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MedKoo Cat#: 522714 | Name: NS1619
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Description:

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

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

NS1619
NS1619
CAS#153587-01-0

Theoretical Analysis

MedKoo Cat#: 522714

Name: NS1619

CAS#: 153587-01-0

Chemical Formula: C15H8F6N2O2

Exact Mass: 362.0490

Molecular Weight: 362.23

Elemental Analysis: C, 49.74; H, 2.23; F, 31.47; N, 7.73; O, 8.83

Price and Availability

Size Price Availability Quantity
25mg USD 150.00 2 Weeks
50mg USD 250.00 2 Weeks
100mg USD 450.00 2 Weeks
200mg USD 750.00 2 Weeks
500mg USD 1,650.00 2 Weeks
1g USD 2,450.00 2 Weeks
2g USD 4,250.00 2 Weeks
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No Data
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
More Info
Product Data
Product Data
Instruction
View handling instruction
Biological target:
NS-1619 is an opener of large conductance Ca2+-activated K+ (BK) channel.
In vitro activity:
To explore the role of BK channels in regulation of apoptosis in human ovarian cancer cells, the effects of the specific BK channel activator NS1619 on induction of apoptosis in A2780 cells were observed. Following treatment with NS1619, cell proliferation was measured by MTT assay. Apoptosis of A2780 cells pretreated with NS1619 was detected by agarose gel electrophoresis of cellular DNA and flow cytometry. Reference: Biochem Biophys Res Commun. 2008 Oct 17;375(2):205-9. https://pubmed.ncbi.nlm.nih.gov/18706395/
In vivo activity:
Adult male ICR mice were pretreated with the KCa-channel opener NS-1619 either 10 min or 24 h before 30 min of global ischemia and 60 min of reperfusion (I/R) in Langendorff mode. Infusion of NS-1619 (10 microM) for 10 min before I/R led to smaller infarct sizes as compared with the vehicle (DMSO)-treated group (P <0.05). This infarct-limiting effect of NS-1619 was associated with improvement in ventricular functional recovery after I/R. Reference: Am J Physiol Heart Circ Physiol. 2004 Nov;287(5):H2070-7. https://pubmed.ncbi.nlm.nih.gov/15217801/
Solvent mg/mL mM
Solubility
DMF 30.0 82.82
DMSO 42.3 117.11
DMSO:PBS (pH 7.2) (1:1) 0.5 1.38
Ethanol 46.1 127.19
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 362.23 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
Formulation protocol:
1. 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. PMID: 18706395. 2. Huang Y, Lau CW, Ho IH. NS 1619 activates Ca2+-activated K+ currents in rat vas deferens. Eur J Pharmacol. 1997 Apr 23;325(1):21-7. doi: 10.1016/s0014-2999(97)00102-7. PMID: 9151934. 3. Gao Y, Zhang H, Li X, Li L, Li F, Li T, Peng R, Wang C, Wang J, Liu X, Zhang S, Zhang J. NS1619 Alleviate Brain-Derived Extracellular Vesicle-Induced Brain Injury by Regulating BKca Channel and Nrf2/HO-1/NF-ĸB Pathway. Oxid Med Cell Longev. 2022 Nov 23;2022:2257427. doi: 10.1155/2022/2257427. PMID: 36466093; PMCID: PMC9711983. 4. Wang X, Yin C, Xi L, Kukreja RC. Opening of Ca2+-activated K+ channels triggers early and delayed preconditioning against I/R injury independent of NOS in mice. Am J Physiol Heart Circ Physiol. 2004 Nov;287(5):H2070-7. doi: 10.1152/ajpheart.00431.2004. Epub 2004 Jun 24. PMID: 15217801.
In vitro protocol:
1. 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. PMID: 18706395. 2. Huang Y, Lau CW, Ho IH. NS 1619 activates Ca2+-activated K+ currents in rat vas deferens. Eur J Pharmacol. 1997 Apr 23;325(1):21-7. doi: 10.1016/s0014-2999(97)00102-7. PMID: 9151934.
In vivo protocol:
1. Gao Y, Zhang H, Li X, Li L, Li F, Li T, Peng R, Wang C, Wang J, Liu X, Zhang S, Zhang J. NS1619 Alleviate Brain-Derived Extracellular Vesicle-Induced Brain Injury by Regulating BKca Channel and Nrf2/HO-1/NF-ĸB Pathway. Oxid Med Cell Longev. 2022 Nov 23;2022:2257427. doi: 10.1155/2022/2257427. PMID: 36466093; PMCID: PMC9711983. 2. Wang X, Yin C, Xi L, Kukreja RC. Opening of Ca2+-activated K+ channels triggers early and delayed preconditioning against I/R injury independent of NOS in mice. Am J Physiol Heart Circ Physiol. 2004 Nov;287(5):H2070-7. doi: 10.1152/ajpheart.00431.2004. Epub 2004 Jun 24. PMID: 15217801.
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)