PF-05085727 - 10mM in DMSO , CAS No.1415637-72-7

CAS: 1415637-72-7 Cat. No.: P656359 분자식: C₂₀H₁₈F₃N₇ 분자량: 413.4 PubChem CID: 71488864

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

개요

PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A ( IC 50 =2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11

In Vitro

PF-05085727 shows weak activity with IC 50 of 162 μM to induce cell death in a cellular toxicity assay using transformed human liver endothelial (THLE) cells. PF-05085727 (3 μM) shows a minimal inhibition of cytochrome P450 enzymes (CYPs), inhibits 1A2, 2C8, 2C9, 2D6 and 3A4 with percentage% of 16%, 18%, 7%, 4%, and 30%, respectively. PF-05085727 (10 μM) inhibits PDE1B, PDE4B, PDE7B and PDE10A with IC 50 values of 12.146 μM, 22,503 μM, 13.157 μM and 6.515 μM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PF-05085727 (subcutaneous injection; 3.2 mg/kg/mice; 3 mg/kg/rat) gives a ratio of unbound brain (C bu ) to unbound plasma (C pu ) of ca. 0.27 and 0.37, respectively . PF-05085727 in mice leads to an acute and exposure-dependent elevation in the accumulation of bulk levels of cGMP in cortex, striatum, and hippocampus as measured by enzyme-linked immunosorbent assay . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:PDE2A 2 nM (IC 50 )

Specifications

사양 및 순도

10mM in DMSO

생화학 및 생리적 메커니즘

PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A ( IC 50 =2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11.

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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작업 유형

INHIBITOR

이름과 식별자

• 이성체 SMILES: CN1C(=C(C=N1)C2=NN(C3=C2C(=NC=N3)N4CCC4)C)C5=CC=C(C=C5)C(F)(F)F
• PubChem CID: 71488864
• 분자량: 413.4

관련 대상(인간)

PDE2A Tclin cGMP-dependent 3',5'-cyclic phosphodiesterase (6 Activities)

Discover Target: PDE2A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

자주 묻는 질문

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 1415637-72-7, the molecular formula is C20H18F3N7, and the molecular weight is 413.4 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.