5.08957

PDE5 Inhibitor, Cpd7a

• 동의어(들): PDE5 Inhibitor, Cpd7a
• 실험식(Hill 표기법): C₂₂H₂₀ClN₃O₂
• CAS Number: 1233518-60-9
• Molecular Weight: 393.87
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• Quality Level: 100
• 형태: solid
• 효능: 270 pM IC₅₀
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: cream
• solubility: DMSO: 100 mg/mL
• 저장 온도: 2-8°C

설명

일반 설명

A cell-permeable, brain permeant, quinoline-based compound that acts as a highly potent and selective inhibitor of phosphodiesterase 5 (PDEV; IC₅₀ = 270 pM). Exhibits over 10,000 fold greater selectivity over various other phosphodiestrases and trivial activity against PDE VI (IC₅₀ = 339 nM). Shown to increase cGMP levels in mouse hippocampus and attenuates long term potentiation and memory defects in mice with elevated levels of oligomeric Aβ42. It is rapidly absorbed with peak plasma concentration observed at 30 min. Displays desirable pharmacokinetic properties with plasma t1/2 = 1.33 h and brain t1/2 = 1.04 h.

A cell-permeable, brain permeant, quinoline-based compound that acts as a highly potent and selective inhibitor of phosphodiesterase 5 (PDEV; IC₅₀ = 270 pM). Exhibits over 10,000 fold greater selectivity over various other phosphodiestrases and trivial activity against PDE VI (IC₅₀ = 339 nM). Shown to increase cGMP levels in mouse hippocampus and attenuates long term potentiation and memory defects in mice with elevated levels of oligomeric Aβ42. It is rapidly absorbed with peak plasma concentration observed at 30 min. Displays desirable pharmacokinetic properties with plasma t1/2 = 1.33 h and brain t1/2 = 1.04 h.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

생화학적/생리학적 작용

Primary Target
PDE5

Reversible: yes

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

재구성

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

기타 정보

Fiorito, J., et al. 2013. Eur. J. Med. Chem.60, 285.

법적 정보

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable