2. Membrane Transporter/Ion Channel Neuronal Signaling Immunology/Inflammation GPCR/G Protein Metabolic Enzyme/Protease
  3. iGluR Histamine Receptor Potassium Channel Cytochrome P450 Adrenergic Receptor
  4. NP10679

NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes.

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NP10679 Chemical Structure

NP10679 Chemical Structure

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 106 In-stock
Solution
10 mM * 1 mL in DMSO USD 106 In-stock
Solid
1 mg USD 48 In-stock
5 mg USD 107 In-stock
10 mg USD 171 In-stock
25 mg USD 360 In-stock
50 mg USD 576 In-stock
100 mg USD 923 In-stock
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

NP10679 is a selective, pH dependent GluN2B subunit-specific N-methyl-D-aspartate (NMDA) receptor inhibitor with high oral bioavailability and good brain penetration. NP10679 inhibits GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively. NP10679 is a histamine H1 antagonist and a hERG channel inhibitor with IC50s of 73 and 620 nM, respectively. NP10679 is a reversible inhibitor of human liver CYP enzymes[1].

IC50 & Target

H1 Receptor

0.073 μM (IC50)

H1 Receptor

0.04 μM (Ki)

Alpha-1A adrenergic receptor

0.154 μM (IC50)

Alpha-1A adrenergic receptor

0.603 μM (Ki)

Alpha-1B adrenergic receptor

1.92 μM (Ki)

Alpha-1D adrenergic receptor

0.495 μM (Ki)

Alpha-2C adrenergic receptor

3.09 μM (Ki)

In Vitro

NP10679 (1-1000 nM) shows pH-dependently effects to GluN2B with IC50s of 23 and 142 nM at pH 6.9 and 7.6, respectively[2].
NP10679 shows functional inhibition to 5-HT2A, α adrenergic receptor-1A (α1A), H1-histamine receptor (H1) and hERG channel with IC50 values of 1.71, 0.154, 0.073 and 0.617 μM, respectively[2].
NP10679 shows Ki values of 2.29, 0.638, 1.92, 0.603, 1.92, 0.495, 3.09, 0.040 and 0.135 for 5-HT1D, 5-HT2A, 5-HT2B, α1A, α1B, α1D, α2C, H1 and serotonin transporter SERT[2].

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

NP10679 Related Antibodies
In Vivo

NP10679 (2, 5 and 10 mg/kg; i.p., prior to transient ischemia) reduces infarct volumes of transient ischemia mice[2].

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

Animal Model: Male C57BL/6 middle cerebral artery occlusion (MCAo) model of transient ischemia mice[2]
Dosage: 2, 5 and 10 mg/kg
Administration: Intraperitoneal injection; 2, 5 and 10 mg/kg, 15 minutes prior to transient ischemia
Result: Dose-dependently reduced infarct volumes with an ED50 of 1 mg/kg.
Clinical Trial
Molecular Weight

449.47

Formula

C23H26F3N3O3
Appearance

Solid

Color

White to light yellow

SMILES

O=C(N1)CCC2=C1C=CC(OC[C@H](O)CN(CC3)CCN3C4=CC=C(C(F)(F)F)C=C4)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (222.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2248 mL 11.1242 mL 22.2484 mL
5 mM 0.4450 mL 2.2248 mL 4.4497 mL
View the 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • Protocol 1

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

    Solubility: 2.5 mg/mL (5.56 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
  • Protocol 2

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

    Solubility: 2.5 mg/mL (5.56 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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. 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 2.2248 mL 11.1242 mL 22.2484 mL 55.6211 mL
5 mM 0.4450 mL 2.2248 mL 4.4497 mL 11.1242 mL
10 mM 0.2225 mL 1.1124 mL 2.2248 mL 5.5621 mL
15 mM 0.1483 mL 0.7416 mL 1.4832 mL 3.7081 mL
20 mM 0.1112 mL 0.5562 mL 1.1124 mL 2.7811 mL
25 mM 0.0890 mL 0.4450 mL 0.8899 mL 2.2248 mL
30 mM 0.0742 mL 0.3708 mL 0.7416 mL 1.8540 mL
40 mM 0.0556 mL 0.2781 mL 0.5562 mL 1.3905 mL
50 mM 0.0445 mL 0.2225 mL 0.4450 mL 1.1124 mL
60 mM 0.0371 mL 0.1854 mL 0.3708 mL 0.9270 mL
80 mM 0.0278 mL 0.1391 mL 0.2781 mL 0.6953 mL
100 mM 0.0222 mL 0.1112 mL 0.2225 mL 0.5562 mL
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NP10679 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

NP10679NP 10679NP-10679iGluRHistamine ReceptorPotassium ChannelCytochrome P450Adrenergic ReceptorIonotropic glutamate receptorsKcsACYPsBeta ReceptorpH dependentoral bioavailabilitybrain penetrationMCAotransient ischemiaInhibitorinhibitorinhibit

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