7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine
![7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine Structure](CAS/20180601/GIF/252977-51-8.gif)
- CAS No.
- 252977-51-8
- Chemical Name:
- 7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine
- Synonyms
- TPA 023;TPA 023, 10 mM in DMSO;7-tert-butyl-6-[(2-ethyl-1,2,4-triazol-3-yl)methoxy]-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine;7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine;inhibit,γ-Aminobutyric acid Receptor,TPA 023,Inhibitor,Gamma-aminobutyric acid Receptor,TPA-023,GABA Receptor,TPA023;1,2,4-Triazolo[4,3-b]pyridazine, 7-(1,1-dimethylethyl)-6-[(1-ethyl-1H-1,2,4-triazol-5-yl)methoxy]-3-(2-fluorophenyl)-;7-(tert-Butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine , TPA 023
- CBNumber:
- CB83164844
- Molecular Formula:
- C20H22FN7O
- Molecular Weight:
- 395.43
- MDL Number:
- MFCD29921350
- MOL File:
- 252977-51-8.mol
- MSDS File:
- SDS
- TDS File:
- TDS
| Product description | Number | Pack Size | Price |
| TPA023 ≥98% (HPLC) | SML2447 | 5MG | $107 |
| TPA023 ≥98% (HPLC) | SML2447 | 25MG | $348 |
| TPA 023 99.75% | orb1307656 | 1mg | $110 |
| TPA 023 99.75% | orb1307656 | 5mg | $180 |
| TPA 023 99.75% | orb1307656 | 1mlx10mM(inDMSO) | $190 |
7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine Properties
| Density | 1.33±0.1 g/cm3(Predicted) |
|---|---|
| storage temp. | 2-8°C |
| solubility | Soluble in DMSO |
| pka | 2.08±0.10(Predicted) |
| form | Solid |
| color | White to off-white |
| InChI | 1S/C20H22FN7O/c1-5-27-17(22-12-23-27)11-29-19-14(20(2,3)4)10-16-24-25-18(28(16)26-19)13-8-6-7-9-15(13)21/h6-10,12H,5,11H2,1-4H3 |
| InChIKey | QKIWQBLNTSQOLY-UHFFFAOYSA-N |
| SMILES | CC(C)(C)C1=CC2=NN=C(C3=CC=CC=C3F)N2N=C1OCC4=NC=NN4CC |
| FDA UNII | 1FI3KTC550 |
| UNSPSC Code | 12352200 |
| NACRES | NA.77 |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302-H315-H319-H335 |
| Precautionary statements | P261-P305+P351+P338 |
| WGK Germany | WGK 3 |
| Storage Class | 11 - Combustible Solids |
7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine price
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML2447 | TPA023 ≥98% (HPLC) | 252977-51-8 | 5MG | $107 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML2447 | TPA023 ≥98% (HPLC) | 252977-51-8 | 25MG | $348 | 2026-04-30 | Buy |
| Biorbyt Ltd | orb1307656 | TPA 023 99.75% | 252977-51-8 | 1mg | $110 | 2026-05-06 | Buy |
| Biorbyt Ltd | orb1307656 | TPA 023 99.75% | 252977-51-8 | 5mg | $180 | 2026-05-06 | Buy |
| Biorbyt Ltd | orb1307656 | TPA 023 99.75% | 252977-51-8 | 1mlx10mM(inDMSO) | $190 | 2026-05-06 | Buy |
7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine Chemical Properties,Uses,Production
Uses
TPA 023 is a GABAA α2/α3 subtype-selective agonist, with Ki of 0.19-0.41 nM.
Biological Activity
TPA023 is a highly potent, functionally selective agonist for α2-, α3-, and α5GABAA receptors th at shows zero efficacy at a1GABAA subtypes. TPA023 exhibits anxiolytic and anticonvulsant effects in both animals and humans but lacks sedative effects and abuse potential.
in vivo
TPA023 displays good receptor occupancy, when administered orally to rats. The dose of TPA023 resulting in 50% occupancy of rat brain GABAA receptors is 0.42 mg/kg, with the corresponding plasma concentration being 25 ng/mL. TPA023 is also efficacious in the mouse pentylenetetrazole-induced seizure model, providing full seizure protection at a dose of 10 mg/kg i.p. (84% occupancy), with the ED50 of 0.19-0.41 nM, for protection against tonic convulsions (1.4 mg/kg i.p.) corresponding to around 50% occupancy. TPA023 (3 mg/kg p.o. in 0.5% methyl cellulose) shows anxiolytic-like effect on rats[1]. TPA023 (0.7, 2.0, and 5 mg/kg, p.o.) blocks ketamine's cognitive-impairing ability but does not influence the behavioral symptoms of rhesus monkeys[2].
References
[1] Atack JR. Subtype-selective GABA(A) receptor modulation yields a novel pharmacological profile: the design and development of TPA023. Adv Pharmacol. 2009;57:137-85 DOI:10.1016/S1054-3589(08)57004-9
[2] Castner SA, et al. Reversal of ketamine-induced working memory impairments by the GABAAalpha2/3 agonist TPA023. Biol Psychiatry. 2010 May 15;67(10):998-1001. DOI:10.1016/j.biopsych.2010.01.001
7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine Preparation Products And Raw materials
Raw materials
Preparation Products
7-(tert-butyl)-6-((1-ethyl-1H-1,2,4-triazol-5-yl)methoxy)-3-(2-fluorophenyl)-[1,2,4]triazolo[4,3-b]pyridazine Suppliers
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| TargetMol Chemicals Inc. | +1-781-999-5354; +17819995354 | marketing@targetmol.com | United States | 32466 | 58 |
| Jilin Chinese Academy of Sciences-yanshen Technology | +undefined18143011203 | info@chemextension.com | China | 42056 | 58 |
| Shanghai EFE Biological Technology Co., Ltd. | 021-65675885 18964387627 | info@efebio.com | China | 9804 | 58 |
| Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9729 | 58 |
| Chengdu Feibai Pharmaceutical Co., Ltd. | 028-84641798 18782128315 | 3302391190@qq.com | China | 5267 | 55 |
| Xi'an Minze Pharmaceutical Technology Co., Ltd | 13981836672 | 2560370848@qq.com | China | 2807 | 58 |
| ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11218 | 58 |
| cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 10336 | 58 |
| Hubei Co-prosperity Medicine Technonlogy Co., Ltd | 2383948258 19172820304 | 2383948258@qq.com | China | 12987 | 58 |
| Beijing Jin Ming Biotechnology Co., Ltd. | 010-60605840 15801484223; | psaitong@jm-bio.com | China | 29757 | 58 |
