XE991 HCl
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    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 532978

CAS#: 122955-13-9

Description: XE991, also known as LS190926, is a potent and selective blocker of KCNQ voltage-gated potassium channels. 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).


Price and Availability

Size
Price

5mg
USD 150
Size
Price

10mg
USD 250
Size
Price

25mg
USD 550

XE991 HCl, purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received. Delivery time: overnight (USA/Canada); 3-5 days (worldwide).


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 532978
Name: XE991 HCl
CAS#: 122955-13-9
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


Technical Data

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).

Harmonized System Code:
293490


References

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.