IHMT-PI3Kδ-372 S-isomer NEW
Price | $117 | $175 | $268 |
Package | 1mg | 2mg | 5mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-11 |
Product Details
Product Name: IHMT-PI3Kδ-372 S-isomer | CAS No.: 2429889-61-0 |
Purity: 99.68% | Supply Ability: 10g |
Release date: 2024/11/11 |
Product Introduction
Bioactivity
名稱 | IHMT-PI3Kδ-372 S-isomer |
描述 | 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. |
體外活性 | 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]. |
體內(nèi)活性 | 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]. |
存儲條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 50 mg/mL (99.3 mM) |
關(guān)鍵字 | IHMTPI3Kδ372Sisomer | IHMT-PI3Kδ-372 S-isomer | IHMT-PI3Kdelta-372 S-isomer |
相關(guān)產(chǎn)品 | Myricetin | Erucic acid | Sapanisertib | (2S,3R,4S)-4-Hydroxyisoleucine | 3-Methyladenine | Duvelisib (R enantiomer) hydrochloride | Isoprenaline hydrochloride | Quercetin | Quercetin Dihydrate | Apilimod | LY294002 | Idelalisib |
相關(guān)庫 | PI3K/Akt/mTOR 化合物庫 | 抗結(jié)直腸癌化合物庫 | 經(jīng)典已知活性庫 | 激酶抑制劑庫 | 抗卵巢癌化合物庫 | 抗癌細(xì)胞代謝庫 | 抑制劑庫 | 代謝化合物庫 | 抗衰老化合物庫 | 已知活性化合物庫 | 含氟化合物庫 | 抗肝癌化合物庫 |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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