NS1619
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MedKoo CAT#: 522714

CAS#: 153587-01-0

Description: NS1619 is a Bkca opener or large-conductance Ca2+-activated potassium (BKCa, KCa1.1) channel activator. NS1619 pretreatment protects against shock-induced vascular hyporeactivity through PDZ-Rho GEF-RhoA-Rho kinase pathway in rats. NS1619 modulates calcium homeostasis in muscle cells by inhibiting SERCA.NS1619 decreases myogenic and neurogenic contractions of rat detrusor smooth muscle.


Chemical Structure

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NS1619
CAS# 153587-01-0

Theoretical Analysis

MedKoo Cat#: 522714
Name: NS1619
CAS#: 153587-01-0
Chemical Formula: C15H8F6N2O2
Exact Mass: 362.049
Molecular Weight: 362.2314
Elemental Analysis: C, 49.74; H, 2.23; F, 31.47; N, 7.73; O, 8.83

Price and Availability

Size Price Availability Quantity
25.0mg USD 150.0 2 Weeks
50.0mg USD 250.0 2 Weeks
100.0mg USD 450.0 2 Weeks
200.0mg USD 750.0 2 Weeks
500.0mg USD 1650.0 2 Weeks
1.0g USD 2450.0 2 Weeks
2.0g USD 4250.0 2 Weeks
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Synonym: NS1619; NS-1619; NS 1619.

IUPAC/Chemical Name: 1-(2-hydroxy-5-(trifluoromethyl)phenyl)-5-(trifluoromethyl)-1,3-dihydro-2H-benzo[d]imidazol-2-one

InChi Key: YLFMCMWKHSDUCT-UHFFFAOYSA-N

InChi Code: InChI=1S/C15H8F6N2O2/c16-14(17,18)7-1-3-10-9(5-7)22-13(25)23(10)11-6-8(15(19,20)21)2-4-12(11)24/h1-6,24H,(H,22,25)

SMILES Code: O=C1NC2=CC(C(F)(F)F)=CC=C2N1C3=CC(C(F)(F)F)=CC=C3O

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: Soluble in DMSO, not in water

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

Preparing Stock Solutions

The following data is based on the product molecular weight 362.2314 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

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1: McCullough DJ, Vang A, Choudhary G. NS1619-induced vasodilation is enhanced and differentially mediated in chronically hypoxic lungs. Lung. 2014 Oct;192(5):811-7. doi: 10.1007/s00408-014-9633-2. Epub 2014 Aug 8. PubMed PMID: 25104232.

2: Wrzosek A. The potassium channel opener NS1619 modulates calcium homeostasis in muscle cells by inhibiting SERCA. Cell Calcium. 2014 Jul;56(1):14-24. doi: 10.1016/j.ceca.2014.03.005. Epub 2014 Apr 18. PubMed PMID: 24813114.

3: Revermann M, Neofitidou S, Kirschning T, Schloss M, Brandes RP, Hofstetter C. Inhalation of the BK(Ca)-opener NS1619 attenuates right ventricular pressure and improves oxygenation in the rat monocrotaline model of pulmonary hypertension. PLoS One. 2014 Jan 31;9(1):e86636. doi: 10.1371/journal.pone.0086636. eCollection 2014. PubMed PMID: 24497961; PubMed Central PMCID: PMC3909005.

4: Hu Y, Yang G, Xiao X, Liu L, Li T. Bkca opener, NS1619 pretreatment protects against shock-induced vascular hyporeactivity through PDZ-Rho GEF-RhoA-Rho kinase pathway in rats. J Trauma Acute Care Surg. 2014 Feb;76(2):394-401. doi: 10.1097/TA.0b013e3182aa2d98. PubMed PMID: 24398773.

5: Gu YT, Xue YX, Wang YF, Wang JH, ShangGuan QR, Zhang JX, Qin LJ. Role of ROS/RhoA/PI3K/PKB signaling in NS1619-mediated blood-tumor barrier permeability increase. J Mol Neurosci. 2012 Sep;48(1):302-12. doi: 10.1007/s12031-012-9789-2. Epub 2012 May 12. PubMed PMID: 22581438.

6: Soder RP, Petkov GV. Large conductance Ca2+ -activated K+ channel activation with NS1619 decreases myogenic and neurogenic contractions of rat detrusor smooth muscle. Eur J Pharmacol. 2011 Nov 16;670(1):252-9. doi: 10.1016/j.ejphar.2011.08.013. Epub 2011 Sep 2. PubMed PMID: 21914438; PubMed Central PMCID: PMC3193563.

7: Chmielewska L, Malińska D. Cytoprotective action of the potassium channel opener NS1619 under conditions of disrupted calcium homeostasis. Pharmacol Rep. 2011;63(1):176-83. PubMed PMID: 21441626.

