Salfaprodil free base

Salfaprodil free base (Neu2000) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Salfaprodil free base is also a free radical scavenger. Salfaprodil free base has excellent neuroprotection against NMDA- and free radical-induced cell death.

Product information

CAS Number: 640290-67-1

Molecular Weight: 383.22

Formula: C15H8F7NO3

Chemical Name: 2-hydroxy-5-({[2,3,5,6-tetrafluoro-4-(trifluoromethyl)phenyl]methyl}amino)benzoic acid

Smiles: OC1C=CC(=CC=1C(O)=O)NCC1=C(F)C(F)=C(C(F)=C1F)C(F)(F)F

InChiKey: HABROHXUHNHQMY-UHFFFAOYSA-N

InChi: InChI=1S/C15H8F7NO3/c16-10-7(11(17)13(19)9(12(10)18)15(20,21)22)4-23-5-1-2-8(24)6(3-5)14(25)26/h1-3,23-24H,4H2,(H,25,26)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : ≥ 112.5 mg/mL (293.57 mM).

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:

Salfaprodil (10-300 μM) shows apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA) at doses as low as 30 μM. Salfaprodil (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner. Salfaprodil (0.1-1 μM) produces a marked reduction of Fe2+-induced neurotoxicity, even at doses of 0.1 to 0.3 μM. Salfaprodil (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures. Salfaprodil (0-350 μM) effectively scavenges superoxide radicals (IC50=63.07±1.44 μM), nitric oxide (IC50=155.8±4.88 μM), and hydroxyl radicals (IC50=58.45±1.74 μM). Salfaprodil (0.78-12.5 μM) decreases the amount of antimycin A-induced ROS/RNS formation in a dose-dependent manner, with an IC50 of 2.21±0.11 μM. Salfaprodil (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC50 of 2.72±0.26 μM. Salfaprodil (0-125 μM) effectively reduces iron-ascorbate-induced lipid peroxidation (IC50=24.56±0.07 μM).

In Vivo:

Salfaprodil (0.5-20 mg/kg; i.v.) reduces cerebral infarct evolving 24 h after 60-mins occlusion of the middle cerebral artery occlusion (MCAO) substantially and dose dependently. Salfaprodil (5 mg/kg; i.v.) protects white matter such as axons and myelin as well as gray matter from ischemic brain injury.

Products are for research use only. Not for human use.