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Fasitibant chloride

Cat. No. M27862
Fasitibant chloride Structure
Synonym:

MEN16132 free base

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Biological Activity

Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model.

Chemical Information
Molecular Weight 800.23
Formula C36H49Cl3N6O6S
CAS Number 1157852-02-2
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Rose-Marie Catalioto, et al. Biochem Pharmacol. Enhanced Ca(2+) response and stimulation of prostaglandin release by the bradykinin B2 receptor in human retinal pigment epithelial cells primed with proinflammatory cytokines

[2] Rose-Marie Catalioto, et al. Biochem Pharmacol. Characterization of a novel proinflammatory effect mediated by BK and the kinin B₂ receptor in human preadipocytes

[3] Claudio Valenti, et al. Br J Pharmacol. Fasitibant chloride, a kinin B₂ receptor antagonist, and dexamethasone interact to inhibit carrageenan-induced inflammatory arthritis in rats

[4] Kenneth J Broadley, et al. J Pharmacol Exp Ther. Bradykinin-induced lung inflammation and bronchoconstriction: role in parainfluenze-3 virus-induced inflammation and airway hyperreactivity

[5] Cecilia Cialdai, et al. J Pharmacol Exp Ther. Effect of Intra-articular 4-(S)-amino-5-(4-{4-[2,4-dichloro-3-(2,4-dimethyl-8-quinolyloxymethyl)phenylsulfonamido]-tetrahydro-2H-4-pyranylcarbonyl} piperazino)-5-oxopentyl](trimethyl)ammonium chloride hydrochloride (MEN16132), a kinin B2 receptor antagoni䲧瘀Ỵ瘁㧀痿羹皘的㸈ܯŘܯð�皚嶁皖Ѐ瑖犨䀹蹞߸ܯð䀸߸彿犩奋犩巫犩鐚߸

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Keywords: Fasitibant chloride, MEN16132 free base supplier, Bradykinin Receptor, inhibitors, activators


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