Synonym
Azetukalner; Encukalner; XEN1101; XEN-1101 XEN 1101; 1OP 2198; VRX 621698; XPF-008;
IUPAC/Chemical Name
N-[4-(6-fluoro-3,4-dihydroisoquinolin-2(1H)-yl)-2,6-dimethylphenyl]-3,3-dimethylbutanamide
InChi Key
FJNPZKZPWVVSON-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H29FN2O/c1-15-10-20(11-16(2)22(15)25-21(27)13-23(3,4)5)26-9-8-17-12-19(24)7-6-18(17)14-26/h6-7,10-12H,8-9,13-14H2,1-5H3,(H,25,27)
SMILES Code
CC(C)(C)CC(NC1=C(C)C=C(N2CC3=C(C=C(F)C=C3)CC2)C=C1C)=O
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
More Info
In vivo, it showed potent anticonvulsant activity in multiple rodent seizure models, including maximal electroshock seizure (MES) and pentylenetetrazol (PTZ) models. Importantly, Encukalner does not require metabolic activation (unlike ezogabine) and exhibits improved pharmacokinetics and CNS penetration. In Phase 2 clinical trials (e.g., X-TOLE study), Encukalner significantly reduced monthly focal seizure frequency in adults with focal epilepsy, with dose-dependent efficacy and a favorable tolerability profile.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
368.50
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: Yang GM, Tian FY, Shen YW, Yang CY, Yuan H, Li P, Gao ZB. Functional characterization and in vitro pharmacological rescue of KCNQ2 pore mutations associated with epileptic encephalopathy. Acta Pharmacol Sin. 2023 Mar 17. doi: 10.1038/s41401-023-01073-y. Epub ahead of print. PMID: 36932231.
2: Elkommos S, Mula M. Current and future pharmacotherapy options for drug- resistant epilepsy. Expert Opin Pharmacother. 2022 Dec;23(18):2023-2034. doi: 10.1080/14656566.2022.2128670. Epub 2022 Sep 27. PMID: 36154780.
3: Bialer M, Johannessen SI, Koepp MJ, Levy RH, Perucca E, Perucca P, Tomson T, White HS. Progress report on new antiepileptic drugs: A summary of the Sixteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XVI): II. Drugs in more advanced clinical development. Epilepsia. 2022 Nov;63(11):2883-2910. doi: 10.1111/epi.17376. Epub 2022 Aug 11. PMID: 35950617.
4: Biondi A, Rocchi L, Santoro V, Rossini PG, Beatch GN, Richardson MP, Premoli I. Spontaneous and TMS-related EEG changes as new biomarkers to measure anti- epileptic drug effects. Sci Rep. 2022 Feb 4;12(1):1919. doi: 10.1038/s41598-022-05179-x. PMID: 35121751; PMCID: PMC8817040.
5: Bialer M, Johannessen SI, Koepp MJ, Levy RH, Perucca E, Perucca P, Tomson T, White HS. Progress report on new antiepileptic drugs: A summary of the Fifteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XV). I. Drugs in preclinical and early clinical development. Epilepsia. 2020 Nov;61(11):2340-2364. doi: 10.1111/epi.16725. Epub 2020 Nov 14. PMID: 33190243.
6: Premoli I, Rossini PG, Goldberg PY, Posadas K, Green L, Yogo N, Pimstone S, Abela E, Beatch GN, Richardson MP. TMS as a pharmacodynamic indicator of cortical activity of a novel anti-epileptic drug, XEN1101. Ann Clin Transl Neurol. 2019 Nov;6(11):2164-2174. doi: 10.1002/acn3.50896. Epub 2019 Sep 30. PMID: 31568714; PMCID: PMC6856596.
7: Bialer M, Johannessen SI, Koepp MJ, Levy RH, Perucca E, Tomson T, White HS. Progress report on new antiepileptic drugs: A summary of the Fourteenth Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XIV). I. Drugs in preclinical and early clinical development. Epilepsia. 2018 Oct;59(10):1811-1841. doi: 10.1111/epi.14557. PMID: 30368792.
