Intermediate
- CAS No.
- 1227056-87-2
- Chemical Name:
- Intermediate
- Synonyms
- TD-9855 HCl;Ampreloxetine hydrochloride
- CBNumber:
- CB24693864
- Molecular Formula:
- C18H18F3NO.ClH
- Molecular Weight:
- 357.8
- MDL Number:
- MOL File:
- 1227056-87-2.mol
| form | Solid |
|---|---|
| color | White to off-white |
| FDA UNII | WC7U64G379 |
Intermediate Chemical Properties,Uses,Production
Uses
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[1].
in vivo
Ampreloxetine hydrochloride (0.3-60 mg/kg; PO; single dose) is irrespective between plasma concentration and dose level in rat model[1].
| 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. |
IC 50
human Norepinephrine transporter: 8.0 (pIC50); human Serotonin transporter: 8.6 (pIC50); rat Norepinephrine transporter: 7.9 (pIC50); rat Serotonin transporter: 8.9 (pIC50)
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
Intermediate Preparation Products And Raw materials
Raw materials
Preparation Products
Intermediate Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai YuanYe Biotechnology Co., Ltd. | 021-61312847; 18021002903 | 3008007409@qq.com | China | 71826 | 60 |
| Shanghai Dexuan Pharmaceutical Technology Co., Ltd | 1701086315 | dexuanpharma@126.com | China | 9475 | 58 |
| Suzhou Zhixin Biotechnology Co., Ltd. | 0512-65118909 15162312715 | sales@szzxbio.com | China | 2978 | 58 |
| Shanghai Yifei Biotechnology Co. , Ltd. | 021-65675885 18964387627 | customer_service@efebio.com | China | 11973 | 58 |
| TargetMol Chemicals Inc. | 15002134094 | marketing@targetmol.cn | China | 19988 | 58 |
| Sangon Biotech (Shanghai) Co.,Ltd. | 400-821-026 | Sales@sangon.com | China | 55710 | 58 |