IHMT-PI3Kδ-372 - 10mM in DMSO , CAS No.2429889-62-1

CAS: 2429889-62-1 Cat. No.: I654815 Fórmula: C₂₆H₂₃F₂N₇O₂ Peso molecular: 503.50

GRAU & PUREZA 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Visão geral

IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC 50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research

In Vitro

IHMT-PI3Kδ-372 (Compound (S)-18; 0.03-3 μM; 1 hour; Raji cells) treatment inhibits PI3Kδ-mediated AKT T308 phosphorylation in Raji cells with an EC 50 value of 67 nM. IHMT-PI3Kδ-372 (compound (S)-18) shows moderate inhibition of CYP2C9 (IC 50 of 2.7 μM) and no apparent inhibition against CYP1A2, CYP2B6, CYP2C19, and CYP3A4 (IC 50 s > 10 μM). MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: Raji cells Concentration: 0.03 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM Incubation Time: 1 hour Result: Inhibited PI3Kδ-mediated AKT T308 phosphorylation in Raji cells with an EC 50 value of 67 nM.

In Vivo

IHMT-PI3Kδ-372 (Compound (S)-18; 1-5 mg/kg; inhalation; daily; for 28 days) improves lung function and reduced the inflammatory patterns characteristic of COPD. The lung function parameters such as forced expiratory volume in the first second (FEV1), forced vital capacity (FVC), and peak expiratory flow (PEF) are improved dose-dependently. The abnormally high level of leukocytes including the alveolar macrophages, neutrophils, and lymphocytes are also reduced. IHMT-PI3Kδ-372 decreases the inflammatory cell infiltration in a dose-dependent manner . In rats, inhalation of 5 mg/kg dose of IHMT-PI3Kδ-372 (compound (S)-18) displays a half-life of 2.3 h, low exposure of 66 ng/mL, and high clearance of 348.5 mL/min/kg in plasma but high exposure of 5599 ng/g (6 h after inhalation) in lung tissue . IHMT-PI3Kδ-372 is stable in human, rat, and mouse liver microsomes, while it has moderate stability in monkey and dog liver microsomes . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Sprague-Dawley (SD) rats (5-week-old) induced with cigarette-smoke and LPS Dosage: 1 mg/kg, 3 mg/kg, and 5 mg/kg Administration: Inhalation; daily; for 28 days Result: Improved lung function and reduced the inflammatory patterns characteristic of COPD.

IC50& Target:PI3Kδ 14 nM (IC 50 ) CYP2C9 2.7 μM (IC 50 )

Especificações

Especificações e pureza

10mM in DMSO

Mecanismos bioquímicos e fisiológicos

IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC 50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (C

Condições de armazenamento de armazenamento

Store at -80°C

Enviado em

Dry ice packs + Cold packs

Este produto requer transporte de cadeia fria. Serviços terrestres e outros serviços econômicos não estão disponíveis.

Tipo de ação

INHIBITOR

Nomes e identificadores

Peso molecular

503.50

Perguntas frequentes

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 2429889-62-1, the molecular formula is C26H23F2N7O2, and the molecular weight is 503.50 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.