1. GPCR/G Protein
    Immunology/Inflammation
    Membrane Transporter/Ion Channel
  2. Histamine Receptor
    TRP Channel

ABT-239 

Cat. No.: HY-12195 Purity: 98.94%
Handling Instructions

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
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 211 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 312 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
25 mg USD 660 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 1188 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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

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].

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].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 3.4 mg/mL (10.29 mM)

*"≥" 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
10 mM 0.3026 mL 1.5132 mL 3.0265 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

330.42

Formula

C₂₂H₂₂N₂O

CAS No.

460746-46-7

SMILES

C[[email protected]]1N(CCC2=CC3=C(C=CC(C4=CC=C(C#N)C=C4)=C3)O2)CCC1

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
ABT-239
Cat. No.:
HY-12195
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ABT-239

Cat. No.: HY-12195