For research use only. Not for therapeutic Use.
ML213 is a selective KV7.2 (KCNQ2) and KV7.4 (KCNQ4) channel opener (EC50 values are 230 and 510 nM for KV7.2 and KV7.4 respectively). ML213 displays > 80-fold selectivity against KV7.1, KV7.3 and KV7.5 in a thallium-based fluorescence assay.
| Catalog Number | R059569 |
| CAS Number | 489402-47-3 |
| Synonyms | N-(2,4,6-Trimethylphenyl)bicyclo[2.2.1]heptane-2-carboxamide; |
| Molecular Formula | C17H23NO |
| Purity | ≥95% |
| Target | Potassium Channel |
| Solubility | Soluble in DMSO > 10 mM |
| Storage | Store at +4C |
| InChI | InChI=1S/C17H23NO/c1-10-6-11(2)16(12(3)7-10)18-17(19)15-9-13-4-5-14(15)8-13/h6-7,13-15H,4-5,8-9H2,1-3H3,(H,18,19) |
| InChIKey | SIQGKPGBLYKQBB-UHFFFAOYSA-N |
| SMILES | CC1=CC(C)=C(NC(C2CC3CCC2C3)=O)C(C)=C1 |
| Reference | </br>1: Rivera-Arconada I, Vicente-Baz J, Lopez-Garcia JA. Targeting Kv7 channels in pain pathways. Oncotarget. 2017 Feb 10. doi: 10.18632/oncotarget.15261. [Epub ahead of print] PubMed PMID: 28199957.</br>2: Abbott GW, Jepps TA. Kcne4 Deletion Sex-Dependently Alters Vascular Reactivity. J Vasc Res. 2016;53(3-4):138-148. PubMed PMID: 27710966; PubMed Central PMCID: PMC5166573.</br>3: Vicente-Baz J, Lopez-Garcia JA, Rivera-Arconada I. Effects of novel subtype selective M-current activators on spinal reflexes in vitro: Comparison with retigabine. Neuropharmacology. 2016 Oct;109:131-8. doi: 10.1016/j.neuropharm.2016.05.025. PubMed PMID: 27263036.</br>4: Chen X, Li W, Hiett SC, Obukhov AG. Novel Roles for Kv7 Channels in Shaping Histamine-Induced Contractions and Bradykinin-Dependent Relaxations in Pig Coronary Arteries. PLoS One. 2016 Feb 4;11(2):e0148569. doi: 10.1371/journal.pone.0148569. PubMed PMID: 26844882; PubMed Central PMCID: PMC4742238.</br>5: Jepps TA, Olesen SP, Greenwood IA, Dalsgaard T. Molecular and functional characterization of Kv 7 channels in penile arteries and corpus cavernosum of healthy and metabolic syndrome rats. Br J Pharmacol. 2016 May;173(9):1478-90. doi: 10.1111/bph.13444. PubMed PMID: 26802314; PubMed Central PMCID: PMC4831315.</br>6: Svalø J, Sheykhzade M, Nordling J, Matras C, Bouchelouche P. Functional and molecular evidence for Kv7 channel subtypes in human detrusor from patients with and without bladder outflow obstruction. PLoS One. 2015 Feb 18;10(2):e0117350. doi: 10.1371/journal.pone.0117350. PubMed PMID: 25692982; PubMed Central PMCID: PMC4333569.</br>7: Brueggemann LI, Haick JM, Cribbs LL, Byron KL. Differential activation of vascular smooth muscle Kv7.4, Kv7.5, and Kv7.4/7.5 channels by ML213 and ICA-069673. Mol Pharmacol. 2014 Sep;86(3):330-41. doi: 10.1124/mol.114.093799. PubMed PMID: 24944189; PubMed Central PMCID: PMC4152906.</br>8: Jepps TA, Bentzen BH, Stott JB, Povstyan OV, Sivaloganathan K, Dalby-Brown W, Greenwood IA. Vasorelaxant effects of novel Kv 7.4 channel enhancers ML213 and NS15370. Br J Pharmacol. 2014 Oct;171(19):4413-24. doi: 10.1111/bph.12805. PubMed PMID: 24909207; PubMed Central PMCID: PMC4209148.</br>9: Svalø J, Bille M, Parameswaran Theepakaran N, Sheykhzade M, Nordling J, Bouchelouche P. Bladder contractility is modulated by Kv7 channels in pig detrusor. Eur J Pharmacol. 2013 Sep 5;715(1-3):312-20. doi: 10.1016/j.ejphar.2013.05.005. PubMed PMID: 23707187.</br>10: Yu H, Wu M, Hopkins C, Engers J, Townsend S, Lindsley C, McManus OB, Li M. A small molecule activator of KCNQ2 and KCNQ4 channels. 2011 Mar 29 [updated 2013 Feb 28]. Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. Available from http://www.ncbi.nlm.nih.gov/books/NBK133435/ PubMed PMID: 23658954.</br>11: Yu H, Wu M, Townsend SD, Zou B, Long S, Daniels JS, McManus OB, Li M, Lindsley CW, Hopkins CR. Discovery, Synthesis, and Structure Activity Relationship of a Series of N-Aryl- bicyclo[2.2.1]heptane-2-carboxamides: Characterization of ML213 as a Novel KCNQ2 and KCNQ4 Potassium Channel Opener. ACS Chem Neurosci. 2011 Oct 19;2(10):572-577. PubMed PMID: 22125664; PubMed Central PMCID: PMC3223964.</br></br> |
