Synonym
AP30663; AP-30663; AP 30663;
IUPAC/Chemical Name
(S)-3-((1H-benzo[d]imidazol-2-yl)amino)-N-(cyanomethyl)-N-methyl-3-(3-(trifluoromethyl)phenyl)propanamide
InChi Key
KPVQYQOKIIKXMI-KRWDZBQOSA-N
InChi Code
InChI=1S/C20H18F3N5O/c1-28(10-9-24)18(29)12-17(13-5-4-6-14(11-13)20(21,22)23)27-19-25-15-7-2-3-8-16(15)26-19/h2-8,11,17H,10,12H2,1H3,(H2,25,26,27)/t17-/m0/s1
SMILES Code
CN(C(C[C@@H](C1=CC(C(F)(F)F)=CC=C1)NC2=NC3=C(N2)C=CC=C3)=O)CC#N
Appearance
To be determined
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
To be determined
Shelf Life
>2 years if stored properly
Drug Formulation
To be determined
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
Preparing Stock Solutions
The following data is based on the
product
molecular weight
401.39
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 |
1: Diness JG, Kirchhoff JE, Speerschneider T, Abildgaard L, Edvardsson N,
Sørensen US, Grunnet M, Bentzen BH. The KCa2 Channel Inhibitor
AP30663 Selectively Increases Atrial Refractoriness, Converts Vernakalant-
Resistant Atrial Fibrillation and Prevents Its Reinduction in Conscious Pigs.
Front Pharmacol. 2020 Feb 28;11:159. doi: 10.3389/fphar.2020.00159. PMID:
32180722; PMCID: PMC7059611.
2: Bentzen BH, Bomholtz SH, Simó-Vicens R, Folkersen L, Abildgaard L,
Speerschneider T, Muthukumarasamy KM, Edvardsson N, Sørensen US, Grunnet M,
Diness JG. Mechanisms of Action of the KCa2-Negative Modulator AP30663, a Novel
Compound in Development for Treatment of Atrial Fibrillation in Man. Front
Pharmacol. 2020 May 6;11:610. doi: 10.3389/fphar.2020.00610. PMID: 32477117;
PMCID: PMC7232560.
3: Holst AG, Tomcsányi J, Vestbjerg B, Grunnet M, Sørensen US, Diness JG,
Bentzen BH, Edvardsson N, Hohnloser SH, Bhatt DL, Dorian P. Inhibition of the
KCa2 potassium channel in atrial fibrillation: a randomized phase 2
trial. Nat Med. 2024 Jan;30(1):106-111. doi: 10.1038/s41591-023-02679-9. Epub
2023 Dec 13. PMID: 38092897; PMCID: PMC10803288.
4: Diness JG, Abildgaard L, Bomholtz SH, Skarsfeldt MA, Edvardsson N, Sørensen
US, Grunnet M, Bentzen BH. Inhibition of KCa2 Channels Decreased the
Risk of Ventricular Arrhythmia in the Guinea Pig Heart During Induced
Hypokalemia. Front Pharmacol. 2020 May 20;11:749. doi: 10.3389/fphar.2020.00749.
PMID: 32508659; PMCID: PMC7251152.
