2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Membrane Transporter/Ion Channel
  3. Histamine Receptor TRP Channel
  4. ABT-239

ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist. 

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

ABT-239 Chemical Structure

ABT-239 Chemical Structure

CAS No. : 460746-46-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 190 In-stock
25 mg USD 380 In-stock
50 mg USD 570 In-stock
100 mg USD 800 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

ABT-239 Related Antibodies

Top Publications Citing Use of Products

View All Histamine Receptor Isoform Specific Products:

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

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TRPC TRPM TRPV TRPA TRPML

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist. 

IC50 & Target

H3 receptor

 

In Vitro

Perfusion of the TMN with ABT-239 (10 μM) increases histamine release from the TMN, NBM, and cortex, but not from the striatum or NAcc. TMN perfusion with ABT-239 activates c-Fos selectively in the NBM and cortex[4].

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

ABT-239 Related Antibodies
In Vivo

ABT-239 (3 mg/kg, i.p.) significantly delays onset of seizure, reduces behavioral seizures elicited by KA, and reduces in the incidence of head bobbing and forelimb clonus in mice. ABT-239 (1 mg/kg, i.p.) in conbination with sub-therapeutic dose of SVP (150 mg/kg, i.p.), significantly decreases the number of immobility, head bobbing and forelimb clonus, where as a higher dose combination of ABT-239 (3 mg/kg, i.p.) causes enhanced reduction in all the stages. ABT-239 (3 mg/kg, i.p.) and TDZD-8 (10 mg/kg, i.p.) have more powerful reduction in the number of pyknotic neurons in mice hippocampi. The high dose combination of ABT-239 and TDZD-8 produces the most pronounced increase in Bcl-2 expression as well as decrease in the level of Bax[1]. ABT-239 (3 mg/kg, i.p.) administration transforms a short-term learning event into a long-term remembered experience in WT but not in histamine-depleted mice[2]. Concomitant administration of either ABT-239 (1 and 3 mg/kg, i.p.) and nicotine (0.035 mg/kg, i.p.), or ABT-239 (0.1 mg/kg, i.p.) and nicotine (0.0175 mg/kg, i.p.) further increases nicotine-induced improvement in both memory acquisition and consolidation[3].

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

330.42

Formula

C22H22N2O
CAS No.
Appearance

Solid

Color

Light yellow to khaki

SMILES

C[C@H]1N(CCC2=CC3=C(C=CC(C4=CC=C(C#N)C=C4)=C3)O2)CCC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (302.65 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0265 mL 15.1323 mL 30.2645 mL
5 mM 0.6053 mL 3.0265 mL 6.0529 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • 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: ≥ 2.5 mg/mL (7.57 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: 2.5 mg/mL (7.57 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
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).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Animal Administration
[1]

Solutions of KA, ABT-239 and SVP are prepared in pyrogen-free normal saline for injection except for TDZD-8, which is dissolved in 10% DMSO and are administered intraperitoneally in a volume not exceeding 10 mL/kg. The animals are divided into ten groups. The first group (CTRL) receive vehicle (0.9% sodium chloride) only whereas animals in the second group (VEH) are given vehicle followed by KA at a dose of 10 mg/kg, i.p. (pH 7.2±1), this being the dose that induces low-grade seizures (stage 0-4) in all the animals without any mortality in a range finding study. The KA dose employs to evoke SE in mice in various studies mostly varied from as low as 6-20 mg/kg to as high as 25-45 mg/kg. Animals in the next two groups are administered ABT-239 in increasing doses of 1 (AL) and 3 mg/kg (AH) 30 min before KA challenge. These doses ranging from 0.1 to 3 mg/kg of ABT-239 display disease modifying attributes in a mice model of Alzheimer׳s disease as well as improved cognitive functions. The fifth and sixth group receive graduated doses of 150 (SL) and 300 mg/kg (SH) of SVP 30 min prior to KA injection. The seventh and eight group receive combinations of subeffective dose (maximum possible dose at which there is no protection) of SVP at 150 mg/kg with ABT-239 at 1 (SLAL) and 3 mg/kg (SLAH) respectively followed 30 min later by KA. The remaining two groups receive low dose combination at 1 and 5 mg/kg (ALTL) and a high dose combination at 3 and 10 mg/kg (AHTH) of ABT-239 and TDZD-8, respectively before KA exposure. The doses of TDZD-8 chosen are based on previous studies where doses ranging from 1 to 10 mg/kg reduced inflammation and tissue injury as well as improve psychiatric conditions.

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.0265 mL 15.1323 mL 30.2645 mL 75.6613 mL
5 mM 0.6053 mL 3.0265 mL 6.0529 mL 15.1323 mL
10 mM 0.3026 mL 1.5132 mL 3.0265 mL 7.5661 mL
15 mM 0.2018 mL 1.0088 mL 2.0176 mL 5.0441 mL
20 mM 0.1513 mL 0.7566 mL 1.5132 mL 3.7831 mL
25 mM 0.1211 mL 0.6053 mL 1.2106 mL 3.0265 mL
30 mM 0.1009 mL 0.5044 mL 1.0088 mL 2.5220 mL
40 mM 0.0757 mL 0.3783 mL 0.7566 mL 1.8915 mL
50 mM 0.0605 mL 0.3026 mL 0.6053 mL 1.5132 mL
60 mM 0.0504 mL 0.2522 mL 0.5044 mL 1.2610 mL
80 mM 0.0378 mL 0.1892 mL 0.3783 mL 0.9458 mL
100 mM 0.0303 mL 0.1513 mL 0.3026 mL 0.7566 mL
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ABT-239 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:

ABT-239460746-46-7ABT239ABT 239Histamine ReceptorTRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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