WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H577743
CAS#: 1009344-33-5
Description: Encukalner, also known as XEN1101, is a calcium-activated potassium channel positive allosteric modulator.
Hodoodo Cat#: H577743
Name: Encukalner
CAS#: 1009344-33-5
Chemical Formula: C23H29FN2O
Exact Mass: 368.23
Molecular Weight: 368.500
Elemental Analysis: C, 74.97; H, 7.93; F, 5.16; N, 7.60; O, 4.34
Synonym: 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
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: 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:
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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 |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
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.
