JAK3-IN-6 NEW
Price | $34 | $55 | $86 |
Package | 2mg | 5mg | 10mg |
Min. Order: | |
Supply Ability: | 10g |
Update Time: | 2024-11-07 |
Product Details
Product Name: JAK3-IN-6 | CAS No.: 1443235-95-7 |
Purity: 99.94% | Supply Ability: 10g |
Release date: 2024/11/07 |
Product Introduction
Bioactivity
名稱 | JAK3-IN-6 |
描述 | JAK3-IN-6 is irreversible Janus Associated Kinase 3 (JAK3) inhibitor, with an IC50 of 0.15 nM |
動(dòng)物實(shí)驗(yàn) | Female Lewis rats were purchased and housed . 48 rats were divided into six groups (n=8/group). Group 1 were drug-na?ve i.e. no compounds were administered throughout the study. On the afternoon of Day 1 (4pm), ABT or vehicle (1 ml/kg p.o.) was administered to Groups 2-5. Days 2-11 (8 am), each animal in Groups 2-5 were administered ABT 10 mpk qd (1 ml/kg p.o.), immediately followed by either vehicle or compound at 5ml/kg p.o. Group 6 animals received vehicle only (5 ml/kg p.o.). Days 2-11 (4 pm) Groups 2-5 were administered vehicle or compound at 5 ml/kg p.o. Animals were monitored and weighed throughout the study. On Day 10, under isoflurane anesthesia, 3 animals from Groups 2-6 were bled via the jugular vein for PK analysis at 4 and 8 h post-8 am dose. On Day 11, blood samples were collected, as described above, at 0 (16 h post-Day 10 pm dose) and 2 h post-am dose for PK, hematology, and clinical chemistry analysis. All remaining animals were euthanized at 2 hrs post-dosing on Day 11 and blood samples were collected for PK, hematology, and clinical chemistry analysis. Data were analyzed using Graphpad prism software. Statistical analyses were performed using a one-way ANOVA with Dunnett s post-hoc test for group comparisons to ABT + vehicle treatment. |
體外活性 | a potent inhibitor of JAK3 (0.15 nM) was 4300-fold selective for JAK3 over JAK1 in enzyme assays, 67-fold (IL-2 vs. IL-6) or 140-fold (IL-2 vs. EPO or GMCSF) selective in cellular reporter assays and >35-fold selective in human PBMC assays (IL-7 vs. IL-6 or GMCSF). In vivo, selective JAK3 inhibition was sufficient to block the development of inflammation in a rat model of Rheumatoid Arthritis, while sparing hematopoiesis. |
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 : 40 mg/mL (114.17 mM), Sonication is recommended. |
關(guān)鍵字 | inhibit | JAK3 IN 6 | JAK | Inhibitor | JAK3IN6 | JAK3-IN-6 | JAK-3-IN-6 | Janus kinase |
相關(guān)產(chǎn)品 | Delgocitinib | Deucravacitinib | Fedratinib | RO8191 | Ruxolitinib | Tofacitinib Citrate | CEP-33779 | Ruxolitinib phosphate | JAK-IN-10 | Baricitinib | Tofacitinib | Ritlecitinib |
相關(guān)庫(kù) | 高選擇性抑制劑庫(kù) | 半胱氨酸共價(jià)化合物庫(kù) | 經(jīng)典已知活性庫(kù) | 激酶抑制劑庫(kù) | JAK-STAT 化合物庫(kù) | 抑制劑庫(kù) | 抗衰老化合物庫(kù) | 已知活性化合物庫(kù) | 共價(jià)抑制劑庫(kù) | 抗癌化合物庫(kù) |
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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