Safotibant  (Synonyms: LF22-0542)

Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with K_i 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].

Safotibant (10 mg/kg, s.c., 3 times a day for 8 days) exhibits analgesic property against bone cancer-induced pain in osteolytic sarcoma xenograft C3H/HeJ mice model, without affecting disease progression^[1].
Safotibant (one eye drop application, twice a day for 7 days) inhibits expressions of inflammatory mediators B1R, iNOS, IL-1β, COX-2, VEGF-R2 and HIF-1α, reverses diabetes-induced retinal inflammation and oxidative stress in streptozotocin (STZ)-diabetic Wistar rats model^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

502.63

C₂₅H₃₄N₄O₅S

633698-99-4

O=C(COCCN(S(=O)(C1=C(C)C=C(OC)C=C1C)=O)C)N(CC2=CC=C(C3=NCCN3)C=C2)C

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• [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.  [Content Brief]

  [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.  [Content Brief]