Nelonemdaz potassium - ≥98% , CAS No.916214-57-8

CAS: 916214-57-8 Cat. No.: N648222 Molecular Weight: 421.31 PubChem CID: 23684338

GRADE & PURITY ≥98%

Storage

Store at 2-8°C,Desiccated

Shipped In

Wet ice

Overview

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

In Vitro

Nelonemdaz potassium (10-300 μM) shows apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA) at doses as low as 30 μM. Nelonemdaz potassium (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner. Nelonemdaz potassium (0.1-1 μM) produces a marked reduction of Fe 2+ -induced neurotoxicity, even at doses of 0.1 to 0.3 μM. Nelonemdaz potassium (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures. Nelonemdaz potassium (0-350 μM) effectively scavenges superoxide radicals (IC 50 =63.07±1.44 μM), nitric oxide (IC 50 =155.8±4.88 μM), and hydroxyl radicals (IC 50 =58.45±1.74 μM). Nelonemdaz potassium (0.78-12.5 μM) decreases the amount of antimycin A-induced ROS/RNS formation in a dose-dependent manner, with an IC 50 of 2.21±0.11 μM. Nelonemdaz potassium (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC 50 of 2.72±0.26 μM. Nelonemdaz potassium (0-125 μM) effectively reduces iron-ascorbate-induced lipid peroxidation (IC 50 =24.56±0.07 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Nelonemdaz potassium (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 . Nelonemdaz potassium (5 mg/kg; i.v.) protects white matter such as axons and myelin as well as gray matter from ischemic brain injury . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male Sprague-Dawley rats (260 to 300 g) (clip occlusion model) Dosage: 0.5-20 mg/kg Administration: I.v. administration 5 mins after reperfusion Result: Produced a large neuroprotective effect, with a maximal reduction in infarct volume of 66% at doses of 2.5 to 5 mg/kg. Not observed neuronal damage in the most vulnerable cortical area after administration of 5 mg/kg. Animal Model: Male Sprague-Dawley rats (260 to 300 g) (intraluminal thread occlusion model) Dosage: 5 mg/kg Administration: I.v. administration 30 mins after reperfusion Result: Did not change physiologic variables such as arterial pH, PCO 2 , PO 2 , and hematocrit. Reduced infarct volume evolving in the cortex and the striatum substantially. Reduced white matter damage in the striatum and external capsule markedly.

Form:Solid

IC50& Target:NMDA

Specifications

Specifications & Purity

≥98%

Biochemical and Physiological Mechanisms

Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA) . Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-

Storage

Store at 2-8°C, Desiccated

Shipped In

Wet ice

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

ANTAGONIST

Purity

≥98%

Names and Identifiers

• Isomeric SMILES: C1=CC(=C(C=C1NCC2=C(C(=C(C(=C2F)F)C(F)(F)F)F)F)C(=O)[O-])O.[K+]
• PubChem CID: 23684338
• Molecular Weight: 421.31

Chemical and Physical Properties

• Solubility: DMSO : 200 mg/mL (474.71 mM; Need ultrasonic)
• Molecular Weight: 421.310 g/mol
• Hydrogen Bond Donor Count: 2
• Hydrogen Bond Acceptor Count: 11
• Rotatable Bond Count: 4
• Exact Mass: 420.995 Da
• Monoisotopic Mass: 420.995 Da
• Topological Polar Surface Area: 72.400 Ų
• Heavy Atom Count: 27
• Formal Charge: 0
• Complexity: 496.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 0
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 0
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 0
• Covalently-Bonded Unit Count: 2

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