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SB 452533

Catalog No. T23322   CAS 459429-39-1

SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).

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SB 452533 Chemical Structure
SB 452533, CAS 459429-39-1
Pack Size Availability Price/USD Quantity
1 mg In stock $ 41.00
2 mg In stock $ 59.00
5 mg In stock $ 97.00
10 mg In stock $ 163.00
25 mg In stock $ 322.00
50 mg In stock $ 497.00
100 mg In stock $ 723.00
500 mg In stock $ 1,520.00
1 mL * 10 mM (in DMSO) In stock $ 128.00
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Purity: 98.52%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).
Targets&IC50 TRPV1:7.8(pKb)
In vitro SB 452533 significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2[1].
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[2].
Molecular Weight 376.29
Formula C18H22BrN3O
CAS No. 459429-39-1

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 50 mg/ml(132.876 mM)

TargetMolReferences and Literature

1. Parisa Vahidi Ferdowsi, et al. TRPV1 Activation by Capsaicin Mediates Glucose Oxidation and ATP Production Independent of Insulin Signalling in Mouse Skeletal Muscle Cells. Cells. 2021 Jun 21;10(6):1560. 2. Lin Ming Lu, et al. Effect of small dose capsaicin for treatment of pulmonary fibrosis in mice and its mechanism. Zhongguo Ying Yong Sheng Li Xue Za Zhi. 2020 May;36(3):216-222. 3. Harshad K Rami, et al. Discovery of small molecule antagonists of TRPV1. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3631-4.

Related compound libraries

This product is contained In the following compound libraries:
Neuronal Signaling Compound Library Bioactive Compounds Library Max Inhibitor Library Bioactive Compound Library Anti-Cancer Compound Library Ion Channel Inhibitor Library ReFRAME Related Library

Related Products

Related compounds with same targets
cim0216 Vanilloid receptor antagonist 1 TRPA1 Antagonist 1 LASSBio-1135 ML329 Rosiglitazone maleate Evifacotrep BCTC

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Keywords

SB 452533 459429-39-1 Membrane transporter/Ion channel TRP/TRPV Channel ATP glucose oxidation inhibit ERK1/2 TRPV1 pulmonary TRP Channel fibrosis CAMKK2 skeletal muscle capsaicin SB452533 Inhibitor SB-452533 Transient receptor potential channels inhibitor

 

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