Cat. No.: HY-12882

Ifenprodil

(Synonyms: NP-120; RC-61-91)

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC₅₀=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC₅₀=146 μM). Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC₅₀ of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease.

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Pureté: 99.94%
CAS No.: 23210-56-2
Formule: C₂₁H₂₇NO₂
Masse moléculaire:325.44

Stockage:

4°C, sealed storage, away from moisture

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

Ifenprodil Chemical Structure

CAS No.: 23210-56-2

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Activité biologique
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (10)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
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Activité biologique

Description

Ifenprodil (NP-120), a cerebral vasodilator, is a noncompetitive NMDA receptor antagonist. Ifenprodil exerts high affinity at NR1A/NR2B receptors (IC₅₀=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC₅₀=146 μM)^[1]. Ifenprodil is an α1 adrenergic receptor antagonist. Ifenprodil inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil has reliable inhibitory effects against A/H1N1 strains (EC₅₀ of 6.6 µM). Ifenprodil has neuroprotective, anticonvulsant and antinociceptive effects. Ifenprodil can be used for the study of cerebrovascular diseases and peripheral arterial obliterative disease^[2]^[4].

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Cellular Effect

Cell Line	Type	Value	Description	References
Cortical neurone	IC₅₀	3.5 μM Compound: 10	Neuroprotective activity in rat Cortical neuron assessed as protection from glutamate-induced neurotoxicity treated after glutamate-challenge by lactate dehydrogenase assay Neuroprotective activity in rat Cortical neuron assessed as protection from glutamate-induced neurotoxicity treated after glutamate-challenge by lactate dehydrogenase assay	[PMID: 23458846]
HEK293	IC₅₀	177.4 nM Compound: Ifenprodil	Antagonist activity against NR1a/NR2B receptor transfected in human HEK293 cells assessed as inhibition of NMDA-induced Ca2+ influx Antagonist activity against NR1a/NR2B receptor transfected in human HEK293 cells assessed as inhibition of NMDA-induced Ca2+ influx	[PMID: 21453995]
Oocyte	IC₅₀	0.073 μM Compound: ifenprodil	Inhibition of rat recombinant NR1/NR2B receptor expressed in Xenopus oocytes assessed as inhibition of glutamate and glycine-induced evoked current by two electrode voltage clamp method Inhibition of rat recombinant NR1/NR2B receptor expressed in Xenopus oocytes assessed as inhibition of glutamate and glycine-induced evoked current by two electrode voltage clamp method	[PMID: 18800760]
Oocyte	IC₅₀	0.11 μM Compound: ifenprodil, (+/-)-1	Inhibition of NR1/NR2B receptor expressed in xenopus oocytes assessed as effect on L-glutamate and glycine-induced current response Inhibition of NR1/NR2B receptor expressed in xenopus oocytes assessed as effect on L-glutamate and glycine-induced current response	[PMID: 18434149]
Oocyte	IC₅₀	0.19 μM Compound: 1	Antagonist activity at wild type NR1/NR2B receptor expressed in Xenopus oocytes assessed as inhibition of agonist-induced current amplitude by two-electrode voltage-clamp method Antagonist activity at wild type NR1/NR2B receptor expressed in Xenopus oocytes assessed as inhibition of agonist-induced current amplitude by two-electrode voltage-clamp method	[PMID: 20692832]
Oocyte	IC₅₀	0.34 μM Compound: 10	Inhibition of GluN1/GluN2B receptor (unknown origin) expressed in Xenopus oocytes by voltage clamp assay Inhibition of GluN1/GluN2B receptor (unknown origin) expressed in Xenopus oocytes by voltage clamp assay	[PMID: 23458846]
Oocyte	IC₅₀	340 nM Compound: Ifenprodil	Antagonist activity against NR1/NR2B receptor expressed in xenopus oocytes assessed as inhibition of NMDA induced Ca2+ influx Antagonist activity against NR1/NR2B receptor expressed in xenopus oocytes assessed as inhibition of NMDA induced Ca2+ influx	[PMID: 21453995]
SH-SY5Y	IC₅₀	0.73 nM Compound: ifenprodil	Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay Neuroprotective activity in human SH-SY5Y cells assessed as protection against NMDA-induced cell death after 6 hrs by MTS assay	[PMID: 23033965]

In Vitro

The degree of inhibition seen with 100 μM Ifenprodil at NR1A/NR2A receptors is not altered by changes in the concentration of extracellular glycine. However, the inhibitory effect of 1 μM Ifenprodil at NR1A/NR2B receptors is reduced by increasing the concentration of glycine^[1].
In oocytes injected with mRNAs for GIRK1/GIRK2, GIRK2 or GIRK1/GIRK4 subunits, Ifenprodil (3 μM) reversibly reduces inward currents through the basal GIRK activity^[2].
Ifenprodil interacts with several other receptors, namely, serotonin (5-HT) subtype 1A, 5-HT2 and 5-HT3 receptors, and σ receptors at nanomolar concentrations and that it inhibits voltage-gated Ca²⁺ channels at micromolar concentrations^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Ifenprodil (0.25-1.13 μmol; intrathecal injection; once) produces a dose-dependent local anesthetic effect in spinal anesthesia in rat^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Sprague-Dawley rats (300-350 g)^[3]
Dosage:

