NS 1738 (NSC 213859)
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 250mg | $1125 | Check With Us |
| 500mg | $1800 | Check With Us |
| 1g | $2700 | Check With Us |
: Cat #: V5093 CAS #: 501684-93-1 Purity ≥ 98%
Description: NS 1738 (also known as NSC 213859) is a novel and potent positive allosteric modulator of the α7 nAChR, with respect to positive modulation of nicotinic alpha7 receptor (α7 nAChR) with EC50 of 3.4 μM in oocyte experiments.
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| Molecular Weight (MW) | 365.13 |
|---|---|
| Molecular Formula | C14H9Cl2F3N2O2 |
| CAS No. | 501684-93-1 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent |
| Protocol | In Vitro | NS 1738 acts by increasing the peak amplitude of acetylcholine (ACh)-evoked currents at all concentrations; thus, it increased the maximal efficacy of ACh. Plotting peak current amplitude against the logarithm of the NS 1738 concentration used for preincubation reveals a sigmoidal concentration-response relationship that is well fit by the Hill equation (EC50=3.4 μM). Under similar experimental conditions, NS 1738 shows comparable efficacy and potency at the rat α7 nAChR (EC50=3.9 μM) |
|---|---|---|
| In Vivo | To estimate the ability of NS 1738 to permeate the blood-brain barrier, rats are administered 10 mg/kg NS 1738 intraperitoneally. Peak brain concentrations are measured approximately 30 min after injection, and they amount to ~80 ng/mL (~200 nM) at this dose. The ratio between the amount of compound entering the brain and that in plasma is AUCbrain/AUCplasma=0.50. The half-life in plasma is estimated to 42 min. Incubation of NS1738 with isolated liver microsomes in vitro indicates that approximately 60 and 75% of NS 1738 is metabolized via the cytochrome P450 system in mouse and rat, respectively, within 1 h. Adult rats administered NS 1738 at 10 and 30 mg/kg i.p. immediately following the initial exposure to a juvenile rat (T1) display significant decreases in the investigative duration of a subsequent exposure to the same juvenile (T2) 2 h later (T2/T1 ratio of 0.69±0.13 and 0.61±0.07, respectively). |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.7388 mL | 13.6938 mL | 27.3875 mL | 54.7750 mL |
| 5mM | 0.5478 mL | 2.7388 mL | 5.4775 mL | 10.9550 mL |
| 10mM | 0.2739 mL | 1.3694 mL | 2.7388 mL | 5.4775 mL |
| 20mM | 0.1369 mL | 0.6847 mL | 1.3694 mL | 2.7388 mL |
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Step One: Enter information below
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Step Two: Enter the in vivo formulation
%DMSO
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%Tween 80
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%ddH2O
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Method for preparing DMSO master liquid:
mg
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,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 add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (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.