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Fasitibant free base

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Fasitibant (free base) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B₂ (BK₂) receptor antagonist. Fasitibant (free base) has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis.

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CAS No.: 869939-83-3
Formule: C₃₆H₄₉Cl₂N₆O₆S⁺
Masse moléculaire:764.78

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Data Sheet (269 KB)

Fasitibant free base Chemical Structure

CAS No.: 869939-83-3

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Description

IC₅₀ & Target^[1]

Bradykinin B2 Receptor (B2R)

Voir tous les produits spécifiques à Isoform Bradykinin Receptor :

In Vitro

Fasitibant (free base) (1 µM; 30 min) reduces BK induced PGE₂ formation and COX-2 gene expression in synovial cells^[1].

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

In Vivo

Fasitibant (free base) (100 µg; knee injection; single dose) significantly reduces the release of IL-1b, IL-6, GRO/PINC-1 synovial cytokines, the formation of PGE metabolites, the activity of myeloperoxidase (MPO) induced by Carrageenan (HY-125474) in rats, and the effect was more significant when combined with Dexamethasone (HY-14648)^[2].

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

Chemical Information

CAS No. 869939-83-3
Masse moléculaire 764.78
Formule C₃₆H₄₉Cl₂N₆O₆S⁺
SMILES

O=C(N(CC1)CCN1C([C@@H](N)CCC[N+](C)(C)C)=O)C2(CCOCC2)N[S](=O)(C(C=CC(Cl)=C3COC4=CC=CC(C(C)=C5)=C4N=C5C)=C3Cl)=O
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Room temperature in continental US; may vary elsewhere.
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Please store the product under the recommended conditions in the Certificate of Analysis.

Publications (1)

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Nat Commun

Endothelial Sp1/Sp3 are essential to the effect of captopril on blood pressure in male mice. [Abstract]

2023 Sep 21;14(1):5891. PMID: 37735515

Pureté et documentation

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Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (269 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. S Meini, et al. Fasitibant prevents the bradykinin and interleukin 1β synergism on prostaglandin E₂ release and cyclooxygenase 2 expression in human fibroblast-like synoviocytes. Naunyn Schmiedebergs Arch Pharmacol. 2012 Aug;385(8):777-86. [Content Brief]

[2]. Claudio Valenti, et al. Fasitibant chloride, a kinin B₂ receptor antagonist, and dexamethasone interact to inhibit carrageenan-induced inflammatory arthritis in rats. Br J Pharmacol. 2012 Jun;166(4):1403-10. [Content Brief]

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1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Fasitibant free base

1 Cited Publications

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Fasitibant free base

Publications Citing Use of MedChemExpress (MCE) Fasitibant free base

Voir tous les produits spécifiques à Isoform Bradykinin Receptor

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Fasitibant free base Related Classifications

Cat. No.: HY-106277