0.25, 0.36, 0.68, 0.90, and 1.13 μmol (50 μL)
Administration:

Intrathecal injection; once
Result:

Produced spinal blockades of motor function and nociception dose-dependently.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 23210-56-2
Appearance Solid
Masse moléculaire 325.44
Formule C₂₁H₂₇NO₂
Color White to off-white
SMILES

OC(C1=CC=C(O)C=C1)C(C)N(CC2)CCC2CC3=CC=CC=C3
Synonyms

NP-120; RC-61-91
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

4°C, sealed storage, away from moisture

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

Publications (10)

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Journal Impact Factor

Chemosphere

Bisphenol-A induces neurodegeneration through disturbance of intracellular calcium homeostasis in human embryonic stem cells-derived cortical neurons. [Abstract]

2019 Aug:229:618-630. PMID: 31102917
Cell Rep

Septo-subicular cholinergic circuit promotes seizure development via astrocytic inflammation. [Abstract]

2025 May 14;44(5):115712. PMID: 40372911
Neurosci Bull

Ketamine Alleviates Fear Generalization Through GluN2B-BDNF Signaling in Mice. [Abstract]

2020 Feb;36(2):153-164. PMID: 31444653
Life Sci

EphrinB2/ephB2 activation facilitates colonic synaptic potentiation and plasticity contributing to long-term visceral hypersensitivity in irritable bowel syndrome. [Abstract]

2022 Apr 15:295:120419. PMID: 35183555
Pharmaceuticals (Basel)

Mechanisms of NMDA Receptor Inhibition by Biguanide Compounds. [Abstract]

2024 Sep 19;17(9):1234. PMID: 39338396
Eur J Pharmacol

Efficacy of GluN2B-Containing NMDA receptor antagonist for antitumor and antidepressant therapy in non-small cell lung cancer. [Abstract]

2024 Jul 25:176860. PMID: 39067562
Eur J Pharmacol

A novel dopamine D2 receptor-NR2B protein complex might contribute to morphine use disorders. [Abstract]

2023 Dec 15:961:176174. PMID: 37939993
Antimicrob Agents Chemother

The glutamate receptor antagonist ifenprodil inhibits hepatitis E virus infection. [Abstract]

2024 Nov 6;68(11):e0103524. PMID: 39360823
Heliyon

Mechanism of new optimized Sheng-Mai-San Formula to regulate cardiomyocyte apoptosis through NMDAR pathway. [Abstract]

2023 May 29;9(6):e16631. PMID: 37416647
Exp Brain Res

The NR2B-targeted intervention alleviates the neuronal injuries at the sub-acute stage of cerebral ischemia: an exploration of stage-dependent strategy against ischemic insults. [Abstract]

2023 Dec;241(11-12):2735-2750. PMID: 37845379

Solvant et solubilité

In Vitro:

DMSO : 12.5 mg/mL (38.41 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.0728 mL

15.3638 mL

30.7276 mL

5 mM

0.6146 mL

3.0728 mL

6.1455 mL

10 mM

0.3073 mL

1.5364 mL

3.0728 mL

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 1.25 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 1.25 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 1.25 mg/mL (3.84 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Williams K, et al. Ifenprodil discriminates subtypes of the N-methyl-D-aspartate receptor: selectivity and mechanisms at recombinant heteromeric receptors. Mol Pharmacol. 1993 Oct;44(4):851-9. [Content Brief]

[2]. Kobayashi T, et al. Inhibition of G protein-activated inwardly rectifying K+ channels by ifenprodil. Neuropsychopharmacology. 2006 Mar;31(3):516-24. [Content Brief]

[3]. Chen YW, et al. Ifenprodil for prolonged spinal blockades of motor function and nociception in rats. Pharmacol Rep. 2016 Apr;68(2):357-62. [Content Brief]

[4]. Jang Y, et al. In Vitro and In Vivo Antiviral Activity of Nylidrin by Targeting the Hemagglutinin 2-Mediated Membrane Fusion of Influenza A Virus. Viruses. 2020 May 25;12(5):581. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0728 mL	15.3638 mL	30.7276 mL	76.8191 mL
	5 mM	0.6146 mL	3.0728 mL	6.1455 mL	15.3638 mL
	10 mM	0.3073 mL	1.5364 mL	3.0728 mL	7.6819 mL
	15 mM	0.2049 mL	1.0243 mL	2.0485 mL	5.1213 mL
	20 mM	0.1536 mL	0.7682 mL	1.5364 mL	3.8410 mL
	25 mM	0.1229 mL	0.6146 mL	1.2291 mL	3.0728 mL
	30 mM	0.1024 mL	0.5121 mL	1.0243 mL	2.5606 mL

Ifenprodil

10 Cited Publications

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Ifenprodil

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Publications Citing Use of MedChemExpress (MCE) Ifenprodil

Voir tous les produits spécifiques à Isoform iGluR

Voir tous les produits spécifiques à Isoform Adrenergic Receptor

Voir tous les produits spécifiques à Isoform Calcium Channel

Activité biologique

Chemical Information

Publications (10)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Ifenprodil Related Classifications

Cat. No.: HY-12882