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BRL-15572

Cat. No. M3524
BRL-15572 Structure
Size Price Availability
10mg USD 90 Custom Synthesis
50mg USD 300 Custom Synthesis
200mg USD 780 Custom Synthesis
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

BRL-15572 is a hydrochloride salt form of BRL-15572 which is a selective  serotonin receptor subtype 5-HT1D antagonist with an IC50 of 260 μM.  BRL-15572 indicates 60-fold selectivity over h5-HT1B, and displays little or no affinity for a range of other receptor types. In the presence of the 5-HT1D antagonist BRL15572 at a dose of 10 μM triggered a significant reduction in evoked IPSC (inhibitory postsynaptic currents) amplitude. Additionally, the antianti-migraine agent sumatriptan (1 μM) produced a striking reduction in evoked IPSC amplitude in the presence of BRL15572 (10 μM) which was not significantly different to that produced in its absence. For a comparison, sumatriptan (1 μM) did not produce a marked reduction in evoked IPSC amplitude in the presence of both NAS181 (10 μM) and BRL15572 (10 μM). In addition, it was observed that the prevention of GABAergic synaptic transmission produced by 5-HT was abolished by the 5-HT1B antagonist NAS181, but not by the 5-HT1A and 5-HT1D antagonists WAY100135 and BRL15572, while that produced by sumatriptan was only abolished in the combined presence of NAS181 and BRL15572.

Protocol
Cell Experiment
Cell lines CHO cells expressing the h5-HT1B or h5-HT1D receptors
Preparation method [35S]GTPγS binding studies. [35S]GTPγS binding studies in CHO cells expressing the h5-HT1B or h5-HT1D receptors are performed. In brief, membranes from 1 × 106 cells are preincubated at 30°C for 30 minutes, in HEPES buffer (HEPES [20 mM], MgCl2 [3 mM], NaCl [100 mM], ascorbate [0.2 mM]), containing GDP (10 µ M), with or without BRL-15572. Starting the reaction by the addition of 10 µL of [35S]GTPγS (100 pM, assay concentration) followed by a further 30 minutes incubation at 30°C. Determing Non-specific binding by addition of unlabelled GTPγS (10 µM), prior to the addition of cells. Stoping the reaction by rapid filtration using Whatman GF/B grade filters followed by five washes with ice-cold HEPES buffer. Determining radioactivity by liquid scintillation spectrometry
Concentrations 0 μM -10 μM
Incubation time 30 minutes
Animal Experiment
Animal models Male Wistar rats with diabetes
Formulation 20% propylene glycol
Dosages 1 mg/kg, 2 mg/kg
Administration Administered via i.v.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 479.87
Formula C25H27ClN2O.2HCl
CAS Number 193611-72-2
Purity >99%
Solubility DMSO 90 mg/mL
Storage at -20°C
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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: BRL-15572 supplier, 5-HT Receptor, inhibitors

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