459429-39-1
459429-39-1 structure
- Name: SB 452533
- Chemical Name: 1-(2-Bromophenyl)-3-{2-[ethyl(3-methylphenyl)amino]ethyl}ure
- CAS Number: 459429-39-1
- Molecular Formula: C18H22BrN3O
- Molecular Weight: 376.29
- Catalog: Signaling Pathways Membrane Transporter/Ion Channel TRP Channel
- Create Date: 2017-09-06 22:34:08
- Modify Date: 2025-08-25 11:35:38
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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 | |
| 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 |
| 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 |
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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 |
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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 |
| Precursor 3 | |
|---|---|
| DownStream 0 | |