Buy Ampreloxetine (USANTooltip) Cas 1227056-84-9
Buy Ampreloxetine (USANTooltip) Cas 1227056-84-9
Buy Ampreloxetine (USANTooltip) Cas 1227056-84-9
Ampreloxetine (INNTooltip International Nonproprietary Name, USANTooltip United States Adopted Name; developmental code name TD-9855) is a selective norepinephrine reuptake inhibitor (NRI) which is under development for the treatment of symptomatic neurogenic orthostatic hypotension (NOH).[2][3][4]
It shows high affinity for both the norepinephrine transporter (NET) and the serotonin transporter (SERT), with 4-fold selectivity for the NET over the SERT, and is thought to act as a dual serotonin–norepinephrine reuptake inhibitor (SNRI) at higher doses.[4][1]
As of November 2023, ampreloxetine is in phase 3 clinical trials for NOH.[2] The drug was also under development for the treatment of attention deficit hyperactivity disorder (ADHD) and fibromyalgia, but development for these uses was discontinued.[2][5]
References
- Kanodia J, Lo A, Baldwin RM, Graham RA, Bourdet DL (January 2021). “Pharmacokinetics of Ampreloxetine, a Norepinephrine Reuptake Inhibitor, in Healthy Subjects and Adults with Attention-Deficit/Hyperactive Disorder or Fibromyalgia Pain”. Clin Pharmacokinet. 60 (1): 121–131. doi:10.1007/s40262-020-00918-7. PMC 7808980. PMID 32856281.
- “Ampreloxetine – Theravance Biopharma”. AdisInsight. 21 November 2023. Retrieved 26 September 2024.
- Hoxhaj P, Shah S, Muyolema Arce VE, Khan W, Sadeghzadegan A, Singh S, Collado GF, Goyal A, Khawaja I, Botlaguduru D, Razzaq W, Abdin ZU, Gupta I (May 2023). “Ampreloxetine Versus Droxidopa in Neurogenic Orthostatic Hypotension: A Comparative Review”. Cureus. 15 (5) e38907. doi:10.7759/cureus.38907. PMC 10257554. PMID 37303338.
- Smith JA, Bourdet DL, Daniels OT, Ding YS, Gallezot JD, Henry S, Kim KH, Kshirsagar S, Martin WJ, Obedencio GP, Stangeland E, Tsuruda PR, Williams W, Carson RE, Patil ST (December 2014). “Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor”. Int J Neuropsychopharmacol. 18 (2). doi:10.1093/ijnp/pyu027. PMC 4368888. PMID 25522383.
- Pozzi M, Bertella S, Gatti E, Peeters GG, Carnovale C, Zambrano S, Nobile M (December 2020). “Emerging drugs for the treatment of attention-deficit hyperactivity disorder (ADHD)”. Expert Opin Emerg Drugs. 25 (4): 395–407. doi:10.1080/14728214.2020.1820481. hdl:2434/851076. PMID 32938246.
Ampreloxetine (TD-9855) is a potent monoamine reuptake inhibitor with pIC50 of 8.0, 8.6 and 6.8 for human NET, SERT, and DAT, respectively.
Ampreloxetine displays an inhibitory selectivity of 4- to 10-fold for NE at human and rat transporter.
Ampreloxetine engaged norepinephrine transporters (NET) and serotonin transporters (SERT) in rat spinal cord, with a plasma EC50 of 11.7 ng/mL and 50.8 ng/mL, respectively.
TD-9855 is an investigational dual norepinephrine (NE) and serotonin (5-HT) reuptake inhibitor with selectivity for NE over 5-HT (NSRI).
4-(2-(2,4,6-Trifluorophenoxymethyl)phenyl)piperidine
- CAS No.
