Safotibant
Based on 1 Customer Validation
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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- Pureté: 98.88%
- CAS No.: 633698-99-4
- Formule: C25H34N4O5S
- Masse moléculaire:502.63
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Stockage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Voir tous les produits spécifiques à Isoform Bradykinin Receptor
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Activité biologique
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.
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Animal Model:Osteolytic sarcoma xenograft C3H/HeJ mice model[1]
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Dosage:10 mg/kg
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Administration:s.c., 3 times a day for 8 days
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Result:Decreased numbers of flinching and time spent on spontaneous guarding.
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Animal Model:Streptozotocin (STZ)-diabetic Wistar rats model[2]
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Dosage:One eye drop
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Administration:On eyes application, twice a day for 7 days
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Result:Reversed retinal vascular hyperpermeability, decreased levels of retinal leukostasis and superoxide anion in 3 retinal nuclear layers.
Chemical Information
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CAS No. 633698-99-4
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Appearance Oil
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Masse moléculaire 502.63
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Formule C25H34N4O5S
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Color White to light yellow
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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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Synonyms
LF22-0542
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
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Fiche technique (269 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Safotibant Related Classifications
HY-100827 Related Classifications
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