Safotibant_product_DataBase

Bioactivity	Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model[1][2].
In Vivo	Safotibant (10 mg/kg，皮下注射，每天 3 次，持续 8 天) 在 C3H/HeJ 小鼠溶骨性肉瘤异种移植模型中，对骨癌引发的疼痛具有镇痛活性，且不影响疾病进程[1]。Safotibant (一滴滴眼液，每天两次，持续 7 天) 在 streptozotocin (STZ) 诱导的大鼠糖尿病模型中，抑制炎症介质 B1R、iNOS、IL-1β、COX-2、VEGF-R2 和 HIF-1α 的表达，减轻糖尿病引发的视网膜炎症和氧化应激反应[2]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
CAS	633698-99-4
Formula	C25H34N4O5S
Molar Mass	502.63
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Sevcik MA, et al., Analgesic efficacy of bradykinin B1 antagonists in a murine bone cancer pain model. J Pain. 2005 Nov;6(11):771-5. [2]. Pouliot M, et al., Ocular application of the kinin B1 receptor antagonist LF22-0542 inhibits retinal inflammation and oxidative stress in streptozotocin-diabetic rats. PLoS One. 2012;7(3):e33864.

PeptideDB