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Ifenprodil Tartrate NMDAR antagonist

Name: Ifenprodil Tartrate
Brand: Selleck Chemicals
SKU: S4091
Availability: InStock
Rating: 5 (5 reviews)

Cat.No.S4091

Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.

Chemical Structure

Molecular Weight: 800.98

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

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Chemical Information, Storage & Stability

Molecular Weight	800.98	Formula	2(C₂₁H₂₇NO₂).C₄H₆O₆	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	23210-58-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	N/A			Smiles	CC(C(C1=CC=C(C=C1)O)O)N2CCC(CC2)CC3=CC=CC=C3.CC(C(C1=CC=C(C=C1)O)O)N2CCC(CC2)CC3=CC=CC=C3.C(C(C(=O)O)O)(C(=O)O)O

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (124.84 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 50 mg/mL

Water : 8 mg/mL

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (6.24mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (1.56mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC₅₀/Ki	NMDA Receptor ^[1] 0.3 μM
In vitro	Ifenprodil inhibits NMDA-induced currents at NR1A/NR2B and NR1A/NR2A receptors with IC50 of 0.34 μM and 146 μM in oocytes voltage-clamped at -70 mV. Ifenprodil may act as a weak open-channel blocker of NR1A/NR2A receptors, the degree of inhibition seen with 100 μM Ifenprodil at NR1A/NR2A receptors is not altered by changes in the concentration of extracellular glycine. The inhibitory effect of 1 mM Ifenprodil at NR1A/NR2B receptors is reduced by increasing the concentration of glycine. ^[1] Ifenprodil (10 μM) inhibits virtually all of the NMDA receptor-evoked current in very young rat cortical neurons that contain a single population of receptors exhibiting a high affinity for glycine. Ifenprodil (10 μM) inhibits both the high-affinity population and a significant proportion of the low-affinity component in older rat cortical neurons, thus revealing three pharmacologically distinct populations of NMDA receptors in single neurons. ^[2] Ifenprodil antagonizes NMDA receptors in an activity-dependent manner, whilst also increasing the receptor affinity for glutamate recognition-site agonists. Ifenprodil inhibition curves against 10 μM and 100 μM NMDA-evoked currents yielded IC50 values of 0.88 μM and 0.17 μM, respectively. Ifenprodil (3 μM) potentiates to approximately 200% of control levels in rat cultured cortical neurones. Ifenprodil exhibits a 39- and 50-fold higher affinity for the agonist-bound activated and desensitized states of the NMDA receptor, respectively, relative to the resting, agonist-unbound state. Ifenprodil binding to the NMDA receptor results in a 6-fold higher affinity for glutamate site agonists. ^[3]
References	[1] https://pubmed.ncbi.nlm.nih.gov/7901753/ [2] https://pubmed.ncbi.nlm.nih.gov/9482779/ [3] https://pubmed.ncbi.nlm.nih.gov/9003561/

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