Биологическая активность
GW274150 is a novel arginine-competitive, NADPH-dependent iNOS ингибитор that has been identified from a series of acetamide amino acids that have a high selectivity for iNOS vs both eNOS (> 260-fold) and nNOS (> 219-fold) and high bioavailability (> 90%) after oral administration.Target: iNOSin vivo: GW274150 demonstrates a narrow neuroprotective therapeutic window against the toxic actions of 6-OHDA. GW274150 administration leads to a dose-dependent decrease in the number of iNOS-positive cells in the SNc of the 6-OHDA-lesioned animals. The iNOS ингибитор GW274150 fails to produce long-term neuroprotection after its withdrawal in the 6-OHDA-lesioned rat. [1]
Оригинал на английском
GW274150 is a novel arginine-competitive, NADPH-dependent iNOS inhibitor that has been identified from a series of acetamide amino acids that have a high selectivity for iNOS vs both eNOS (> 260-fold) and nNOS (> 219-fold) and high bioavailability (> 90%) after oral administration.Target: iNOSin vivo: GW274150 demonstrates a narrow neuroprotective therapeutic window against the toxic actions of 6-OHDA. GW274150 administration leads to a dose-dependent decrease in the number of iNOS-positive cells in the SNc of the 6-OHDA-lesioned animals. The iNOS inhibitor GW274150 fails to produce long-term neuroprotection after its withdrawal in the 6-OHDA-lesioned rat. [1]
Химические свойства
- CAS №
- 210354-22-6
- Брутто-формула
- C₈H₁₇N₃O₂S
- Мол. масса
- 219.30 г/моль
- SMILES
- CC(NCCSCCC(C(=O)O)N)=O
- Синонимы
- GW-274150; GW 274150
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]. Broom L, et al. Neuroprotection by the selective iNOS inhibitor GW274150 in a model of Parkinson disease. Free Radic Biol Med. 2011 Mar 1;50(5):633-40. [2]. Seymour M, et al. Ultrasonographic measures of synovitis in an early phase clinical trial: a double-blind, randomised, placebo and comparator controlled phase IIa trial of GW274150 (a selective inducible nitric oxide synthase inhibitor) in rheumatoid arthritis. Clin Exp Rheumatol. 2012 Mar-Apr;30(2):254-61.
Безопасность и документация
Только для научно-исследовательского применения. Не предназначено для использования у пациентов или в качестве лекарственного средства.