| Size | Price | Stock | Qty |
|---|---|---|---|
| 25mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
|
Purity: ≥98%
Lu AE58054 (also known as Idalopirdine) is potent and selective antagonist of the 5-HT(6) receptor with Ki value of 0.83 nM. Lu AE58054, in a 5-HT(6) GTPgammaS efficacy assay, exhibited strong inhibition of 5-HT-mediated activation but no agonist activity. Not only did Lu AE58054 exhibit medium affinity for adrenergic alpha(1A)- and alpha(1B)-adrenoreceptors, but it also showed >50-fold selectivity for over 70 targets that were studied. Phase III clinical trials are being conducted on Lu AE58054 as an augmentation therapy to treat cognitive deficits linked to schizophrenia and Alzheimer's disease.
| Targets |
5-HT6 Receptor ( Ki = 0.83 nM )
|
|
|---|---|---|
| ln Vitro |
|
|
| ln Vivo |
|
|
| Animal Protocol |
Male Wistar rats
5 mg/kg intraperitoneal injection, daily, 28 days |
|
| References |
|
| Molecular Formula |
C₂₀H₁₉F₅N₂O
|
|
|---|---|---|
| Molecular Weight |
398.37
|
|
| Exact Mass |
398.14
|
|
| Elemental Analysis |
C, 60.30; H, 4.81; F, 23.84; N, 7.03; O, 4.02
|
|
| CAS # |
467459-31-0
|
|
| Related CAS # |
Idalopirdine Hydrochloride; 467458-02-2
|
|
| Appearance |
Solid powder
|
|
| SMILES |
C1=CC(=CC(=C1)OCC(C(F)F)(F)F)CNCCC2=CNC3=C2C=CC(=C3)F
|
|
| InChi Key |
YBAWYTYNMZWMMJ-UHFFFAOYSA-N
|
|
| InChi Code |
InChI=1S/C20H19F5N2O/c21-15-4-5-17-14(11-27-18(17)9-15)6-7-26-10-13-2-1-3-16(8-13)28-12-20(24,25)19(22)23/h1-5,8-9,11,19,26-27H,6-7,10,12H2
|
|
| Chemical Name |
2-(6-fluoro-1H-indol-3-yl)-N-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]methyl]ethanamine
|
|
| Synonyms |
|
|
| 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) |
|
|||
|---|---|---|---|---|
| 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 | 2.5102 mL | 12.5511 mL | 25.1023 mL | |
| 5 mM | 0.5020 mL | 2.5102 mL | 5.0205 mL | |
| 10 mM | 0.2510 mL | 1.2551 mL | 2.5102 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02019394 | Completed | Drug: Lu AE58054 | Healthy | H. Lundbeck A/S | December 2013 | Phase 1 |
| NCT02122692 | Completed | Drug: Lu AE58054 30 mg Drug: Itraconazole |
Healthy Volunteers | H. Lundbeck A/S | March 2014 | Phase 1 |
| NCT02231450 | Completed | Drug: Lu AE58054 encapsulated film-coated tablets |
Heptic Impairment | H. Lundbeck A/S | July 2014 | Phase 1 |
| NCT01019421 | Completed | Drug: Lu AE58054 Drug: Placebo |
Alzheimer's Disease | H. Lundbeck A/S | December 2009 | Phase 2 |
| NCT00810667 | Completed | Drug: Lu AE58054 Drug: Placebo |
Schizophrenia Cognition |
H. Lundbeck A/S | November 2008 | Phase 2 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
