SB 452533

SKU: orb1305665

Description

SB 452533 is a potent and selective vanilloid receptor 1 (TRPV1) antagonist with a pKb of 7.8. This compound is a valuable research tool for studying TRPV1-mediated pathways in pain, inflammation, and neurogenic disorders in both cellular and animal models.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 459429-39-1
• MW: 376.29
• Purity: 99.87% (May vary between batches)
• Formula: C₁₈H₂₂BrN₃O
• SMILES: CCN(CCNC(=O)Nc1ccccc1Br)c1cccc(C)c1
• Target: TRP/TRPV Channel
• Solubility: Ethanol:< 1 mg/mL (insoluble or slightly soluble);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.32 mM);DMSO:60 mg/mL (159.45 mM)

Bioactivity

• Target IC50:
  TRPV1:7.8(pKb)
• In Vivo:
  Small dose Cap significantly reduced bleomycin-induced pulmonary fibrosis in mice and obviously reversed alveolar epithelial cells epithelial-mesenchymal transition (EMT) (the expression of E-cadherin and ZO-1 were increased(P＜0.05 or P＜0.01)and the expression of α-SMA and Vimentin were decreased (P＜0.05 or P＜0.01) after drugs treatment for 21 day, concomitantly with the increase the expressions of TRPV1 and CGRP (P＜0.05 or P＜0.01), and inhibiting ERK1/2 phosphorylation and eIF3a expression (P＜0.05 or P＜0.01). These effects of small dose Cap were abolished in the presence of TRPV1 receptor antagonist SB 452533.
• In Vitro:
  SB 452533 significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CAMKK2, capsaicin, ATP, inhibit, Inhibitor, ERK1/2, glucose oxidation, fibrosis, TRPVChannel, TRPV1, TRPV Channel, TRPChannel, TRP Channel, Transient receptor potential channels, skeletal muscle, pulmonary, SB 452533, SB452533, SB-452533

Compound Identifiers

PubChem CID

9842609