1. GPCR/G Protein
  2. Bradykinin Receptor
  3. Safotibant

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.

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Safotibant Chemical Structure

Safotibant Chemical Structure

CAS No. : 633698-99-4

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Description

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, 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.

Animal Model: Osteolytic sarcoma xenograft C3H/HeJ mice model[1]
Dosage: 10 mg/kg
Administration: s.c., 3 times a day for 8 days
Result: Decreased numbers of flinching and time spent on spontaneous guarding.
Animal Model: Streptozotocin (STZ)-diabetic Wistar rats model[2]
Dosage: One eye drop
Administration: On eyes application, twice a day for 7 days
Result: Reversed retinal vascular hyperpermeability, decreased levels of retinal leukostasis and superoxide anion in 3 retinal nuclear layers.
Molecular Weight

502.63

Formula

C25H34N4O5S

CAS No.
SMILES

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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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Safotibant Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Safotibant
Cat. No.:
HY-100827
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