| Size | Price | |
|---|---|---|
| Other Sizes |
| ln Vitro |
Compound 14 (NAB-14) has an IC50 of 15 µM and 5.1 µM, respectively, which inhibits the GluN1/2AC1/2CC2 and GluN1/2AC1/2CC2 receptors [1]. Although native GluN2A or GluN2B-containing NMDARs in cultured cortical neurons are unaffected by NAB-14 (20 µM; 24 hours), it inhibits native GluN2D-containing receptors in brain slices [1]. The evoked EPSCs' peak amplitude is reduced to 55 ± 3.0% and the τW of EPSC inactivation is dramatically decreased by NAB-14 (10 µM) [1]. The amount of NAB-14 (10 µM) that decreased the interneuron EPSCs' peak amplitude and charge transfer to 59 ± 9.9% and 63 ± 9.7%, respectively. NAB-14 lowers interneuron EPSCs' τW from 150 ± 12 ms to 101 ± 14 ms[1].
|
|---|---|
| ln Vivo |
NAB-14 (20 mg/kg; oral) causes a significant systemic exposure; in mice and rats, peak brain free concentrations are 3.2 and 3.8 nM, respectively [1].
|
| Animal Protocol |
Animal/Disease Models: Mice and rats [1]
Doses: 20 mg/kg Route of Administration: Oral Experimental Results: Demonstrated high systemic exposure, with peak intracerebral peaks of 3.2 and 3.8 nM in mice and rats, respectively. |
| References |
| Molecular Formula |
C20H21N3O3
|
|---|---|
| Molecular Weight |
351.399044752121
|
| Exact Mass |
351.158
|
| CAS # |
1237541-73-9
|
| PubChem CID |
46862257
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.4
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
26
|
| Complexity |
487
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
O(C1C=CC(=CC=1)C(NC1=CC=CC2C=CNC=21)=O)C(N(CC)CC)=O
|
| InChi Key |
WCGIKJOMEYPSIP-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H21N3O3/c1-3-23(4-2)20(25)26-16-10-8-15(9-11-16)19(24)22-17-7-5-6-14-12-13-21-18(14)17/h5-13,21H,3-4H2,1-2H3,(H,22,24)
|
| Chemical Name |
[4-(1H-indol-7-ylcarbamoyl)phenyl] N,N-diethylcarbamate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8458 mL | 14.2288 mL | 28.4576 mL | |
| 5 mM | 0.5692 mL | 2.8458 mL | 5.6915 mL | |
| 10 mM | 0.2846 mL | 1.4229 mL | 2.8458 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
