| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| Other Sizes |
|
Purity: ≥98%
LY-404187 is an ampakine, AMPA receptor potentiator. LY-404187 has been demonstrated to enhance cognitive function in animal studies, and has also shown effects suggesting antidepressant action as well as having possible application in the treatment of schizophrenia, Parkinson's disease and ADHD. These effects appear to be mediated through multiple mechanisms of action secondary to AMPA receptor potentiation, with a prominent effect seen in research being increased levels of BDNF in the brain.
| ln Vitro |
Human GluR4-transfected HEK293 cells exhibit enhanced glutamate-evoked inward current in response to LY-404187 (3-10 nM) [2]. In acutely isolated pyramidal neurons, LY-404187 (0.03-10 µM) selectively increases glutamate-evoked currents through AMPA receptors/channels with notable potency (EC50=1.3±0.3 µM) and efficacy (Emax = 45.3±8.0 times increase) [3]. At a dosage of 10 µM, LY-404187 has no effect on the amplitude or time course of whole-cell K+ or Na+ currents in pyramidal neurons of the prefrontal cortex (PFC) [3].
|
|---|---|
| ln Vivo |
Mice exposed to 0.5 mg/kg of LY-404187 subcutaneously for 11 days are protected against MPTP-induced neurotoxicity [4]. When administered subcutaneously for 28 days at a dose of 0.5 mg/kg, LY-404187 significantly prevents the loss of tyrosine hydroxylase-positive substantia nigra cell bodies and reduces apomorphine-induced counterrotation [4]. The substantia nigra of rats infused with 6-hydroxydopamine is protected functionally, neurochemically, and histologically by LY-404187 (0.1 or 0.5 mg/kg; subcutaneously for 14 days) [4]. Improvements in both function and histology were observed with LY-404187 (0.5 mg/kg) applied subcutaneously for 14 days after therapy was delayed. This suggests that the drug may have a nutritional impact when given after cell death [4]. LY-404187 raises GAP-43 immunoreactivity in the striatum in a dose-dependent manner when administered subcutaneously for 14 days at 0.1 and 0.5 mg/kg [4].
|
| Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice (20-25 g) were challenged with MPTP on day 8 [4]
Doses: 0.5 mg/kg Route of Administration: Sc; twice (two times) daily on weekdays and one time/day on weekends for 11 days Experimental Results: Attenuated loss of tyrosine hydroxylase immunoreactivity in the substantia nigra. There were no significant changes in dorsal and ventral striatal tyrosine hydroxylase immunoreactivity. |
| References |
[1]. Quirk JC, et, al. LY404187: a novel positive allosteric modulator of AMPA receptors. CNS Drug Rev. Fall 2002; 8(3): 255-82.
[2]. Miu P, et, al. Novel AMPA receptor potentiators LY392098 and LY404187: effects on recombinant human AMPA receptors in vitro. Neuropharmacology. 2001 Jun; 40(8): 976-83. [3]. Baumbarger PJ, et, al. Positive modulation of alpha-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptors in prefrontal cortical pyramidal neurons by a novel allosteric potentiator. J Pharmacol Exp Ther. 2001 Jul; 298(1): 86-102. [4]. O'Neill MJ, et, al. Neurotrophic actions of the novel AMPA receptor potentiator, LY404187, in rodent models of Parkinson's disease. Eur J Pharmacol. 2004 Feb 20; 486(2): 163-74. |
| Molecular Formula |
C19H22N2O2S
|
|---|---|
| Molecular Weight |
342.46
|
| Exact Mass |
342.1402
|
| CAS # |
211311-95-4
|
| Related CAS # |
211311-95-4;
|
| SMILES |
CC(S(=O)(NCC(C1=CC=C(C2=CC=C(C#N)C=C2)C=C1)C)=O)C References
|
| InChi Key |
HOQAVGZLYRYHSO-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C19H22N2O2S/c1-14(2)24(22,23)21-13-15(3)17-8-10-19(11-9-17)18-6-4-16(12-20)5-7-18/h4-11,14-15,21H,13H2,1-3H3
|
| Chemical Name |
2-Propanesulfonamide, N-(2-(4'-cyano(1,1'-biphenyl)-4-yl)propyl)-
|
| Synonyms |
LY-404187 LY 404187 LY404187.
|
| 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) |
DMSO : ~100 mg/mL (~292.00 mM)
|
|---|---|
| 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 | 2.9200 mL | 14.6002 mL | 29.2005 mL | |
| 5 mM | 0.5840 mL | 2.9200 mL | 5.8401 mL | |
| 10 mM | 0.2920 mL | 1.4600 mL | 2.9200 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
COA