- 1227056-84-9
- Chemical Name:
- 4-(2-(2,4,6-Trifluorophenoxymethyl)phenyl)piperidine
- Synonyms
- TD9855;TD-9855;4-(2-(2,4,6-Trifluorophenoxymethyl)phenyl)piperidine;Piperidine, 4-[2-[(2,4,6-trifluorophenoxy)methyl]phenyl]-
- CBNumber:
- CB05419911
- Molecular Formula:
- C18H18F3NO
- Molecular Weight:
- 321.34
- MDL Number:
- MOL File:
- 1227056-84-9.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| Ampreloxetine | CS-0068698 | 5mg | $260 |
| Ampreloxetine | CS-0068698 | 10mg | $422 |
| Ampreloxetine | CS-0068698 | 25mg | $845 |
| Ampreloxetine | CS-0068698 | 50mg | $1354 |
| Ampreloxetine | CS-0068698 | 100mg | $2167 |
| form | Liquid |
|---|---|
| color | Colorless to light yellow |
| FDA UNII | 19997EZ42I |
4-(2-(2,4,6-Trifluorophenoxymethyl)phenyl)piperidine price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| ChemScene | CS-0068698 | Ampreloxetine | 1227056-84-9 | 5mg | $260 | 2026-06-04 | Buy |
| ChemScene | CS-0068698 | Ampreloxetine | 1227056-84-9 | 10mg | $422 | 2026-06-04 | Buy |
| ChemScene | CS-0068698 | Ampreloxetine | 1227056-84-9 | 25mg | $845 | 2026-06-04 | Buy |
| ChemScene | CS-0068698 | Ampreloxetine | 1227056-84-9 | 50mg | $1354 | 2026-06-04 | Buy |
| ChemScene | CS-0068698 | Ampreloxetine | 1227056-84-9 | 100mg | $2167 | 2026-06-04 | Buy |
4-(2-(2,4,6-Trifluorophenoxymethyl)phenyl)piperidine Chemical Properties, Uses, Production
Uses
Ampreloxetine (TD-9855) is a potent and orally active norepinephrine (NE) and serotonin 5-HT inhibitor. Ampreloxetine has the potential for the research of neurogenic orthostatic hypotension[1][2].
in vivo
Ampreloxetine (0.3, 1, 5, 10, 30, 60 mg/kg; p.o.; single dose) shows a plasma EC50s of 11.7ng/mL and 50.8ng/mL in rat, respectively[1].
| Animal Model: | Male Sprague Dawley rats[1] |
| Dosage: | 0.3, 1, 5, 10, 30, 60 mg/kg |
| Administration: | P.o.; single dose |
| Result: | Showed good PK and PD parameter with Emax of 79%, 92% for SERT and NET, respectively; EC50 values of 50.8, 11.7 ng/mL for SERT, NET, respectively. |
IC 50
5-HT Receptor
References
[1] Smith JA, et al. Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor. Int J Neuropsychopharmacol. 2014 Dec 13;18(2):pyu027. DOI:10.1093/ijnp/pyu027
[2] Kaufmann H, et al. Safety and efficacy of ampreloxetine in symptomatic neurogenic orthostatic hypotension: a phase 2 trial. Clin Auton Res. 2021 Dec;31(6):699-711. DOI:10.1007/s10286-021-00827-0
4-(2-(2,4,6-Trifluorophenoxymethyl)phenyl)piperidine Preparation Products And Raw materials
Raw materials
Preparation Products
Ampreloxetine（Cat No.:I009729）is an investigational selective norepinephrine reuptake inhibitor (NRI) being developed for the treatment of major depressive disorder (MDD) and attention-deficit hyperactivity disorder (ADHD). By increasing the levels of norepinephrine in the brain, Ampreloxetine aims to improve mood, attention, and cognitive function in individuals with these conditions. Preclinical and early clinical studies suggest it may offer benefits over traditional antidepressants by targeting specific neurotransmitter pathways. Ongoing clinical trials are evaluating its safety, efficacy, and potential as a new therapeutic option for patients with MDD, ADHD, and other related disorders.
| CAS Number | 1227056-84-9 |
| Synonyms | 4-[2-[(2,4,6-trifluorophenoxy)methyl]phenyl]piperidine |
| Molecular Formula | C18H18F3NO |
| Purity | ≥95% |
| IUPAC Name | 4-[2-[(2,4,6-trifluorophenoxy)methyl]phenyl]piperidine |
| InChI | InChI=1S/C18H18F3NO/c19-14-9-16(20)18(17(21)10-14)23-11-13-3-1-2-4-15(13)12-5-7-22-8-6-12/h1-4,9-10,12,22H,5-8,11H2 |
| InChIKey | TZIALEBTHQWNAO-UHFFFAOYSA-N |
| SMILES | C1CNCCC1C2=CC=CC=C2COC3=C(C=C(C=C3F)F)F |
| Chemistry Calculators | Dilution Calculator In vivo Formulation Calculator Molarity Calculator Molecular Weight Calculator Reconstitution Calculator |
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