Description
Fipamezole (MPV 1730; JP-1730) is a potent and orally active α2-adrenergic receptor antagonist with Ki values of 9.2 nM, 17 nM, and 55 nM for human α2A, α2B, and α2C, receptors, respectively. Fipamezole is an anti-dyskinetic agent, and can be used for the study of Parkinson's disease.
Product information
CAS Number: 150586-58-6
Molecular Weight: 230.28
Formula: C14H15FN2
Smiles: CCC1(CC2=CC=C(F)C=C2C1)C1=CN=CN1
InChiKey: KXSUAWAUCNFBQJ-UHFFFAOYSA-N
InChi: InChI=1S/C14H15FN2/c1-2-14(13-8-16-9-17-13)6-10-3-4-12(15)5-11(10)7-14/h3-5,8-9H,2,6-7H2,1H3,(H,16,17)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
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:
In functional assays, the potent antagonist properties of Fipamezole (JP-1730) are demonstrated by its ability to reduce adrenaline-induced 35S-GTPγS binding with KB values of 8.4 nM, 16 nM, 4.7 nM at human α2A, α2B, and α2C receptors, respectively. Fipamezole also has moderate affinity at histamine H1 and H3 receptors and the serotonin (5-HT) transporter (IC50 of 100 nM-1 μM).
In Vivo:
In the MPTP-lesioned marmoset, Fipamezole (1-10 mg/kg; po; once) significantly reduces L-dopa-induced dyskinesia without compromising the anti-parkinsonian action of L-DOPA (HY-N0304).
Products are for research use only. Not for human use.
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