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

CAS: 2429889-62-1 Cat. No.: I654815 Molecular Weight: 503.50

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

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 )

Specifications

Specifications & Purity

10mM in DMSO

Biochemical and Physiological Mechanisms

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

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Action Type

INHIBITOR

Names and Identifiers

• Molecular Weight: 503.50