價(jià)格 | ¥689 | ¥1630 | ¥2890 |
包裝 | 1mg | 5mg | 10mg |
最小起訂量 | 1mg |
發(fā)貨地 | 上海 |
更新日期 | 2024-12-12 |
中文名稱:化合物 AZD7986 | 英文名稱:Brensocatib |
CAS:1802148-05-5 | 品牌: TargetMol |
產(chǎn)地: 美國(guó) | 保存條件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
純度規(guī)格: 99.05% | 產(chǎn)品類別: 抑制劑 |
貨號(hào): TQ0038 |
名稱 | Brensocatib |
描述 | Brensocatib (AZD7986) is a Dipeptidyl peptidase 1 (DPP1) inhibitor (pIC50s: 6.85, 7.7, 7.6, 7.8, and 7.8 in human, rat, mouse, rabbit, and dog, respectively). |
細(xì)胞實(shí)驗(yàn) | Cellular potency is studied using the DPP1-expressing monocytic U937 cell line. Briefly, cells grown in RPMI are plated on 384-well polypropylene v-bottom plates at a density of 5×10^5 cells/mL per well. Added to this is 10 μL of AZD7986 at 37°C for 60 min, followed by 350 μM Gly-Phe-AFC. The well fluorescence is read using a multilabel plate reader. Data are analyzed to calculate pIC50 values. |
激酶實(shí)驗(yàn) | Activation of neutrophil serine proteases is assessed in vitro using primary bone marrow-derived CD34+ neutrophil progenitor cells. Cells are cultured in media supplemented with rhSCF and rhIL-3 for 7 days, and then for a further 7 days in the presence of G-CSF and different concentrations of AZD7986 (38 pM to 10 μM). After harvesting and lysis with 10% Triton X-100 buffer, cell lysates are kept at -20°C until NSP activity analysis. |
動(dòng)物實(shí)驗(yàn) | Rats are used for the in vivo study. Naive rats are dosed orally twice daily with AZD7986 at 0.2, 2, and 20 mg/kg/day for 8 days. At termination, bone marrow is taken by femural aspiration for neutrophil serine proteases activity analysis using commercial synthetic peptide substrates. |
體外活性 | AZD7986在丙醛活性測(cè)定中表現(xiàn)穩(wěn)定,半衰期超過(guò)50小時(shí)。經(jīng)AZD7986(38 pM至10 μM)處理后,觀察到DPP1及所有三種NSPs(NE、Pr3、CatG)的細(xì)胞裂解物酶活性呈濃度依賴性下降。AZD7986以濃度依賴性方式抑制所有三種NSPs的激活,三者的pIC50值均約為7。這種活性降低幾乎是完全的,NE、Pr3和CatG的活性在10 μM AZD7986下降至對(duì)照的4至10%。 |
體內(nèi)活性 | AZD7986在血漿中顯示出良好的穩(wěn)定性,半衰期超過(guò)10小時(shí)。在體內(nèi),AZD7986以劑量依賴的方式抑制了骨髓細(xì)胞裂解物中的Pr3和NE的激活,但不抑制CatG的激活。 |
存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : ≥100 mg/mL (237.83 mM) H2O : Insoluble |
關(guān)鍵字 | Dipeptidyl Peptidase | AZD 7986 | AZD-7986 | INS1007 | DPP | inhibit | INS-1007 | Brensocatib | Inhibitor |
相關(guān)產(chǎn)品 | Teneligliptin hydrobromide | Bortezomib | Sitagliptin | Anagliptin | TCH-165 | Alloxan monohydrate | Saxagliptin hydrate | Sitagliptin phosphate monohydrate | 4'-Hydroxychalcone | Vildagliptin | Linagliptin | Aprotinin |
相關(guān)庫(kù) | 抑制劑庫(kù) | 經(jīng)典已知活性庫(kù) | 已知活性化合物庫(kù) | HIF-1化合物庫(kù) | NO PAINS 化合物庫(kù) | 泛素化化合物庫(kù) | 臨床期小分子藥物庫(kù) | 口服活性化合物庫(kù) | 藥物功能重定位化合物庫(kù) |
成立日期 | 2013-04-18 (12年) | 注冊(cè)資本 | 566.265100萬(wàn)人民幣 |
員工人數(shù) | 100-500人 | 年?duì)I業(yè)額 | ¥ 1億以上 |
主營(yíng)行業(yè) | 天然產(chǎn)物,生化試劑,分子生物學(xué),分子砌塊,生物技術(shù)服務(wù) | 經(jīng)營(yíng)模式 | 貿(mào)易,工廠,試劑,定制,服務(wù) |
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