SML3379

D159687

≥98% (HPLC)

• Sinonimo/i: 1-(4-((3′-Chloro-6-methoxy-[1,1′-biphenyl]-3-yl)methyl)phenyl)urea, D 159687, N-[4-[(3′-Chloro-6-methoxy[1,1′-biphenyl]-3-yl)methyl]phenyl]urea, [4-(3′-Chloro-6-methoxy-biphenyl-3-ylmethyl)phenyl]urea, [4-[[3-(3-Chlorophenyl)-4-methoxyphenyl]methyl]phenyl]urea
• Formula empirica (notazione di Hill): C₂₁H₁₉ClN₂O₂
• Numero CAS: 1155877-97-6
• Peso molecolare: 366.84
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD26793458
• Assay: ≥98% (HPLC)
• Form: powder

Proprietà

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (Warmed)
• storage temp.: 2-8°C
• SMILES string: Clc1cc(ccc1)c2c(ccc(c2)Cc3ccc(cc3)NC(=O)N)OC
• InChI: 1S/C21H19ClN2O2/c1-26-20-10-7-15(12-19(20)16-3-2-4-17(22)13-16)11-14-5-8-18(9-6-14)24-21(23)25/h2-10,12-13H,11H2,1H3,(H3,23,24,25)
• InChI key: RJJLUTWHJUDZFP-UHFFFAOYSA-N

Descrizione

Biochem/physiol Actions

Brain-penetrant, orally available, potent and selective PDE4D negative allosteric modulator (NAM), more effective & much less emetic than Rolipram in vivo.

D159687 is a brain-penetrant, orally available, highly potent and selective negative allosteric modulator (NAM) against phosphodiesterase 4 (PDE4) subtype PDE4D (hPDE4D7 IC50 = 27 nM; PDE4A1/B1/C1 IC50 = 2.50/1.47/6.80 μM; IC50 ≥29 μM against PDE1/2/3/5/7/8/9/10/11 subtypes). Comparing to Rolipram, D159678 offers similar in vivo efficacy on long-term memory formation by novel object recognition test (MED = 3 μg/kg mouse iv., 1 μg/kg rat p.o.), while being more effective in the scopolamine-impaired Y-maze tests (D159678/Rolipram MED = 0.1/1 μg/kg mouse iv. or 30/100 μg/kg mouse p.o.) and much less emetic in shrews/dog/monkeys (by 100-/3000-/500-fold).

Informazioni sulla sicurezza

• Classe di stoccaggio: 11 - Combustible Solids
• Che succede?: WGK 3
• Punto di infiammabilità (°F): Not applicable
• Punto di infiammabilità (°C): Not applicable