| Bioactivity | NS-1619 is an opener of large conductance Ca2+-activated K+ (BK) channel. NS-1619 is a highly effective relaxant with an EC50 of about 10 – 30 μM in several smooth muscles of blood vessels and other tissues[1]. NS1619 inhibits proliferation and induces apoptosis in A2780 ovarian cancer cells[2]. | ||||||||||||
| Invitro | NS1619 (5, 10, 30, 50, and 100 μM) inhibits the proliferation of A2780 cells in a dosage and time dependent manner IC50=31.1 μM for 48 h pretreatment[2].NS1619 (30 μM) exhibits augmenting effect on whole cell IK in human ovarian cancer cells A2780[2].NS1619 (10, 30, 50, and 100 μM) increases levels of p53, p21Cip1 and Bax proteins in A2780 cells[2].DNA content of A2780 cells was significantly decreased after 36 and 48 h of pretreatment. The breakdown of DNA results in death of the tumor cells[2]. Cell Viability Assay[2] Cell Line: | ||||||||||||
| In Vivo | Opening of KCa channels with NS-1619 (1 mg/kg; i.p.) can delay protection in mouse hearts[3]. Animal Model: | ||||||||||||
| Name | NS-1619 | ||||||||||||
| CAS | 153587-01-0 | ||||||||||||
| Formula | C15H8F6N2O2 | ||||||||||||
| Molar Mass | 362.23 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. H Yamamura, et al. BK channel activation by NS-1619 is partially mediated by intracellular Ca2+ release in smooth muscle cells of porcine coronary artery. Br J Pharmacol. 2001 Feb;132(4):828-34. [2]. Xiaobing Han,et al. 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. [3]. Xiaoyin Wang, et al. 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. |