Биологическая активность
T16Ainh-A01 is an ингибитор of the calcium-activated chloride channel TMEM16A, inhibits Ca2+-activated Cl− channel (CACC) activity in TMEM16A-transfected FRT cells с IC50 of 1 uM; T16Ainh-A01 (1-30 uM) inhibited single calcium (Ca2+)-activated chloride (Cl−) channels and whole клетка currents activated by 500 nM free Ca2+; T16Ainh-A01 relaxed mouse thoracic aorta pre-contracted with methoxamine with an IC50 of 1.6 uM and suppressed the methoxamine concentration-effect curve; blocks calcium-activated chloride channels in vascular smooth muscle cells and relaxes murine and human blood vessels.
Оригинал на английском
T16Ainh-A01 is an inhibitor of the calcium-activated chloride channel TMEM16A, inhibits Ca2+-activated Cl− channel (CACC) activity in TMEM16A-transfected FRT cells with IC50 of 1 uM; T16Ainh-A01 (1-30 uM) inhibited single calcium (Ca2+)-activated chloride (Cl−) channels and whole cell currents activated by 500 nM free Ca2+; T16Ainh-A01 relaxed mouse thoracic aorta pre-contracted with methoxamine with an IC50 of 1.6 uM and suppressed the methoxamine concentration-effect curve; blocks calcium-activated chloride channels in vascular smooth muscle cells and relaxes murine and human blood vessels.
Химические свойства
- CAS №
- 552309-42-9
- Брутто-формула
- C₁₉H₂₀N₄O₃S₂
- Мол. масса
- 416.51 г/моль
- SMILES
- COC1C=CC(C2=CSC(NC(CSC3NC(C)=C(CC)C(=O)N=3)=O)=N2)=CC=1
- Синонимы
- T16Ainh-A01|
3D-структура молекулы
Вращайте мышью · Колесо — масштаб
Хранение и физические свойства
- Условия хранения
- 2 года -20°C порошок, 2 недели 4°C в ДМСО, 6 мес. -80°C в ДМСО Publication: 1. Davis AJ, et al. Br J Pharmacol. 2013 Feb;168(3):773-84. 2. Mazzone A, et al. Biochem Biophys Res Commun. 2012 Oct 19;427(2):248-53. 3. Forrest AS, Am J Physiol Cell Physiol. 2012 Dec 15;303(12):C1229-43. 4. Namkung W, et al. J Biol Chem. 2011 Jan 21;286(3):2365-74.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.