SML2732

DO34

≥98% (HPLC)

• Synonym(e): (2-Benzyl-4-{[(2-methyl-2-propanyl)oxy]carbonyl}piperazinyl){4-[(4-trifluoromethoxy)phenyl]-1H-1,2,3-triazol-1-yl}methanone, 3-(Phenylmethyl)-4-[[4-[4-(trifluoromethoxy)phenyl]-1H-1,2,3-triazol-1-yl]carbonyl]-1-piperazinecarboxylic acid, 1,1-dimethylethyl ester
• Empirische Formel (Hill-System): C₂₆H₂₈F₃N₅O₄
• CAS-Nummer: 1848233-58-8
• Molekulargewicht: 531.53
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD31807614
• Assay: ≥98% (HPLC)
• Form: powder

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: −20°C
• SMILES string: O=C(N1CCN(CC1CC2=CC=CC=C2)C(OC(C)(C)C)=O)N3N=NC(C4=CC=C(C=C4)OC(F)(F)F)=C3
• InChI: 1S/C26H28F3N5O4/c1-25(2,3)38-24(36)32-13-14-33(20(16-32)15-18-7-5-4-6-8-18)23(35)34-17-22(30-31-34)19-9-11-21(12-10-19)37-26(27,28)29/h4-12,17,20H,13-16H2,1-3H3
• InChI key: CQGMWUWJVBKTRM-UHFFFAOYSA-N

Beschreibung

Biochem/physiol Actions

Brain-penetrant, selective and highly potent diacylglycerol lipase (DAGLα/β, DAGLalpha & DAGLbeta) inhibitor in vitro and in vivo.

DO34 is a brain-penetrant, selective and highly potent diacylglycerol lipase inhibitor (recom human DAGLα/β pIC₅₀ = 8.2/8.1 by SAG hydrolysis; mouse brain DAGLα/β pIC₅₀ = 9.1-9.3/8.6 by ABPP ReDiMe) with detectable off-target activity toward only ABHD6 & PLA2G7 among all mouse brain serine hydrolases and little affinity toward cannabinoid receptors CB1/2. DO34 blocks depolarization-induced suppression of excitation (DSE IC₅₀ = 0.18 μM) and inhibition (100% DSI blockage at 1 μM) in mouse cerebellar and hippocampal slices ex vivo, and attenuate LPS-induced neuroinflammatory responses by lowering brain 2-AG & PGE2 level in mice in vivo (50 mg/kg, i.p).

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable