SB 452533

Modify Date: 2024-01-28 19:29:50

SB 452533 structure	Common Name	SB 452533
	CAS Number	459429-39-1	Molecular Weight	376.29
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₈H₂₂BrN₃O	Melting Point	N/A
	MSDS	Chinese USA	Flash Point	N/A
	Symbol	GHS07, GHS09	Signal Word	Warning

Use of SB 452533

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

Name	1-(2-Bromophenyl)-3-{2-[ethyl(3-methylphenyl)amino]ethyl}ure

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.

Molecular Formula	C₁₈H₂₂BrN₃O
Molecular Weight	376.29
Exact Mass	375.09500
PSA	47.86000
LogP	4.68290
Storage condition	-20°C

Symbol	GHS07, GHS09
Signal Word	Warning
Hazard Statements	H302-H410
Precautionary Statements	P273-P501
RIDADR	UN 3077 9 / PGIII

N-Ethyl-3-methy...

CAS#:102-27-2

SB 452533

CAS#:459429-39-1

Literature: Rami, Harshad K.; Thompson, Mervyn; Wyman, Paul; Jerman, Jeffrey C.; Egerton, Julie; Brough, Stephen; Stevens, Alexander J.; Randall, Andrew D.; Smart, Darren; Gunthorpe, Martin J.; Davis, John B. Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 14 p. 3631 - 3634