Description
5-BDBD, a potent and selective P2X4 receptor antagonist, inhibits rP2X4R-mediated currents, with an IC50 of 0.75 μM. 5-BDBD completely blocks the basal and acute hyperalgesia induced by nitroglycerin (NTG).
Product information
CAS Number: 768404-03-1
Molecular Weight: 355.19
Formula: C17H11BrN2O2
Chemical Name: 10-(3-bromophenyl)-8-oxa-11,14-diazatricyclo[7.5.0.0²,⁷]tetradeca-1(9),2,4,6,10-pentaen-13-one
Smiles: O=C1CN=C(C2OC3=CC=CC=C3C=2N1)C1C=C(Br)C=CC=1
InChiKey: NKYMVQPXXTZHSF-UHFFFAOYSA-N
InChi: InChI=1S/C17H11BrN2O2/c18-11-5-3-4-10(8-11)15-17-16(20-14(21)9-19-15)12-6-1-2-7-13(12)22-17/h1-8H,9H2,(H,20,21)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
5-BDBD inhibits 10 µM ATP-induced currents of rP2X4R-expressing HEK293 cells in a concentration-dependent manner, with an IC50 of 0.75 μM. 5-BDBD displaces rightward the ATP concentration-response curve, with an EC50 of 4.7 to 15.9 μM. 5-BDBD could be specifically used to discriminate between P2X1R, P2X2aR, P2X2bR, P2X3R, P2X4R, and P2X7R.
In Vivo:
5-BDBD (28 mg/kg; i.p.; daily for 9 days) can completely blocke the basal hyperalgesia induced by recurrent NTG injection.
Products are for research use only. Not for human use.
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