WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 532978
CAS#: 122955-13-9 (HCl)
Description: XE991, also known as LS190926, is a potent and selective KCNQ channel blocker. XE991 blocks KCNQ2+3/M-currents (IC50 = 0.6-0.98 μM) and KCNQ1 homomeric channels (IC50 = 0.75 μM) but is less potent against KCNQ1/minK channels (IC50 = 11.1 μM).
MedKoo Cat#: 532978
Name: XE991 HCl
CAS#: 122955-13-9 (HCl)
Chemical Formula: C26H22Cl2N2O
Exact Mass: 376.1576
Molecular Weight: 449.375
Elemental Analysis: C, 69.49; H, 4.93; Cl, 15.78; N, 6.23; O, 3.56
Related CAS #: 122955-13-9 (HCl) 122955-42-4 (free base)
Synonym: XE991; XE 991; XE-991; LS 190926; LS190926.
IUPAC/Chemical Name: 10,10-bis(4-pyridinylmethyl)-9(10H)-anthracenone, dihydrochloride
InChi Key: WOGWMARIFDNZON-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H20N2O.2ClH/c29-25-21-5-1-3-7-23(21)26(17-19-9-13-27-14-10-19,18-20-11-15-28-16-12-20)24-8-4-2-6-22(24)25;;/h1-16H,17-18H2;2*1H
SMILES Code: O=C1C2=C(C=CC=C2)C(CC3=CC=NC=C3)(CC4=CC=NC=C4)C5=CC=CC=C15
Appearance: White to off-white 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
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
The following data is based on the product molecular weight 449.375 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: Greene DL, Kang S, Hoshi N. XE991 and Linopirdine are state-dependent inhibitors for Kv7/KCNQ channels that favor activated single subunits. J Pharmacol Exp Ther. 2017 May 8. pii: jpet.117.241679. doi: 10.1124/jpet.117.241679. [Epub ahead of print] PubMed PMID: 28483800.
2: Tsvetkov D, Tano JY, Kassmann M, Wang N, Schubert R, Gollasch M. The Role of DPO-1 and XE991-Sensitive Potassium Channels in Perivascular Adipose Tissue-Mediated Regulation of Vascular Tone. Front Physiol. 2016 Aug 4;7:335. doi: 10.3389/fphys.2016.00335. eCollection 2016. PubMed PMID: 27540364; PubMed Central PMCID: PMC4973012.
3: Rode F, Svalø J, Sheykhzade M, Rønn LC. Functional effects of the KCNQ modulators retigabine and XE991 in the rat urinary bladder. Eur J Pharmacol. 2010 Jul 25;638(1-3):121-7. doi: 10.1016/j.ejphar.2010.03.050. Epub 2010 Apr 10. PubMed PMID: 20385123.
4: Fontán-Lozano A, Suárez-Pereira I, Delgado-García JM, Carrión AM. The M-current inhibitor XE991 decreases the stimulation threshold for long-term synaptic plasticity in healthy mice and in models of cognitive disease. Hippocampus. 2011 Jan;21(1):22-32. doi: 10.1002/hipo.20717. PubMed PMID: 19921704.
5: Boehlen A, Kunert A, Heinemann U. Effects of XE991, retigabine, losigamone and ZD7288 on kainate-induced theta-like and gamma network oscillations in the rat hippocampus in vitro. Brain Res. 2009 Oct 27;1295:44-58. doi: 10.1016/j.brainres.2009.08.031. Epub 2009 Aug 20. PubMed PMID: 19699191.
6: Song MK, Cui YY, Zhang WW, Zhu L, Lu Y, Chen HZ. The facilitating effect of systemic administration of Kv7/M channel blocker XE991 on LTP induction in the hippocampal CA1 area independent of muscarinic activation. Neurosci Lett. 2009 Sep 11;461(1):25-9. doi: 10.1016/j.neulet.2009.05.042. Epub 2009 May 20. PubMed PMID: 19463897.
7: Elmedyb P, Calloe K, Schmitt N, Hansen RS, Grunnet M, Olesen SP. Modulation of ERG channels by XE991. Basic Clin Pharmacol Toxicol. 2007 May;100(5):316-22. PubMed PMID: 17448117.
8: Yeung SY, Greenwood IA. Electrophysiological and functional effects of the KCNQ channel blocker XE991 on murine portal vein smooth muscle cells. Br J Pharmacol. 2005 Oct;146(4):585-95. PubMed PMID: 16056238; PubMed Central PMCID: PMC1751185.
9: MacVinish LJ, Guo Y, Dixon AK, Murrell-Lagnado RD, Cuthbert AW. Xe991 reveals differences in K(+) channels regulating chloride secretion in murine airway and colonic epithelium. Mol Pharmacol. 2001 Oct;60(4):753-60. PubMed PMID: 11562437.
10: Wang HS, Brown BS, McKinnon D, Cohen IS. Molecular basis for differential sensitivity of KCNQ and I(Ks) channels to the cognitive enhancer XE991. Mol Pharmacol. 2000 Jun;57(6):1218-23. PubMed PMID: 10825393.