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IHMT-PI3Kδ-372 S-isomer

🥰Excellent
Catalog No. T60196Cas No. 2429889-61-0

IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer 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.

IHMT-PI3Kδ-372 S-isomer

IHMT-PI3Kδ-372 S-isomer

🥰Excellent
Purity: 99.68%
Catalog No. T60196Cas No. 2429889-61-0
IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer 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.
Pack SizePriceAvailabilityQuantity
1 mg$117In Stock
2 mg$175In Stock
5 mg$268In Stock
10 mg$394In Stock
25 mg$592In Stock
50 mg$828In Stock
100 mg$1,130In Stock
1 mL x 10 mM (in DMSO)$327In Stock
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Purity:99.68%
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Product Introduction

Bioactivity
Description
IHMT-PI3Kδ-372 S-isomer is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 S-isomer 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 (S)-18 (0.03-3 μM; 1 hour; Raji cells) treatment inhibits PI3Kδ-mediated AKT T308 phosphorylation in Raji cells with an EC50 value of 67 nM. IHMT-PI3Kδ-372 (S)-18 shows moderate inhibition of CYP2C9 (IC50 of 2.7 μM) and no apparent inhibition against CYP1A2, CYP2B6, CYP2C19, and CYP3A4 (IC50s > 10 μM)[1].
In vivo
IHMT-PI3Kδ-372 (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 (S)-18 decreases the inflammatory cell infiltration in a dose-dependent manner. In rats, inhalation of 5 mg/kg dose of IHMT-PI3Kδ-372 (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 (S)-18 is stable in human, rat, and mouse liver microsomes, while it has moderate stability in monkey and dog liver microsomes[1].
Chemical Properties
Molecular Weight503.5
FormulaC26H23F2N7O2
Cas No.2429889-61-0
Smiles[C@@H](CC)(N1C=2C(C(=N1)C3=CC(F)=C(OC)C=C3)=C(N)N=CN2)C=4N(C(=O)C=5C(N4)=CC=CC5F)C6CC6
Relative Density.1.55 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (99.3 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9861 mL9.9305 mL19.8610 mL99.3049 mL
5 mM0.3972 mL1.9861 mL3.9722 mL19.8610 mL
10 mM0.1986 mL0.9930 mL1.9861 mL9.9305 mL
20 mM0.0993 mL0.4965 mL0.9930 mL4.9652 mL
50 mM0.0397 mL0.1986 mL0.3972 mL1.9861 mL

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