SB 452533

Names

[ CAS No. ]:
459429-39-1

[ Name ]:
SB 452533

Biological Activity

[Description]:

SB 452533 is a potent and selective TRPV1 antagonist with the pKb of 7.8[1].

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> TRP Channel

Research Areas >> Inflammation/Immunology

[In Vitro]

SB 452533 is potent as an antagonist at the cloned recombinant rat TRPV1 receptor in HEK293 cells with a pKb of 7.7 and a pIC50 of 7.0[1]. SB-452533 reduces phosphorylation of CAMKK2 and AMPK[2]. Western Blot Analysis[2] Cell Line: Skeletal muscle (C2C12) cells Concentration: 0, 50, 100, 200, and 400 μM Incubation Time: 30 minutes; followed by 200 μM Capsaicin treatment for another 30 min. Result: Significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2.

[In Vivo]

Capsaicin (Cap; small dose 2 mg/kg) significantly reduces Bleomycin-induced pulmonary fibrosis in mice. SB-452533 abolishes the effects of small dose Cap[3]. Animal Model: BALB/c mice bearing pulmonary fibrosis model[3] Dosage: 2.5 mg/kg Administration: Treatment received daily drug via subcutaneous injection for 21 days Result: The effect (reduced Bleomycin-induced pulmonary fibrosis) of Cap were abolished in the presence of SB-452533.

[References]

[1]. Harshad K Rami, et al. Discovery of small molecule antagonists of TRPV1. Bioorg Med Chem Lett. 2004 Jul 16;14(14):3631-4.

[2]. 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.

[3]. 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.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₈H₂₂BrN₃O

[ Molecular Weight ]:
376.29

[ Exact Mass ]:
375.09500

[ PSA ]:
47.86000

[ LogP ]:
4.68290

[ Storage condition ]:
-20°C

Safety Information

[ Symbol ]:

GHS07, GHS09

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302-H410

[ Precautionary Statements ]:
P273-P501

[ RIDADR ]:
UN 3077 9 / PGIII

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds

The content on this webpage is sourced from various professional data sources. If you have any questions or concerns regarding the content, please feel free to contact service1@chemsrc.com.