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Art. -Nr.: HY-106277

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Fasitibant free base

1 Cited Publications

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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. Nr.: 869939-83-3
Formel: C₃₆H₄₉Cl₂N₆O₆S⁺
Molecular Weight:764.78

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

Data Sheet (269 KB)

Fasitibant free base Chemical Structure

CAS. Nr.: 869939-83-3

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- In Vitro
- In Vivo
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Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

Bradykinin B2 Receptor (B2R)

Alle Bradykinin Receptor Isoform-spezifische Produkte anzeigen :

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. Nr. 869939-83-3
Molecular Weight 764.78
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Handling Instructions (2659 KB)

Verweise

[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]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

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

Alle Bradykinin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Reinheit & Dokumentation

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Fasitibant free base Related Classifications

Art. -Nr.: HY-106277