[CAS NO. 916918-84-8] Ansofaxine hydrochloride
PRODUCTS SPECIFICATIONS [916918-84-8]
DESCRIPTION [916918-84-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 417.97 |
| Molecular Formula | C24H32ClNO3 |
| SMILES | O=C(OC1=CC=C(C(C2(O)CCCCC2)CN(C)C)C=C1)C3=CC=C(C)C=C3.[H]Cl |
Summary
Ansofaxine hydrochloride (LY03005; LPM570065) is a triple reuptake inhibitor; inhibits serotonin , dopamine and norepinephrine reuptake with IC 50 values of 723, 491 and 763 nM, respectively.
IC50 & Target
|
serotonin 723 nM (IC 50 ) |
Dopamine Receptor 491 nM (IC 50 ) |
In Vivo
Ansofaxine rapidly penetrates the rat striatum, converts into desvenlafaxine and exhibits larger total exposure compared with the administration of desvenlafaxine. Acute and chronic administration of oral suspension of ansofaxine increases the 5-HT, dopamine and norepinephrine levels more than the relative administration of desvenlafaxine. Unlike desvenlafaxine, acute administration of an intravenous ansofaxine solution does not induce the undesirable 90% decrease in extracellular 5-HT levels. The acute administration of ansofaxine shows a capped increase in extracellular 5-HT levels when combined with WAY-100635. Acute and chronic administration of ansofaxine reduces the immobility time more than the relative administration of desvenlafaxine [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02988024 | Luye Pharma Group Ltd. |
Major Depression
|
December 7, 2016 | Phase 1 |
| NCT04853407 | Luye Pharma Group Ltd. |
Major Depressive Disorder (MDD)
|
December 5, 2018 | Phase 3 |
| NCT02271412 | Luye Pharma Group Ltd. |
Major Depressive Disorder, Recurrent, Unspecified
|
October 2014 | Phase 1 |
| NCT03785652 | Luye Pharma Group Ltd.|Shandong Luye Pharmaceutical Co., Ltd. |
Major Depressive Disorder
|
October 9, 2015 | Phase 1 |
| NCT02055300 | Luye Pharma Group Ltd. |
Major Depressive Disorder
|
February 2014 | Phase 1 |
| NCT03822065 | Luye Pharma Group Ltd. |
Major Depressive Disorder
|
January 16, 2019 | Phase 1 |
| NCT03733574 | Luye Pharma Group Ltd. |
Major Depressive Disorder
|
June 19, 2018 | Phase 1 |
| NCT03357796 | Luye Pharma Group Ltd. |
Major Depressive Disorder
|
November 27, 2017 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvent & Solubility
DMSO : 31.25 mg/mL ( 74.77 mM ; Need ultrasonic)
H 2 O : 6.67 mg/mL ( 15.96 mM ; ultrasonic and warming and heat to 60°C)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.3925 mL | 11.9626 mL | 23.9252 mL |
| 5 mM | 0.4785 mL | 2.3925 mL | 4.7850 mL |
| 10 mM | 0.2393 mL | 1.1963 mL | 2.3925 mL |