Биологическая активность
VU0134992 (VU 0134992) is a мощный, селективный blocker of the inward rectifier potassium channel Kir4.1 (KCNJ10) с IC50 of 0.97 uM in whole-клетка patch clamp electrophysiology assays; displays 9-fold selectivity for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 uM) at -120 mV; VU0134992 is greater than 30-fold селективный for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2, is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1, and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2 in Tl+ flux assays; causes dose-dependent diuresis, natriuresis, and kaliuresis in rats after oral treatment; VU0134992 represents the first in vivo-active tool compound for probing the therapeutic potential of Kir4.1 as a novel diuretic target for the treatment of hypertension.
Оригинал на английском
VU0134992 (VU 0134992) is a potent, selective blocker of the inward rectifier potassium channel Kir4.1 (KCNJ10) with IC50 of 0.97 uM in whole-cell patch clamp electrophysiology assays; displays 9-fold selectivity for homomeric Kir4.1 over Kir4.1/5.1 concatemeric channels (IC50=9 uM) at -120 mV; VU0134992 is greater than 30-fold selective for Kir4.1 over Kir1.1, Kir2.1, and Kir2.2, is weakly active toward Kir2.3, Kir6.2/SUR1, and Kir7.1, and is equally active toward Kir3.1/3.2, Kir3.1/3.4, and Kir4.2 in Tl+ flux assays; causes dose-dependent diuresis, natriuresis, and kaliuresis in rats after oral treatment; VU0134992 represents the first in vivo-active tool compound for probing the therapeutic potential of Kir4.1 as a novel diuretic target for the treatment of hypertension.
Химические свойства
- CAS №
- 755002-90-5
- Брутто-формула
- C₂₀H₃₁BrN₂O₂
- Мол. масса
- 411.38 г/моль
- SMILES
- O=C(NC1CC(C)(C)NC(C)(C)C1)COC2=CC=C(C(C)C)C=C2Br
- Синонимы
- VU 0134992
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. Kharade SV, et al. Mol Pharmacol. 2018 Jun 12. pii: mol.118.112359.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.