Ampreloxetine hydrochloride
Based on 1 Customer Validation
Ampreloxetine (TD-9855) hydrochloride is an orally active and CNS-penetrant inhibitor of Norepinephrine transporter (NET) and Serotonin 5-HT uptake transporter (SERT), but not Dopamine transporter (DAT). Ampreloxetine hydrochloride binds norepinephrine transporters (NET) and serotonin transporters (SERT) with EC50 values of 11.7 ng/mL and 50.8 ng/mL, respectively, in plasma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.43%
- CAS. Nr.: 1227056-87-2
- Formel: C18H19ClF3NO
- Molecular Weight:357.80
-
Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
-
Biologische Aktivität
-
Chemical Information
-
Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
-
Neuronal Signaling Compound Library
HY-L013
-
Clinical Compound Library
HY-L026
-
CNS-Penetrant Compound Library
HY-L028
-
Drug Repurposing Compound Library
HY-L035
-
Orally Active Compound Library
HY-L061
-
Antidepressant Compound Library
HY-L108
-
Coagulation and Anti-coagulation Compound Library
HY-L136
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Multi-Target Compound Library
HY-L176
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
Biologische Aktivität
|
human Norepinephrine transporter 8.0 (pIC50) |
human Serotonin transporter 8.6 (pIC50) |
rat Norepinephrine transporter 7.9 (pIC50) |
rat Serotonin transporter 8.9 (pIC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Rat[1]
-
Dosage:0.3, 1, 5, 10, 30, and 60mg/kg
-
Administration:PO; euthanized by decapitation at 0.5, 2, 4, 6, and 8 hr for 5mg/ kg dose level; 2 hr for 0.3, 1, 10, 30, and 60mg/kg dose levels
-
Result:In the effect compartment PK/PD analysis for NET and SERT occupancy, the estimated EC50 for occupancy was 11.7ng/mL for NET and 50.8ng/mL for SERT in rat spinal cords, and the projected human plasma EC50 values were 5.5ng/mL for NET and 23.9ng/mL for SERT.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 1227056-87-2
-
Appearance Solid
-
Molecular Weight 357.80
-
Formel C18H19ClF3NO
-
Color White to off-white
-
SMILES
FC1=C(C(F)=CC(F)=C1)OCC2=C(C3CCNCC3)C=CC=C2.Cl
-
Synonyms
TD-9855 hydrochloride
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (279.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Reinheit & Dokumentation
-
Data Sheet (275 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
-
Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.7949 mL | 13.9743 mL | 27.9486 mL | 69.8714 mL |
| 5 mM | 0.5590 mL | 2.7949 mL | 5.5897 mL | 13.9743 mL | |
| 10 mM | 0.2795 mL | 1.3974 mL | 2.7949 mL | 6.9871 mL | |
| 15 mM | 0.1863 mL | 0.9316 mL | 1.8632 mL | 4.6581 mL | |
| 20 mM | 0.1397 mL | 0.6987 mL | 1.3974 mL | 3.4936 mL | |
| 25 mM | 0.1118 mL | 0.5590 mL | 1.1179 mL | 2.7949 mL | |
| 30 mM | 0.0932 mL | 0.4658 mL | 0.9316 mL | 2.3290 mL | |
| 40 mM | 0.0699 mL | 0.3494 mL | 0.6987 mL | 1.7468 mL | |
| 50 mM | 0.0559 mL | 0.2795 mL | 0.5590 mL | 1.3974 mL | |
| 60 mM | 0.0466 mL | 0.2329 mL | 0.4658 mL | 1.1645 mL | |
| 80 mM | 0.0349 mL | 0.1747 mL | 0.3494 mL | 0.8734 mL | |
| 100 mM | 0.0279 mL | 0.1397 mL | 0.2795 mL | 0.6987 mL |
Powered by Bioz