Cat. No.: HY-12882A

Ifenprodil tartrate

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

10 Cited Publications

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Based on 10 publication(s) in Google Scholar

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

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Pureté: 99.94%
CAS No.: 23210-58-4
Formule: C₂₁H₂₇NO₂.1/2C₄H₆O₆
Masse moléculaire:400.49

Stockage:

4°C, sealed storage, away from moisture

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

Ifenprodil tartrate Chemical Structure

CAS No.: 23210-58-4

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (10)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Bioz

Activité biologique

Description

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

IC₅₀ & Target

NMDA Receptor

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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]
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	0.19 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]
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 tartrate at NR1A/NR2A receptors is not altered by changes in the concentration of extracellular glycine. However, the inhibitory effect of 1 μM Ifenprodil tartrate 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) tartrate reversibly reduces inward currents through the basal GIRK activity^[2].
Ifenprodil tartrate 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) tartrate 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.

Chemical Information

CAS No. 23210-58-4
Appearance Solid
Masse moléculaire 400.49
Formule C₂₁H₂₇NO₂.1/2C₄H₆O₆
Color White to off-white
SMILES

OC(C1=CC=C(O)C=C1)C(C)N(CC2)CCC2CC3=CC=CC=C3.O=C(O)[C@H](O)[C@@H](O)C(O)=O.[1/2]
Synonyms

NP-120 tartrate; RC-61-91 tartrate
Structure Classification
- Alkaloids
- Piperidine Alkaloids
Initial Source
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 : ≥ 500 mg/mL (1248.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 5 mg/mL (12.48 mM; Need ultrasonic)

* "≥" means soluble, but saturation unknown.

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

2.4969 mL

12.4847 mL

24.9694 mL

5 mM

0.4994 mL

2.4969 mL

4.9939 mL

10 mM

0.2497 mL

1.2485 mL

2.4969 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Calculateur de molarité

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

Mass

Concentration

Volume

Molecular Weight

Calculateur de dilution

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

Concentration _(start)

Volume _(start)

Concentration _(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: 1% DMSO 99% Saline

Solubility: ≥ 1 mg/mL (2.50 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 0.5% CMC-Na/saline water

Solubility: 12.22 mg/mL (30.51 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage
mg/kg
Animal Weight (Per Animal)
g
Dosing Volume (Per Animal)
μL
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 (279 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)
- 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
H₂O / DMSO	1 mM	2.4969 mL	12.4847 mL	24.9694 mL	62.4235 mL
	5 mM	0.4994 mL	2.4969 mL	4.9939 mL	12.4847 mL
	10 mM	0.2497 mL	1.2485 mL	2.4969 mL	6.2424 mL
DMSO	15 mM	0.1665 mL	0.8323 mL	1.6646 mL	4.1616 mL
	20 mM	0.1248 mL	0.6242 mL	1.2485 mL	3.1212 mL
	25 mM	0.0999 mL	0.4994 mL	0.9988 mL	2.4969 mL
	30 mM	0.0832 mL	0.4162 mL	0.8323 mL	2.0808 mL
	40 mM	0.0624 mL	0.3121 mL	0.6242 mL	1.5606 mL
	50 mM	0.0499 mL	0.2497 mL	0.4994 mL	1.2485 mL
	60 mM	0.0416 mL	0.2081 mL	0.4162 mL	1.0404 mL
	80 mM	0.0312 mL	0.1561 mL	0.3121 mL	0.7803 mL
	100 mM	0.0250 mL	0.1248 mL	0.2497 mL	0.6242 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Ifenprodil tartrate

10 Cited Publications

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Ifenprodil tartrate

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Publications Citing Use of MedChemExpress (MCE) Ifenprodil tartrate

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 tartrate Related Classifications

Cat. No.: HY-12882A