Senicapoc NEW
| Price | $32 | $52 | $79 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-15 |
Product Details
| Product Name: Senicapoc | CAS No.: 289656-45-7 |
| Purity: 99.5% | Supply Ability: 10g |
| Release date: 2024/11/15 |
Product Introduction
Bioactivity
| 名稱 | Senicapoc |
| 描述 | Senicapoc (ICA-17043) is a potent inhibitor of the Gardos channel that ameliorates RBC dehydration in the SAD mouse. It blocks Ca2+-induced rubidium flux from human RBCs with an IC50 value of 11 ± 2 nM (CLT IC50 = 100 ± 12 nM) and inhibits RBC dehydration with an IC50 of 30 ± 20 nM. Senicapoc is used in the treatment of Sickle Cell Disease and Sickle Cell Anemia. |
| 細(xì)胞實(shí)驗(yàn) | Senicapoc is dissolved in DMSO or 100% ethanol. The whole blood is initially diluted 1:1 with Modified Flux Buffer (MFB), consisting of 140 mM NaCl, 5 mM KCl, 10 mM Tris (tris(hydroxymethyl)aminomethane), 0.1 mM EGTA (ethyleneglycoltetraacetic acid) (pH=7.4). The blood is centrifuged at 1000 rpm, and the pellet comprised primarily of RBCs is washed 3 times with MFB. The cells are then loaded with?86Rb+?by incubating the washed cells with 86Rb+?at a final concentration of 0.185 MBq/mL (5 μCi/mL) in MFB for at least 3 hours at 37°C. After loading with 86Rb+, the RBCs are washed 3 times with chilled MFB. The cells are then incubated for 10 minutes with test compound (senicapoc) at concentrations that ranged from 1 nM to 10?000 nM. Efflux of?86Rb+?is initiated by raising intracellular calcium levels in the RBCs with the addition of CaCl2?and A23187 (a calcium ionophore) to final concentrations of 2 mM and 5 μM, respectively. After 10 minutes of incubation at room temperature, the RBCs are pelleted in a microcentrifuge, and the supernatant is removed and counted in a Wallac MicroBeta liquid scintillation counter. |
| 體外活性 | ICA-17043 is shown to block the Gardos channel of mouse (C57 Black) RBCs with an IC50 of 50±6 nM. ICA-17043 blocks this increase in cellular hemoglobin concentration in human RBCs in a concentration-dependent fashion[1]. |
| 體內(nèi)活性 | ICA-17043?(10 mg/kg, p.o.) administration produces a significant decrease in Gardos channel activity measured at day 11 and 21 and is associated with a corresponding increase in red cell K+ content without changes in Na+ content. ICA-17043 (10 mg/kg, twice a day) induces a significant increase in Hct after 11 days of dosing in the SAD mouse[1]. Senicapoc (30 mg/kg, p.o.) reduces airway hyperresponsiveness, eosinophil numbers in bronchoalveolar lavage taken 48 hours post-allergen challenge, and vascular remodelling in the sheep[2]. |
| 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 : 50 mg/mL (154.64 mM), Sonication is recommended. |
| 關(guān)鍵字 | KcsA | Senicapoc | inhibit | ICA 17043 | Potassium Channel | ICA17043 | Inhibitor |
| 相關(guān)產(chǎn)品 | Minoxidil sulfate | Glibenclamide | (±)-Naringenin | Tolbutamide | Tetraethylammonium bromide | Halothane | Butamben | Cloperastine hydrochloride | 2,2,2-Trichloroethanol | Indapamide |
| 相關(guān)庫 | 經(jīng)典已知活性庫 | 疼痛相關(guān)化合物庫 | 膜蛋白靶向化合物庫 | 抗癌臨床化合物庫 | 藥物功能重定位化合物庫 | 抑制劑庫 | 已知活性化合物庫 | 鉀通道分子庫 | 離子通道庫 | 抗癌藥物庫 |
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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