2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. nAChR
  4. Tebanicline dihydrochloride

Tebanicline dihydrochloride  (Synonyms: Ebanicline dihydrochloride; ABT-594 dihydrochloride)

Cat. No.: HY-14316A Purity: ≥98.0%
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Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.

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

Tebanicline dihydrochloride Chemical Structure

Tebanicline dihydrochloride Chemical Structure

CAS No. : 209326-19-2

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Based on 1 publication(s) in Google Scholar

Other Forms of Tebanicline dihydrochloride:

Tebanicline dihydrochloride Related Antibodies

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Description

Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM[1].

IC50 & Target

Ki: 37 pM (nAChR)[1]
In Vitro

Tebanicline is a novel, potent cholinergic nAChR ligand with analgesic properties that shows preferential selectivity for neuronal nAChRs. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM. Functionally, tebanicline is an agonist. At the transfected human α4β2 neuronal nAChR in K177 cells, with increased 86Rb+ efflux as a measure of cation efflux, ABT-594 has an EC50 value of 140 nM with an intrinsic activitycompared with (−)-nicotine of 130%; at the nAChR subtype expressed in IMR-32 cells, an EC50 of 340 nM; at the F11 dorsal root ganglion cell line, an EC50 of 1220 nM; and via direct measurement of ion currents, an EC50 value of 56,000 nM at the human α7 homo-oligimeric nAChR produced in oocytes[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tebanicline dihydrochloride Related Antibodies
In Vivo

Tebanicline is a potent antinociceptive agent with full efficacy in models of acute and persistent pain and that these effects are mediated predominately by an action at central neuronal nAChRs[2]. Tebanicline produces significant antinociceptive effects in mice against both acute noxious thermal stimulation. ABT-594 is orally active, but 10-fold less potent by this route than after i.p. administration. The antinociceptive effect of ABT-594 is prevented, but not reversed, by the noncompetitive neuronal nicotinic acetylcholine receptor antagonist[3]. Tebanicline has antinociceptive effects in rat models of acute thermal, persistent chemical, and neuropathic pain. Direct injection of tebanicline into the nucleus raphe magnus (NRM) is antinociceptive in a thermal threshold test and destruction of serotonergic neurons in the NRM attenuates the effect of systemic tebanicline[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

271.57

Formula

C9H13Cl3N2O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

[H]Cl.ClC(C=C1)=NC=C1OC[C@@H]2NCC2.[H]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: 

H2O : 100 mg/mL (368.23 mM; Need ultrasonic)

DMSO : ≥ 34 mg/mL (125.20 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6823 mL 18.4115 mL 36.8229 mL
5 mM 0.7365 mL 3.6823 mL 7.3646 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (7.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.66 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 25 mg/mL (92.06 mM); Clear solution; Need ultrasonic

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
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥98.0%

COA (249 KB) HNMR (178 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[2][3]

Rats: Rats are dosed with either saline or ABT-594 (0.3 μM/kg i.p.) b.i.d. for 5 days. Treatments are separated by approximately 6 h (i.e., morning and afternoon). In the hot box experiment, animals are tested in the morning and afternoon on days 1, 2 and 5. For each test, a base-line measure is recorded, and then animals are tested 15, 30 and 45 min after treatment. For the afternoon treatment on day 5, all animals received a challenge dose of ABT-594 (0.3 μM/kg i.p.) before being tested. For the motor coordination experiment, animals are tested only in the afternoon on day 5[2].

Mice: Tebanicline is dissolved and diluted in sterile 0.9% saline. The effects of tebanicline are tested for anxiolytic-like activity using the elevated plus-maze procedure. Mice are injected with ABT-594 (0.019, 0.062, or 0.19 μM/kg) or saline, the mouse is placed in the center of the maze and allowed to explore the maze for 5 min. During this period, an auto-mated video tracking system is used to record the time spent on the open arms and the total distance traveled. Diazepam (10.5 μM/kg, i.p). is used as a positive control compound[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 / H2O 1 mM 3.6823 mL 18.4115 mL 36.8229 mL 92.0573 mL
5 mM 0.7365 mL 3.6823 mL 7.3646 mL 18.4115 mL
10 mM 0.3682 mL 1.8411 mL 3.6823 mL 9.2057 mL
15 mM 0.2455 mL 1.2274 mL 2.4549 mL 6.1372 mL
20 mM 0.1841 mL 0.9206 mL 1.8411 mL 4.6029 mL
25 mM 0.1473 mL 0.7365 mL 1.4729 mL 3.6823 mL
30 mM 0.1227 mL 0.6137 mL 1.2274 mL 3.0686 mL
40 mM 0.0921 mL 0.4603 mL 0.9206 mL 2.3014 mL
50 mM 0.0736 mL 0.3682 mL 0.7365 mL 1.8411 mL
60 mM 0.0614 mL 0.3069 mL 0.6137 mL 1.5343 mL
80 mM 0.0460 mL 0.2301 mL 0.4603 mL 1.1507 mL
100 mM 0.0368 mL 0.1841 mL 0.3682 mL 0.9206 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Tebanicline dihydrochloride 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:

Tebanicline209326-19-2EbaniclineABT-594ABT594ABT 594nAChRNicotinic acetylcholine receptorsInhibitorinhibitorinhibit

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