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  3. Nelonemdaz potassium

Nelonemdaz potassium  (Synonyms: Salfaprodil; Neu2000 potassium)

Cat. No.: HY-106408A Purity: 99.86%
COA Handling Instructions

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.

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Nelonemdaz potassium Chemical Structure

Nelonemdaz potassium Chemical Structure

CAS No. : 916214-57-8

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

IC50 & Target

NMDA[1]

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[1].
Nelonemdaz potassium (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner[1].
Nelonemdaz potassium (0.1-1 μM) produces a marked reduction of Fe2+-induced neurotoxicity, even at doses of 0.1 to 0.3 μM[1].
Nelonemdaz potassium (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures[1].
Nelonemdaz potassium (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)[3].
Nelonemdaz potassium (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[3].
Nelonemdaz potassium (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC50 of 2.72±0.26 μM[3].
Nelonemdaz potassium (0-125 μM) effectively reduces iron-ascorbate-induced lipid peroxidation (IC50=24.56±0.07 μM)[3].

MedChemExpress (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[1].
Nelonemdaz potassium (5 mg/kg; i.v.) protects white matter such as axons and myelin as well as gray matter from ischemic brain injury[1].

MedChemExpress (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)[1]
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)[1]
Dosage: 5 mg/kg
Administration: I.v. administration 30 mins after reperfusion
Result: Did not change physiologic variables such as arterial pH, PCO2, PO2, and hematocrit.
Reduced infarct volume evolving in the cortex and the striatum substantially.
Reduced white matter damage in the striatum and external capsule markedly.
Molecular Weight

421.31

Formula

C15H7F7KNO3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC1=CC=C(C=C1C(O[K])=O)NCC2=C(C(F)=C(C(F)=C2F)C(F)(F)F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (474.71 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3735 mL 11.8677 mL 23.7355 mL
5 mM 0.4747 mL 2.3735 mL 4.7471 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3735 mL 11.8677 mL 23.7355 mL 59.3387 mL
5 mM 0.4747 mL 2.3735 mL 4.7471 mL 11.8677 mL
10 mM 0.2374 mL 1.1868 mL 2.3735 mL 5.9339 mL
15 mM 0.1582 mL 0.7912 mL 1.5824 mL 3.9559 mL
20 mM 0.1187 mL 0.5934 mL 1.1868 mL 2.9669 mL
25 mM 0.0949 mL 0.4747 mL 0.9494 mL 2.3735 mL
30 mM 0.0791 mL 0.3956 mL 0.7912 mL 1.9780 mL
40 mM 0.0593 mL 0.2967 mL 0.5934 mL 1.4835 mL
50 mM 0.0475 mL 0.2374 mL 0.4747 mL 1.1868 mL
60 mM 0.0396 mL 0.1978 mL 0.3956 mL 0.9890 mL
80 mM 0.0297 mL 0.1483 mL 0.2967 mL 0.7417 mL
100 mM 0.0237 mL 0.1187 mL 0.2374 mL 0.5934 mL
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Nelonemdaz potassium Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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