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 longlasting nonpeptide bradykinin B2 (BK2) receptor antagonist. Fasitibant chloride hydrochloride has proinflammatory effects and can be used for the research of osteoarthritis and rheumatoid arthritis, et al.

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

Size Stock
100 mg   Get quote  
250 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Other Forms of Fasitibant chloride hydrochloride:

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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

IC50 & Target

IC50: Bradykinin B2 Receptor [1]

In Vitro

Fasitibant exhibits high affinity for the BK binding site, pKi values 8.9 in intact cells and 10.17-Ki 0.067 nM in cell membrane in synovial cells.Fasitibant also echibits high antagonist potency in blocking the effects produced by BK in these cells both after 1 h-(phospholipase C activation, pKB=9.9) and 24 h-incubation (release of IL-6 and IL-8, pIC50 8.1 and 8.4, respectively)[1].
Fasitibant chloride hydrochloride (1 μM; 30 min preincubation before BK) prevents BK-induced sustained production of PGE2 and transient COX-2 gene expression in synovial fibroblasts[1].
Fasitibant chloride hydrochloride completely prevents the potentiating effect of BK on IL-1β, both in terms of PGE2 production and COX-2 gene expression in synovial fibroblasts[1].

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

In Vivo

Fasitibant chloride hydrochloride (injection into the knee joint ;100 µg per knee; combines with dexamethasone) is more effective than each agent administered alone in inhibiting knee joint inflammation and release of inflammatory mediators. Fasitibant chloride alone reaches a comparable maximal inhibitory effect of about 40–45% on the carrageenan-induced joint pain, however, Combination administration achieves full inhibition in male Wistar rats  with inflammatory arthritis[2].

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.

869880-33-1

SMILES

O=C(N(CC1)CCN1C([[email protected]@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.

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Fasitibant chlorideMEN16132MEN 16132MEN-16132Bradykinin Receptorsynovial fibroblastosteoarthritisRheumatoid arthritisIL-6Inhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Fasitibant chloride hydrochloride
Cat. No.:
HY-106277A
Quantity:
MCE Japan Authorized Agent: