Share to
Overview
Specs
Technical Documents
Related
Articles
reviews
Consult
returns
Product introduction
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. Form:Solid IC50& Target:PI3Kδ 14 nM (IC 50 ) CYP2C9 2.7 μM (IC 50 )
Chinese name
IHMT-PI3Kδ-372
English name
IHMT-PI3Kδ-372
Chinese alias
-
English alias
-
CAS number
2429889-62-1
molecular formula
C26H23F2N7O2
molecular weight
503.50 g/mol
Exact mass
≥99%
PSA
-
Logp
-
Technical Documents
「No technical documents」
Related
「No upstream and downstream information yet」
Articles
「No related articles yet」
user reviews
Loading...
Consultation

Warm reminder:

Because the manufacturer may temporarily adjust product specifications, prices, inventory, parameters and other information without notice, and there are differences in each user's consultation time and procurement needs, the platform reply content is only of reference value within a certain period. Sorry for the inconvenience caused to you, and thank you for your understanding and support! Please consult the online customer service for the latest details. Everything is subject to the real-time reply of the customer service.!

After Sales Services

Please check the quantity, appearance and product information in time when you receive the goods. In case of damage, wrong delivery, abnormal quality and other problems, please feel free to contact us.

Service Hotline:400-6226-992 ,We will handle it for you as soon as possible, thank you for your support and trust.!

IHMT-PI3Kδ-372 1ml

IHMT-PI3Kδ-372 1ml; supplied for laboratory research, analysis, inspection, and scientific procurement use; specifications: 1ml.

item number:I654815-1ml
Product model:1ml
level: 1ml
Lead Time:30days
sold 130 Items
Ask Solution engineer
Specifications:

1ml

Qty

Recommended for you