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  3. Nelonemdaz

Nelonemdaz  (Synonyms: Salfaprodil free base; Neu2000)

Cat. No.: HY-106408 Purity: 99.84%
COA Handling Instructions

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

For research use only. We do not sell to patients.

Nelonemdaz Chemical Structure

Nelonemdaz Chemical Structure

CAS No. : 640290-67-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 211 In-stock
Solution
10 mM * 1 mL in DMSO USD 211 In-stock
Solid
1 mg USD 80 In-stock
5 mg USD 250 In-stock
10 mg USD 450 In-stock
50 mg USD 1250 In-stock
100 mg USD 1850 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Nelonemdaz (Salfaprodil free base) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz is also a free radical scavenger. Nelonemdaz has excellent neuroprotection against NMDA- and free radical-induced cell death[1][2].

IC50 & Target

NMDA receptor[1]

In Vitro

Nelonemdaz (10-300 μM) shows apparent neuroprotection against 300 μM N-methyl-d-aspartate (NMDA) at doses as low as 30 μM[1].
Nelonemdazl (10-500 μM) inhibits the electrophysiologic response of cultured cortical neurons to 300 μM NMDA in a concentration-dependent manner[1].
Nelonemdaz (0.1-1 μM) produces a marked reduction of Fe2+-induced neurotoxicity, even at doses of 0.1 to 0.3 μM[1].
Nelonemdaz (0.1-1 μM) blocks the degeneration of neurons and glia in cortical cell cultures[1].
Nelonemdaz (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 (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 (0.19-12.5 μM) inhibits malondialdehyde (MDA) formation with an IC50 of 2.72±0.26 μM[3].
Nelonemdaz (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 (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 (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

383.22

Formula

C15H8F7NO3

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC(C1=C(O)C=CC(NCC2=C(C(F)=C(C(F)(F)F)C(F)=C2F)F)=C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 112.5 mg/mL (293.57 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6095 mL 13.0473 mL 26.0947 mL
5 mM 0.5219 mL 2.6095 mL 5.2189 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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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

Purity: 99.84%

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6095 mL 13.0473 mL 26.0947 mL 65.2367 mL
5 mM 0.5219 mL 2.6095 mL 5.2189 mL 13.0473 mL
10 mM 0.2609 mL 1.3047 mL 2.6095 mL 6.5237 mL
15 mM 0.1740 mL 0.8698 mL 1.7396 mL 4.3491 mL
20 mM 0.1305 mL 0.6524 mL 1.3047 mL 3.2618 mL
25 mM 0.1044 mL 0.5219 mL 1.0438 mL 2.6095 mL
30 mM 0.0870 mL 0.4349 mL 0.8698 mL 2.1746 mL
40 mM 0.0652 mL 0.3262 mL 0.6524 mL 1.6309 mL
50 mM 0.0522 mL 0.2609 mL 0.5219 mL 1.3047 mL
60 mM 0.0435 mL 0.2175 mL 0.4349 mL 1.0873 mL
80 mM 0.0326 mL 0.1631 mL 0.3262 mL 0.8155 mL
100 mM 0.0261 mL 0.1305 mL 0.2609 mL 0.6524 mL
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  • Do most proteins show cross-species activity?

    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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Nelonemdaz
Cat. No.:
HY-106408
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