MedKoo Cat#: 145652 | Name: Encukalner HCl

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Encukalner, also known as XEN1101, is a selective positive allosteric modulator of KCNQ2/3 (Kv7.2/7.3) voltage-gated potassium channels, which are critical regulators of neuronal excitability. It enhances M-current in neurons, thereby stabilizing the resting membrane potential and reducing neuronal firing. Preclinical electrophysiological studies demonstrated that Encukalner significantly increased potassium currents in cells expressing KCNQ2/3 channels with an EC₅₀ in the low micromolar range (~0.3–1 μM).

Chemical Structure

Encukalner HCl
Encukalner HCl
CAS#Encukalner HCl

Theoretical Analysis

MedKoo Cat#: 145652

Name: Encukalner HCl

CAS#: Encukalner HCl

Chemical Formula: C23H30ClFN2O

Exact Mass: 368.2300

Molecular Weight: 404.95

Elemental Analysis: C, 68.22; H, 7.47; Cl, 8.75; F, 4.69; N, 6.92; O, 3.95

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Synonym
Encukalner HCl; Encukalner hydrohloride; 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 hydrochloride
InChi Key
NPVDOWWJLBLKDK-UHFFFAOYSA-N
InChi Code
InChI=1S/C23H29FN2O.ClH/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);1H
SMILES Code
CC(C)(C)CC(NC1=C(C)C=C(N2CC3=C(C=C(F)C=C3)CC2)C=C1C)=O.[H]Cl
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
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 404.95 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.

Recalculate based on batch purity %
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: Lattanzi S, Trinka E, Meletti S, Striano P, Matricardi S, Silvestrini M, Brigo F. A profile of azetukalner for the treatment of epilepsy: from pharmacology to potential for therapy. Expert Rev Clin Pharmacol. 2024 May- Jun;17(5-6):423-432. doi: 10.1080/17512433.2024.2337012. Epub 2024 Apr 3. PMID: 38571335. 2: Bialer M, Johannessen SI, Koepp MJ, Perucca E, Perucca P, Tomson T, White HS. Progress report on new medications for seizures and epilepsy: A summary of the 17th Eilat Conference on New Antiepileptic Drugs and Devices (EILAT XVII). II. Drugs in more advanced clinical development. Epilepsia. 2024 Oct;65(10):2858-2882. doi: 10.1111/epi.18075. Epub 2024 Aug 22. PMID: 39171993.