DS28120313
目录号 : GC35902
DS28120313 是一种口服型铁调素 (hepcidin) 生成抑制剂, IC50值为 0.093 μM。
Cas No.:2146177-09-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
DS28120313 (compound 32) is an orally hepcidin production inhibitor with an IC50 of 0.093 μM[1]. IC50: 0.093 μM (hepcidin production)[1]
DS28120313 (deliver orally; 30 mg/kg; 30 min before IL-6 administration) inhibits hepcidin production and reduces the blood hepcidin level in IL-6 induced acute inflammatory C57BL/6 mouse model[1].
[1]. Fukuda T, et al. Discovery of DS28120313 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4,6-disubstituted indazole derivatives. Bioorg Med Chem Lett. 2017 Dec 1;27(23):5252-5257.
| Cas No. | 2146177-09-3 | SDF | |
| Canonical SMILES | CC(NN=C1C2CC2)=C1C3=CC(NC(OC)=O)=C(C=NN4)C4=C3 | ||
| 分子式 | C16H17N5O2 | 分子量 | 311.34 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.2119 mL | 16.0596 mL | 32.1192 mL |
| 5 mM | 0.6424 mL | 3.2119 mL | 6.4238 mL |
| 10 mM | 0.3212 mL | 1.606 mL | 3.2119 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Discovery of DS28120313 as a potent orally active hepcidin production inhibitor: Design and optimization of novel 4,6-disubstituted indazole derivatives
Bioorg Med Chem Lett 2017 Dec 1;27(23):5252-5257.PMID:29079471DOI:10.1016/j.bmcl.2017.10.031
Hepcidin has emerged as the central regulatory molecule in systemic iron homeostasis, and its inhibition could be a favorable strategy for treating anemia of chronic disease (ACD). Here, we report the design, synthesis and structure-activity relationships (SAR) of a series of 4,6-disubstituted indazole compounds as hepcidin production inhibitors. The optimization study of multi-kinase inhibitor 1 led to the design of a potent and bioavailable hepcidin production inhibitor, 32 (DS28120313), which showed serum hepcidin-lowering effects in an interleukin-6-induced acute inflammatory mouse model.