8: Liu CY, Li N, Zhao YF, Ma B. [BK(Ca) channel agonist NS1619 and Kv channel antagonist 4-AP on the facial mechanical pain threshold in a rat model of chronic constriction injury of the infraorbital nerve]. Sheng Li Xue Bao. 2010 Oct 25;62(5):441-9. Chinese. PubMed PMID: 20945047.

9: Gáspár T, Domoki F, Lenti L, Katakam PV, Snipes JA, Bari F, Busija DW. Immediate neuronal preconditioning by NS1619. Brain Res. 2009 Aug 18;1285:196-207. doi: 10.1016/j.brainres.2009.06.008. Epub 2009 Jun 11. PubMed PMID: 19523929; PubMed Central PMCID: PMC2744349.

10: Han X, Xi L, Wang H, Huang X, Ma X, Han Z, Wu P, Ma X, Lu Y, Wang G, Zhou J, Ma D. The potassium ion channel opener NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells. Biochem Biophys Res Commun. 2008 Oct 17;375(2):205-9. doi: 10.1016/j.bbrc.2008.07.161. Epub 2008 Aug 13. PubMed PMID: 18706395.

11: Gáspár T, Katakam P, Snipes JA, Kis B, Domoki F, Bari F, Busija DW. Delayed neuronal preconditioning by NS1619 is independent of calcium activated potassium channels. J Neurochem. 2008 May;105(4):1115-28. doi: 10.1111/j.1471-4159.2007.05210.x. Epub 2007 Dec 25. PubMed PMID: 18182041; PubMed Central PMCID: PMC2814534.

12: Saleh SN, Angermann JE, Sones WR, Leblanc N, Greenwood IA. Stimulation of Ca2+-gated Cl- currents by the calcium-dependent K+ channel modulators NS1619 [1,3-dihydro-1-[2-hydroxy-5-(trifluoromethyl)phenyl]-5-(trifluoromethyl)-2H-benzi midazol-2-one] and isopimaric acid. J Pharmacol Exp Ther. 2007 Jun;321(3):1075-84. Epub 2007 Mar 8. PubMed PMID: 17347326.

13: Kuhlmann CR, Trümper JR, Abdallah Y, Wiebke Lüdders D, Schaefer CA, Most AK, Backenköhler U, Neumann T, Walther S, Piper HM, Tillmanns H, Erdogan A. The K+-channel opener NS1619 increases endothelial NO-synthesis involving p42/p44 MAP-kinase. Thromb Haemost. 2004 Nov;92(5):1099-107. PubMed PMID: 15543339.

14: Kicinska A, Szewczyk A. Large-Conductance Potassium Cation Channel Opener NS1619 Inhibits Cardiac Mitochondria Respiratory Chain. Toxicol Mech Methods. 2004;14(1-2):59-61. doi: 10.1080/15376520490257482. PubMed PMID: 20021124.

15: Zhang XF, Gopalakrishnan M, Shieh CC. Modulation of action potential firing by iberiotoxin and NS1619 in rat dorsal root ganglion neurons. Neuroscience. 2003;122(4):1003-11. PubMed PMID: 14643767.

16: Körper S, Nolte F, Rojewski MT, Thiel E, Schrezenmeier H. The K+ channel openers diazoxide and NS1619 induce depolarization of mitochondria and have differential effects on cell Ca2+ in CD34+ cell line KG-1a. Exp Hematol. 2003 Sep;31(9):815-23. PubMed PMID: 12962728.

17: Debska G, Kicinska A, Dobrucki J, Dworakowska B, Nurowska E, Skalska J, Dolowy K, Szewczyk A. Large-conductance K+ channel openers NS1619 and NS004 as inhibitors of mitochondrial function in glioma cells. Biochem Pharmacol. 2003 Jun 1;65(11):1827-34. PubMed PMID: 12781334.

18: Patel HJ, Giembycz MA, Keeling JE, Barnes PJ, Belvisi MG. Inhibition of cholinergic neurotransmission in guinea pig trachea by NS1619, a putative activator of large-conductance, calcium-activated potassium channels. J Pharmacol Exp Ther. 1998 Aug;286(2):952-8. PubMed PMID: 9694955.

19: Khan RN, Smith SK, Ashford ML. Contribution of calcium-sensitive potassium channels to NS1619-induced relaxation in human pregnant myometrium. Hum Reprod. 1998 Jan;13(1):208-13. PubMed PMID: 9512259.

20: Holland M, Langton PD, Standen NB, Boyle JP. Effects of the BKCa channel activator, NS1619, on rat cerebral artery smooth muscle. Br J Pharmacol. 1996 Jan;117(1):119-29. PubMed PMID: 8825352; PubMed Central PMCID: PMC1909362.

(last updated: 4/20/2016)

NS1619

25.0mg / USD 150.0