B3561

BAY 73-6691

≥98% (HPLC), powder

• Synonim(y): 1-(2-Chlorophenyl)-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
• Wzór empiryczny (zapis Hilla): C₁₅H₁₂ClF₃N₄O
• Numer CAS: 794568-92-6
• Masa cząsteczkowa: 356.73
• Numer MDL: MFCD08705319
• Kod UNSPSC: 41106305
• Identyfikator substancji w PubChem: 24724419
• NACRES: NA.77

Właściwości

• Poziom jakości: 100
• Próba: ≥98% (HPLC)
• Postać: powder
• kolor: off-white
• rozpuszczalność: DMSO: >20 mg/mL
• inicjator: Bayer
• temp. przechowywania: 2-8°C
• ciąg SMILES: C[C@H](CC1=Nc2c(cnn2-c3ccccc3Cl)C(=O)N1)C(F)(F)F
• InChI: 1S/C15H12ClF3N4O/c1-8(15(17,18)19)6-12-21-13-9(14(24)22-12)7-20-23(13)11-5-3-2-4-10(11)16/h2-5,7-8H,6H2,1H3,(H,21,22,24)/t8-/m1/s1
• Klucz InChI: FFPXPXOAFQCNBS-MRVPVSSYSA-N

Opis

Zastosowanie

BAY 73-6691 has been used as a phosphodiesterase 9 inhibitor in ischemic heart samples and in structural studies. It may be used as a PDE 9 inhibitor in neuroblastoma SH-SY5Y cells.

Działania biochem./fizjol.

BAY 73-6691 was characterized in vitro as the first potent and selective inhibitor of phosphodiesterase 9 (PDE9), which is currently under preclinical development for the treatment of Alzheimer′s disease. This compound selectively inhibits human (IC₅₀ = 55 nM) and murine (IC₅₀ = 100 nM) PDE9 activity in vitro and shows only moderate activity against other cyclic nucleotide-specific phosphodiesterases. BAY 73-6691 alone did not significantly increase basal cGMP levels. The PDE9 inhibitor significantly potentiated the cGMP signals generated by sGC activating compounds such as BAY 58-2667 or 5-cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine (BAY 41-2272) and induced leftward shifts of the corresponding concentration-response curves. The newly generated PDE9 reporter cell line show that BAY 73-6691 is able to efficiently penetrate cells and to inhibit intracellular PDE9 activity.†

Cechy i korzyści

This compound is a featured product for Cyclic Nucleotide research. Click here to discover more featured Cyclic Nucleotide products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound is featured on the Phosphodiesterases page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

This compound was developed by Bayer. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

This page may contain text that has been machine translated.

Informacja o środkach bezpieczeństwa

• Piktogramy: GHS06
• Hasło ostrzegawcze: Danger
• Zwroty wskazujące rodzaj zagrożenia: H300,H315,H319,H335,H413
• Zwroty wskazujące środki ostrożności: P273 - P301 + P310 + P330 - P302 + P352 - P305 + P351 + P338
• Klasyfikacja zagrożeń: Acute Tox. 2 Oral - Aquatic Chronic 4 - Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3
• Organy docelowe: Respiratory system
• Kod klasy składowania: 6.1A - Combustible acute toxic Cat. 1 and 2 / very toxic hazardous materials
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable
• Środki ochrony indywidualnej: Eyeshields, Faceshields, Gloves, type P2 (EN 143) respirator cartridges