Ifenprodil
Based on 12 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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.94%
- No. CAS: 23210-56-2
- Fòrmula: C21H27NO2
- Peso molecular:325.44
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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HY-12882A
Ifenprodil tartrate -
HY-B0184
Felbamate -
HY-100806
Kynurenic acid -
HY-12881
Eliprodil -
HY-N0368
Linalool,98% (stabilized with MEHQ) -
HY-100806R
Kynurenic acid (Standard) -
HY-100807
Quinolinic acid -
HY-100714A
D-AP5 -
HY-B0184R
Felbamate (Standard) -
HY-N0368R
Linalool (Standard) -
HY-15084
Dizocilpine maleate
Publications Citing Use of MedChemExpress (MCE) Ifenprodil
More- Cell Rep. 2025 May 14;44(5):115712. [Abstract]
- Neurosci Bull. 2020 Feb;36(2):153-164. [Abstract]
- Life Sci. 2022 Apr 15:295:120419. [Abstract]
- Eur J Pharmacol. 2024 Oct 5:980:176860. [Abstract]
- Pharmaceuticals (Basel). 2024 Sep 19;17(9):1234. [Abstract]
- Eur J Pharmacol. 2023 Dec 15:961:176174. [Abstract]
- Neuropharmacology. 2026 Nov 1:298:111083. [Abstract]
- Antimicrob Agents Chemother. 2024 Nov 6;68(11):e0103524. [Abstract]
- Exp Brain Res. 2023 Dec;241(11-12):2735-2750. [Abstract]
- Folia Neuropathol. 2026 Apr 1;64(2).
- Heliyon. 2023 May 29;9(6):e16631. [Abstract]
- Chemosphere. 2019 Aug:229:618-630. [Abstract]
Ver todos los productos específicos de isoformas iGluR
MoreVer todos los productos específicos de isoformas Adrenergic Receptor
MoreVer todos los productos específicos de isoformas Calcium Channel
More
Actividad biológica
Descripciòn
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Cortical neurone | IC50 |
3.5 μM
Compound: 10
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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
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[PMID: 23458846] |
| HEK293 | IC50 |
177.4 nM
Compound: Ifenprodil
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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
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[PMID: 21453995] |
| Oocyte | IC50 |
0.073 μM
Compound: ifenprodil
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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
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[PMID: 18800760] |
| Oocyte | IC50 |
0.11 μM
Compound: ifenprodil, (+/-)-1
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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
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[PMID: 18434149] |
| Oocyte | IC50 |
0.19 μM
Compound: 1
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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
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[PMID: 20692832] |
| Oocyte | IC50 |
0.34 μM
Compound: 10
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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
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[PMID: 23458846] |
| Oocyte | IC50 |
340 nM
Compound: Ifenprodil
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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
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[PMID: 21453995] |
| SH-SY5Y | IC50 |
0.73 nM
Compound: ifenprodil
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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
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[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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Sprague-Dawley rats (300-350 g)[3]
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Dosage:0.25, 0.36, 0.68, 0.90, and 1.13 μmol (50 μL)
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Administration:Intrathecal injection; once
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Result:Produced spinal blockades of motor function and nociception dose-dependently.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 23210-56-2
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Appearance Solid
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Peso molecular 325.44
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Fòrmula C21H27NO2
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Color White to off-white
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SMILES
OC(C1=CC=C(O)C=C1)C(C)N(CC2)CCC2CC3=CC=CC=C3
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Synonyms
NP-120; RC-61-91
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (12)
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Journal Impact Factor
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Most Recent
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Cell Rep
Septo-subicular cholinergic circuit promotes seizure development via astrocytic inflammation. [Abstract]2025 May 14;44(5):115712. PMID: 40372911 -
Neurosci Bull
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 -
Eur J Pharmacol
Efficacy of GluN2B-Containing NMDA receptor antagonist for antitumor and antidepressant therapy in non-small cell lung cancer. [Abstract]2024 Oct 5:980:176860. PMID: 39067562 -
Pharmaceuticals (Basel)
2024 Sep 19;17(9):1234. PMID: 39338396 -
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 -
Neuropharmacology
DNMT3a-mediated GluN2B desilencing in the anterior cingulate cortex underlies chemotherapy-induced neuropathic pain. [Abstract]2026 Nov 1:298:111083. PMID: 42341912 -
Antimicrob Agents Chemother
2024 Nov 6;68(11):e0103524. PMID: 39360823 -
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 -
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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 -
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
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (274 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
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 | 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 Related Classifications
HY-12882 Related Classifications
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Keywords
- Ifenprodil
- 23210-56-2
- NP-120
- RC-61-91
- NP120
- NP 120
- iGluR
- Adrenergic Receptor
- Potassium Channel
- Calcium Channel
- Influenza Virus
- α1 adrenergic receptor
- NMDA receptor antagonist
- cerebral vasodilator
- GIRK
- Kir3
- neuroprotective
- anticonvulsant and antinociceptive effects
- cerebrovascular diseases
- peripheral arterial obliterative disease
- Inhibitor
- inhibitor
- inhibit