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5-BDBD

Cat. No. M6347
5-BDBD Structure
Synonym:

5BDBD

Size Price Availability Quantity
10mg USD 180  USD180 In stock
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Quality Control & Documentation
Biological Activity

5-BDBD is a potent P2X4 receptor antagonist. Blocks P2X4-mediated currents in Chinese hamster ovary cells (IC50 = 0.50 μM). 5-BDBD exhibits no significant antagonist effects at other P2X receptors. 5-BDBD reduces long-term potentiation (LTP) in rat hippocampal slices.

Chemical Information
Molecular Weight 355.19
Formula C17H11BrN2O2
CAS Number 768404-03-1
Solubility (25°C) DMSO 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Stefan Bidula, et al. Structural Basis of the Negative Allosteric Modulation of 5-BDBD at Human P2X4 Receptors

[2] Pranay Srivastava, et al. Neuroprotective and neuro-rehabilitative effects of acute purinergic receptor P2X4 (P2X4R) blockade after ischemic stroke

[3] Claudio Coddou, et al. Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor

[4] Bing Hu, et al. 5-BDBD ameliorates an OVA-induced allergic asthma by the reduction of Th2 cytokines production

[5] Min Wang, et al. Synthesis and preliminary biological evaluation of radiolabeled 5-BDBD analogs as new candidate PET radioligands for P2X4 receptor

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  Catalog
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Keywords: 5-BDBD, 5BDBD supplier, P2 Receptor, inhibitors, activators


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