 1593673-23-4
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Appearance Oil
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Molecular Weight 452.59
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Formel C27H36N2O4
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Color Brown to wine red
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SMILES
O=C(OC)C1=CC=CC(CCN(CCC[C@](C2=CC=C(OC)C(OC)=C2)(C#N)C(C)C)C)=C1
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Synonyms
MSP-2017; (-)-MSP-2017
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Lösungsmittel & Löslichkeit
Ethanol : 120 mg/mL (265.14 mM; Need ultrasonic)
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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 3 mg/mL (6.63 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 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% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 3 mg/mL (6.63 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 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.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 3 mg/mL (6.63 mM); Clear solution
This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.
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.
Working solution concentration: 0.22 mg/mL
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Stambler BS, et al. Etripamil Nasal Spray for Rapid Conversion of Supraventricular Tachycardia to Sinus Rhythm. J Am Coll Cardiol. 2018 Jul 31;72(5):489-497. [Content Brief]
[3]. Ascah A, et al. Cardiovascular and Pharmacokinetic Profiles of Intravenous Etripamil in Conscious Telemetered Cynomolgus Monkeys. Int J Toxicol. 2025 Apr 1:10915818251327963. [Content Brief]
[4]. Pion J, et al. Preclinical Safety Evaluation of Etripamil Nasal Spray in Cynomolgus Macaques (Macaca fascicularis) to Assess for Safety in Patients With Paroxysmal Supraventricular Tachycardia. Int J Toxicol. 2024 Sep-Oct;43(5):503-510. [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. 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 |
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| Ethanol | 1 mM | 2.2095 mL | 11.0475 mL | 22.0951 mL | 55.2376 mL |
| 5 mM | 0.4419 mL | 2.2095 mL | 4.4190 mL | 11.0475 mL | |
| 10 mM | 0.2210 mL | 1.1048 mL | 2.2095 mL | 5.5238 mL | |
| 15 mM | 0.1473 mL | 0.7365 mL | 1.4730 mL | 3.6825 mL | |
| 20 mM | 0.1105 mL | 0.5524 mL | 1.1048 mL | 2.7619 mL | |
| 25 mM | 0.0884 mL | 0.4419 mL | 0.8838 mL | 2.2095 mL | |
| 30 mM | 0.0737 mL | 0.3683 mL | 0.7365 mL | 1.8413 mL | |
| 40 mM | 0.0552 mL | 0.2762 mL | 0.5524 mL | 1.3809 mL | |
| 50 mM | 0.0442 mL | 0.2210 mL | 0.4419 mL | 1.1048 mL | |
| 60 mM | 0.0368 mL | 0.1841 mL | 0.3683 mL | 0.9206 mL | |
| 80 mM | 0.0276 mL | 0.1381 mL | 0.2762 mL | 0.6905 mL | |
| 100 mM | 0.0221 mL | 0.1105 mL | 0.2210 mL | 0.5524 mL |
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