| Field | Specification |
|---|---|
| Target | |
| Alternative names | MEN16132 |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C36H50Cl4N6O6S |
| SMILES | |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Fasitibant chloride hydrochloride, also known as MEN16132, is a potent, selective, high-affinity, long-lasting nonpeptide antagonist of the bradykinin B2 (BK2) receptor. It has proinflammatory effects and can be used for research on osteoarthritis and rheumatoid arthritis[1]. It has the molecular formula C36H50Cl4N6O6S and a molecular weight of 836.70 g/mol.
Physical & Chemical Properties
| CAS Number | 869880-33-1 |
|---|---|
| Molecular Formula | C36H50Cl4N6O6S |
| Molecular Weight | 836.70 g/mol |
| 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 |
| Target | Bradykinin B2 Receptor (B2R) |
| Signaling Pathway | GPCR/G Protein |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with your institution's chemical hygiene plan.
In Vitro
In synovial cells, Fasitibant chloride hydrochloride (1 μM; 30 min) lowers BK induced PGE2 formation and COX-2 gene expression[1].
In Vivo
In rats, a single knee injection of Fasitibant chloride hydrochloride (100 μg) significantly lowers Carrageenan-induced release of the synovial cytokines IL-1b, IL-6, GRO/PINC-1, formation of PGE metabolites, and myeloperoxidase (MPO) activity; the effect is more pronounced when combined with Dexamethasone[2].
| 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. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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