ABT 239 free base · Synonyms: ABT-239 · ABT239
ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 antagonist.
For research use only. Not for human or veterinary use.
ABT 239 structure
CAS No.: 460746-46-7
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 50 mg | USD 420.00 | BP-02175-50mg | In stock | Get quote |
| 100 mg | USD 660.00 | BP-02175-100mg | In stock | Get quote |
| 250 mg | USD 1,320.00 | BP-02175-250mg | In stock | Get quote |
| 500 mg | USD 2,150.00 | BP-02175-500mg | In stock | Get quote |
| 1 g | USD 3,440.00 | BP-02175-1g | In stock | Get quote |
Need another size or custom synthesis? Request a quote.
Description
ABT-239 is a novel, highly efficacious, non-imidazole class of H3R antagonist and a transient receptor potential vanilloid type 1 (TRPV1) antagonist.
Biological activity
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. 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.
Identifiers
- SMILES
-
C[C@H]1N(CCC2=CC3=C(C=CC(C4=CC=C(C#N)C=C4)=C3)O2)CCC1 - InChIKey
-
KFHYZKCRXNRKRC-MRXNPFEDSA-N
Specifications
- MW (average)
- 330.4229
- Formula
- C22H22N2O
- CAS No.
- 460746-46-7
- Physical state
- Solid
- Color
- Light yellow to khaki
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃, 3 years; 4℃, 2 years; In solvent -20℃, 1 year;
Solubility
Soluble in DMSO