LEO 39652 - 10mM in DMSO , CAS No.1445656-91-6

CAS: 1445656-91-6 Cat. No.: L654506 Fórmula: C₂₃H₂₃N₃O₅ Peso molecular: 421.45 PubChem CID: 71611998

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

LEO 39652 is a dual-soft PDE4 inhibitor with IC 50 s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A , PDE4B , PDE4C and PDE4D , respectively. LEO 39652 also inhibits TNF-α with an IC 50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD)

In Vitro

LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin .\nPharmacokinetic Analysis LEO 39652 exhibits total clearance (rats 930, minipigs 200 and monkey 300 mL/min/kg) and ratio to total AUC (rats 4, minipigs 6 and monkey 6 %) following intravenous administration (rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg) . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 3 male Sprague Dawley rats, 2 female Göttingen minipigs, 2 male Göttingen minipigs, 2 female cynomolgus monkeys and 2 male cynomolgus monkeys Dosage: Rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg Administration: Intravenous injection Result: Total clearance of 930, 200 and 300 mL/min/kg for rats, minipigs and monkeys, respectively.

IC50& Target:PDE4D 3.8 nM (IC 50 ) TNF-α 6.0 nM (IC 50 ) PDE4A 1.2 nM (IC 50 ) PDE4B 1.2 nM (IC 50 ) PDE4C2 3.0 nM (IC 50 )

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

LEO 39652 is a dual-soft PDE4 inhibitor with IC 50 s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A , PDE4B , PDE4C and PDE4D , respectively. LEO 39652 also inhibits TNF-α with an IC 50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic der

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

INHIBITOR

Nombres e identificadores

• Isómeros SMILES: CC(C)COC(=O)C1(CC1)C2=NN3C(=CC=C(C3=N2)OC)C4=CC5=C(C=C4)C(=O)OC5
• PubChem CID: 71611998
• Peso molecular: 421.45

Objetivos asociados (humanos)

PDE4D Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4D (2 Activities)

Discover Target: PDE4D

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

PDE4C Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4C (1 Activities)

Discover Target: PDE4C

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

PDE4A Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4A (1 Activities)

Discover Target: PDE4A

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

PDE4B Tclin cAMP-specific 3',5'-cyclic phosphodiesterase 4B (1 Activities)

Discover Target: PDE4B

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

Preguntas frecuentes

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 1445656-91-6, the molecular formula is C23H23N3O5, and the molecular weight is 421.45 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.