WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H206441
CAS#: 1593673-23-4
Description: Etripamil is a calcium channel blocker. Calcium channel blockers (CCB), calcium channel antagonists or calcium antagonists are several medications that disrupt the movement of calcium (Ca2+) through calcium channels. Calcium channel blockers are used as antihypertensive drugs, i.e., as medications to decrease blood pressure in patients with hypertension.
Hodoodo Cat#: H206441
Name: Etripamil
CAS#: 1593673-23-4
Chemical Formula: C27H36N2O4
Exact Mass: 452.27
Molecular Weight: 452.600
Elemental Analysis: C, 71.65; H, 8.02; N, 6.19; O, 14.14
Synonym: (-)-MSP-2017; MSP-2017; MSP 2017; MSP2017; MSP-2017A; MSP-2017B; Etripamil
IUPAC/Chemical Name: methyl (S)-3-(2-((4-cyano-4-(3,4-dimethoxyphenyl)-5-methylhexyl)(methyl)amino)ethyl)benzoate
InChi Key: VAZNEHLGJGSQEL-MHZLTWQESA-N
InChi Code: InChI=1S/C27H36N2O4/c1-20(2)27(19-28,23-11-12-24(31-4)25(18-23)32-5)14-8-15-29(3)16-13-21-9-7-10-22(17-21)26(30)33-6/h7,9-12,17-18,20H,8,13-16H2,1-6H3/t27-/m0/s1
SMILES Code: O=C(OC)C1=CC=CC(CCN(CCC[C@](C2=CC=C(OC)C(OC)=C2)(C#N)C(C)C)C)=C1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
| Biological target: | L-type calcium channel |
| In vitro activity: | TBD |
| In vivo activity: | This phase 2 study was performed during electrophysiological testing in patients with previously documented SVT who were induced into SVT prior to undergoing a catheter ablation. Patients in sustained SVT for 5 min received either placebo or 1 of 4 doses of active compound. The primary endpoint was the SVT conversion rate within 15 min of study drug administration. Secondary endpoints included time to conversion and adverse events. One hundred four patients were dosed. Conversion rates from SVT to sinus rhythm were between 65% and 95% in the etripamil nasal spray groups and 35% in the placebo group; the differences were statistically significant (Pearson chi-square test) in the 3 highest active compound dose groups versus placebo. In patients who converted, the median time to conversion with etripamil was <3 min. Adverse events were mostly related to the intranasal route of administration or local irritation. Reductions in blood pressure occurred predominantly in the highest etripamil dose. Etripamil nasal spray rapidly terminated induced SVT with a high conversion rate. The safety and efficacy results of this study provide guidance for etripamil dose selection for future studies involving self-administration of this new intranasal calcium-channel blocker in a real-world setting for the termination of SVT. Reference: Stambler BS, Dorian P, Sager PT, Wight D, Douville P, Potvin D, Shamszad P, Haberman RJ, Kuk RS, Lakkireddy DR, Teixeira JM, Bilchick KC, Damle RS, Bernstein RC, Lam WW, O'Neill G, Noseworthy PA, Venkatachalam KL, Coutu B, Mondésert B, Plat F. Etripamil Nasal Spray for Rapid Conversion of Supraventricular Tachycardia to Sinus Rhythm. J Am Coll Cardiol. 2018 Jul 31;72(5):489-497. doi: 10.1016/j.jacc.2018.04.082. PMID: 30049309. |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| Ethanol | 120.0 | 265.13 |
The following data is based on the product molecular weight 452.60 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | Stambler BS, Dorian P, Sager PT, Wight D, Douville P, Potvin D, Shamszad P, Haberman RJ, Kuk RS, Lakkireddy DR, Teixeira JM, Bilchick KC, Damle RS, Bernstein RC, Lam WW, O'Neill G, Noseworthy PA, Venkatachalam KL, Coutu B, Mondésert B, Plat F. Etripamil Nasal Spray for Rapid Conversion of Supraventricular Tachycardia to Sinus Rhythm. J Am Coll Cardiol. 2018 Jul 31;72(5):489-497. doi: 10.1016/j.jacc.2018.04.082. PMID: 30049309. |
| In vitro protocol: | TBD |
| In vivo protocol: | Stambler BS, Dorian P, Sager PT, Wight D, Douville P, Potvin D, Shamszad P, Haberman RJ, Kuk RS, Lakkireddy DR, Teixeira JM, Bilchick KC, Damle RS, Bernstein RC, Lam WW, O'Neill G, Noseworthy PA, Venkatachalam KL, Coutu B, Mondésert B, Plat F. Etripamil Nasal Spray for Rapid Conversion of Supraventricular Tachycardia to Sinus Rhythm. J Am Coll Cardiol. 2018 Jul 31;72(5):489-497. doi: 10.1016/j.jacc.2018.04.082. PMID: 30049309. |
