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SB 452533
CAS No. 459429-39-1
SB 452533( —— )
Catalog No. M27705 CAS No. 459429-39-1
SB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 1 mL x 10 mM in DMSO | 67 | In Stock |
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| 2MG | 33 | In Stock |
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| 5MG | 55 | In Stock |
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| 10MG | 93 | In Stock |
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| 25MG | 183 | In Stock |
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| 50MG | 277 | In Stock |
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| 100MG | 403 | In Stock |
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| 200MG | 573 | In Stock |
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| 500MG | Get Quote | In Stock |
|
| 1G | Get Quote | In Stock |
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Biological Information
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Product NameSB 452533
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NoteResearch use only, not for human use.
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Brief DescriptionSB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).
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DescriptionSB 452533 is an antagonist of the vanilloid receptor 1(pKb: 7.8).(In Vitro):SB 452533 significantly reduced Capsaicin-induced phosphorylation of AMPK and CAMKK2.(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.
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In VitroSB 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. SB-452533 reduces phosphorylation of CAMKK2 and AMPK. Western Blot Analysis 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.
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In VivoCapsaicin (Cap; small dose 2 mg/kg) significantly reduces Bleomycin-induced pulmonary fibrosis in mice. SB-452533 abolishes the effects of small dose Cap. Animal Model:BALB/c mice bearing pulmonary fibrosis model 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.
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Synonyms——
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PathwayMembrane Transporter/Ion Channel
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TargetTRP/TRPV Channel
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RecptorNF-κB|p65
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Research Area——
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Indication——
Chemical Information
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CAS Number459429-39-1
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Formula Weight376.298
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Molecular FormulaC18H22BrN3O
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 100 mg/mL (265.75 mM)
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SMILESCCN(CCNC(=O)Nc1ccccc1Br)c1cccc(C)c1
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
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Pyr6
Pyr6 is a selective TRPC3 inhibitor with IC50 of 0.49 uM(Ca2+ influx inhibition in thapsigargin depleted native RBL-2H3 cells).Pyr6 is an inhibitor of Ca2+ entry, which displays higher potency to inhibit Ca2+ entry mediated by CRAC channel than by TRPC3.Pyr3 is selective inhibitor of TRPC3, inhibited Orai1- and TRPC3-mediated Ca(2+) entry and currents as well as mast cell activation with similar potency.?
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EIPA
EIPA (L593754, MH 12-43) is a TRPP3 channel inhibitor (IC50: 10.5 μM). It also inhibits Na+/H+-exchanger (NHE) and macropinocytosis.It is found that EIPA, benzamil, and phenamil rapidly and reversibly block Ca2+-activated TRPP3 channel activation at -50 mV, with IC50s of 143, 10.5, 1.1, and 0.14 μM, respectively.
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N-Oleoyl Glutamine
N-Oleoyl Glutamine (Oleoyl-L-glutamine) is an N-acyl amino acid involved in the regulation of PM20D1 and antagonizes TRPV1 of the transient receptor potential (TRP) calcium channel.
