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BRL54443
CAS No. 57477-39-1
BRL54443( BRL 54443 | BRL-54443 )
Catalog No. M15098 CAS No. 57477-39-1
BRL54443 is a potent, releative selective 5-HT1E/1F agonist with Ki of 2/1 nM, respectively.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 43 | In Stock |
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| 10MG | 68 | In Stock |
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| 25MG | 144 | In Stock |
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| 50MG | 227 | In Stock |
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| 100MG | 381 | In Stock |
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| 200MG | Get Quote | In Stock |
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Biological Information
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Product NameBRL54443
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NoteResearch use only, not for human use.
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Brief DescriptionBRL54443 is a potent, releative selective 5-HT1E/1F agonist with Ki of 2/1 nM, respectively.
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DescriptionBRL54443 is a potent, releative selective 5-HT1E/1F agonist with Ki of 2/1 nM, respectively; shows low affinity for other receptors 5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10,000 nM), 5-HT7 (>10,000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM); selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production with IC50 of 14 nM in DG membranes; significantly reduces formalin-induced flinching in rats.
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In VitroDespite its low affinity for other receptors [5-HT1A (63 nM), 5-HT1B (126 nM), 5-HT1D (63 nM), 5-HT2A (1259 nM), 5-HT2B (100 nM), 5-HT2C (316 nM), 5-HT6 (>10,000 nM), 5-HT7 (>10,000 nM), D2 (501 nM), D3 (631 nM), and α1B-adrenoceptors (1259 nM)], BRL54443 binds with high affinity at 5-HT1F receptors. In DG membranes, BRL54443 selectively stimulates 5-HT1E receptors and potently inhibits forskolin-dependent cAMP production (IC50=14 nM). BRL 54443 also induces contraction (-log EC50=6.52).
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In VivoReduction of flinching was considered as antinociception. Ipsilateral, but not contralateral, peripheral administration of BRL54443 (5-HT(1E/1F); 3-300 microg/paw) significantly reduced formalin-induced flinching in rats.
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SynonymsBRL 54443 | BRL-54443
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PathwayEndocrinology/Hormones
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Target5-HT Receptor
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Recptor5-HT1A|5-HT1B|5-HT1D|5-HT1E|5-HT1F
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Research AreaCardiovascular Disease
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Indication——
Chemical Information
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CAS Number57477-39-1
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Formula Weight230.3055
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Molecular FormulaC14H18N2O
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Purity>98% (HPLC)
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SolubilityDMSO: ≥ 51 mg/mL
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SMILESCN1CCC(C2=CNC3=C2C=C(O)C=C3)CC1
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Chemical Name1H-Indol-5-ol, 3-(1-methyl-4-piperidinyl)-
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Klein MT, et al. J Pharmacol Exp Ther. 2011 Jun;337(3):860-7.
2. Klein MT,et al. Br J Pharmacol. 2012 Jun;166(4):1290-302.
3. Granados-Soto V, et al. Neuroscience. 2010 Jan 20;165(2):561-8.
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