1. GPCR/G Protein
  2. Bradykinin Receptor
  3. Fasitibant chloride hydrochloride

Fasitibant chloride hydrochloride  (Synonyms: MEN16132)

Cat. No.: HY-106277A
Handling Instructions

Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis.

For research use only. We do not sell to patients.

Fasitibant chloride hydrochloride Chemical Structure

Fasitibant chloride hydrochloride Chemical Structure

CAS No. : 869880-33-1

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Description

Fasitibant chloride hydrochloride (MEN16132) is a potent, selective, high affinity, and long-lasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis[1].

IC50 & Target

Bradykinin B2 Receptor (B2R)

 

In Vitro

Fasitibant chloride hydrochloride (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 chloride hydrochloride (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.

Animal Model: Male wistar rats with inflammatory arthritis[2]
Dosage: 100 µg per knee
Administration: Injection into the knee joint; 100 µg per knee; combines with dexamethasone
Result: Was more effective than each drug administered alone in inhibiting knee joint inflammation.
Reduced joint pain and diminished joint oedema.
Animal Model: Male Wistar rats with inflammatory arthritis[2]
Dosage: 100 µg per knee
Administration: Injection into the knee joint; 100 µg per knee; combines with dexamethasone
Result: Was more effective than each drug administered alone in inhibiting knee joint inflammation.
Reduced joint pain and diminished joint oedema.
Clinical Trial
Molecular Weight

836.70

Formula

C36H50Cl4N6O6S

CAS No.
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.[Cl-].Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Fasitibant chloride hydrochloride 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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Fasitibant chloride hydrochloride
Cat. No.:
HY-106277A
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