Биологическая активность
Pyr10 is a pyrazole derivative and a селективный TRP cation 3 (TRPC3) ингибитор. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between рецептор-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].
Оригинал на английском
Pyr10 is a pyrazole derivative and a selective TRP cation 3 (TRPC3) inhibitor. Pyr10 inhibits Ca2+ influx in carbachol-stimulated TRPC3-transfected HEK293 cells with an IC50 of 0.72 μM (IC50 of 13.08 μM for store operated Ca2+ entry in BRL-2H3 cells). Pyr10 has the ability to distinguish between receptor-operated TRPC3 and native stromal interaction molecule 1 (STIM1)/Orai1 channels[1].
Химические свойства
- CAS №
- 1315323-00-2
- Брутто-формула
- C₁₈H₁₃F₆N₃O₂S
- Мол. масса
- 449.37 г/моль
- SMILES
- O=S(=O)(NC1C=CC(N2C(C(F)(F)F)=CC(C(F)(F)F)=N2)=CC=1)C1C=CC(C)=CC=1
- Синонимы
- Pyr-10; Pyr 10
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]. Schleifer H, et al. Novel pyrazole compounds for pharmacological discrimination between receptor-operated and store-operated Ca(2+) entry pathways. Br J Pharmacol. 2012 Dec;167(8):1712-1722. [2]. Saliba Y, et al. Transient Receptor Potential Canonical 3 and Nuclear Factor of Activated T Cells C3 Signaling Pathway Critically Regulates Myocardial Fibrosis. Antioxid Redox Signal. 2019 Jun 1;30(16):1851-1879.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.