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| 25mg |
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Purity: ≥98%
NS-1619 is a selective activator of the large conductance Ca2+-activated K+-channel (BKCa, KCa1.1). 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. NS-1619 induced concentration-dependent activation of BKCa channels with a calculated EC50 of 32 µM. The NS 1619-induced activity was dependent on the presence of free Ca2+ at the intracellular surface, but was not associated with a change in channel voltage sensitivity. NS 1619 (50 µM) inhibited the noradrenaline-induced contraction.
| ln Vitro |
A2780 cell proliferation is inhibited by NS1619 (5, 10, 30, 50, and 100 μM) in a dosage and time dependent manner (IC50=31.1 μM for 48 h pretreatment)[2]. Human ovarian cancer cells A2780 show an augmenting effect of NS1619 (30 μM) on whole cell IK[2]. In A2780 cells, NS1619 (10, 30, 50, and 100 μM) raises the levels of the proteins p53, p21Cip1, and Bax[2]. A2780 cells' DNA content dramatically dropped 36 and 48 hours after pretreatment. Tumor cells die as a result of DNA deterioration[2].
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| ln Vivo |
In mouse hearts, KCa channel opening with NS-1619 (1 mg/kg; ip) can postpone protection[3].
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| Cell Assay |
Cell Viability Assay[2]
Cell Types: The human ovarian cancer cell line A2780 Tested Concentrations: 5, 10, 30, 50, and 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited cell growth in a time and concentration-dependent manner, IC50=31.1 μM. Proliferation was Dramatically inhibited at concentrations of NS1619 higher than 10 μM. Western Blot Analysis[2] Cell Types: A2780 cells Tested Concentrations: 0, 5, 10, 30, 50, and 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: Expression of p53, p21, and Bax in A2780 cells was Dramatically increased in comparison with control. Western Blot Analysis[2] Cell Types: A2780 cells Tested Concentrations: 30 μM Incubation Duration: 36 and 48 hrs (hours) Experimental Results: DNA content of A2780 cells was Dramatically diminished after 36 and 48 h of pretreatment. The breakdown of DNA results in death of the tumor cells. |
| Animal Protocol |
Animal/Disease Models: Adult male outbred ICR mice[3]
Doses: 1 mg/kg Route of Administration: Pretreated ip 24 h before I/R Experimental Results: Pretreatment induced delayed protection 24 h later. Resulted in significant cardioprotection 24 h later, ie, infarct size was decreased from 38.8 ± 3.7% to 19.8 ± 2.9%. |
| References |
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| Additional Infomation |
NS 1619 is a member of the class of benzimidazoles that is 1,3-dihydro-2H-benzimidazol-2-one in which the hydrogens at positions 1 and 5 are replaced are replaced by 2-hydroxy-5-(trifluoromethyl)phenyl and trifluoromethyl groups, respectively. It is an opener/activator of the large-conductance calcium-activated potassium channel (Bkca). It has a role as a potassium channel opener. It is a member of benzimidazoles, a member of phenols and a member of (trifluoromethyl)benzenes.
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| Molecular Formula |
C15H8F6N2O2
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| Molecular Weight |
362.23
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| Exact Mass |
362.049
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| CAS # |
153587-01-0
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| Related CAS # |
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| PubChem CID |
4552
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| Appearance |
White to off-white solid powder
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| Density |
1.563g/cm3
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| Melting Point |
234 °C(dec.)
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| Index of Refraction |
1.538
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| LogP |
4.062
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
25
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| Complexity |
523
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
YLFMCMWKHSDUCT-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
3-[2-hydroxy-5-(trifluoromethyl)phenyl]-6-(trifluoromethyl)-1H-benzimidazol-2-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7607 mL | 13.8034 mL | 27.6068 mL | |
| 5 mM | 0.5521 mL | 2.7607 mL | 5.5214 mL | |
| 10 mM | 0.2761 mL | 1.3803 mL | 2.7607 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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