2. Neuronal Signaling
  3. Serotonin Transporter
  4. Ampreloxetine hydrochloride

Ampreloxetine hydrochloride  (Synonyms: TD-9855 hydrochloride)

Cat. No.: HY-107128 Purity: 99.47%
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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.

For research use only. We do not sell to patients.

Ampreloxetine hydrochloride Chemical Structure

Ampreloxetine hydrochloride Chemical Structure

CAS No. : 1227056-87-2

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5 mg USD 240 In-stock
10 mg USD 390 In-stock
25 mg USD 780 In-stock
50 mg USD 1250 In-stock
100 mg USD 2000 In-stock
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Based on 1 publication(s) in Google Scholar

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Ampreloxetine hydrochloride Related Antibodies

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Description

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].

IC50 & Target[1]

human Norepinephrine transporter

8.0 (pIC50)

human Serotonin transporter

8.6 (pIC50)

rat Norepinephrine transporter

7.9 (pIC50)

rat Serotonin transporter

8.9 (pIC50)

In Vivo

Ampreloxetine hydrochloride (0.3-60 mg/kg; PO; single dose) is irrespective between plasma concentration and dose level in rat model[1].

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.
Clinical Trial
Molecular Weight

357.80

Formula

C18H19ClF3NO
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

FC1=C(C(F)=CC(F)=C1)OCC2=C(C3CCNCC3)C=CC=C2.Cl
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
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7949 mL 13.9743 mL 27.9486 mL
5 mM 0.5590 mL 2.7949 mL 5.5897 mL
View the 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.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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Ampreloxetine hydrochloride Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ampreloxetine1227056-87-2TD-9855TD9855TD 9855Serotonin Transporter5-HTTSERTSLC6A4orally activeCNS-penetrantNorepinephrine transporterSerotonin 5-HT uptake transporterDopamine transporterInhibitorinhibitorinhibit

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