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Cat. No.: HY-12962A

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NMDA-IN-1 dihydrochloride

Name: NMDA-IN-1 dihydrochloride
Brand: MedChemExpress
SKU: HY-12962A
Price: 100.00 USD
Availability: InStock
Rating: 5 (1 reviews)

NMDA-IN-1 dihydrochloride is a selective NMDA NR2B antagonist with a Ki of 0.85 nM; NR2B Ca₂₊ influx IC₅₀ is 9.7 nM. NMDA-IN-1 dihydrochloride inhibits Glu/Gly stimulated Ca₂₊ flux in Ltk- cells expressing the hNR1a/NR2B with a IC₅₀ of 9.7 nM. NMDA-IN-1 dihydrochloride has no activities on NR2A, NR2C, NR2D, hERG-channel and α1-adrenergic receptor. NMDA-IN-1 dihydrochloride shows excellent activity in the mechanical hyperalgesia assay in rats. NMDA-IN-1 dihydrochloride can be used for the studies of stroke, parkinson, and neuropathic pain.

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

CAS No.: 1784252-90-9
Formula: C₂₀H₂₄Cl₂FN₃O
Molecular Weight:412.33

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (268 KB)

NMDA-IN-1 dihydrochloride Chemical Structure

CAS No.: 1784252-90-9

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Parmacokinetics
- In Vivo
Chemical Information
Protocols (2)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

All iGluR Isoforms :

Parmacokinetics

Species	Dose	Route	T_1/2	CL	F
Dog	3 mg/kg	p.o.	390 min	0.6 mL/min/kg	87 %
Rat	2 mg/kg	i.v.	60 min	12.3 mL/min/kg	/

In Vivo

NMDA-IN-1 dihydrochloride (Compound 37a) (1, 3 and 10 mg/kg, i.v., single dose) shows good activity with an ED₅₀ of <3 mg/kg in carrageenan-induced mechanical hyperalgesia model in rats^[1].
NMDA-IN-1 dihydrochloride (30 mg/kg for rats and 3 mg/kg for dogs, p.o., single dose) shows poor oral bioavailability in rat but, in contrast, demonstrated good pharmacokinetic profiles in dog^[1].

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

Chemical Information

CAS No. 1784252-90-9
Molecular Weight 412.33
Formula C₂₀H₂₄Cl₂FN₃O
SMILES

OC1=CC=C2N=C(CN3CCC(CC4=CC=CC=C4F)CC3)NC2=C1.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Protocols

All Cell Biology

Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Ca²⁺ Staining Technique
Ca²⁺ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca²⁺ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 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)
Handling Instructions (2659 KB)

References

[1]. McCauley JA,et al. NR2B-selective N-methyl-D-aspartate antagonists: synthesis and evaluation of 5-substituted benzimidazoles. J Med Chem. 2004 Apr 8;47(8):2089-96. [Content Brief]

Calculators

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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.

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100 mg

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