(±)-CPSI 1306
(Synonyms: 2-(3-(2,4-二氟苯基)-4,5-二氢异恶唑-5-基)-1-吗啉乙酮) 目录号 : GC16005
A MIF inhibitor
Cas No.:1309793-47-2
Sample solution is provided at 25 µL, 10mM.
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(±) -CPSI 1306 is an inhibitor of macrophage inhibitory factor (MIF) [1].
MIF is a proinflammatory cytokine and is an important regulation element of innate immunity. MIF plays an important role in the pathogenesis of many autoimmune inflammatory diseases [1].
In Skh-1 hairless mice with UVB exposure, CPSI 1306 reduced myeloperoxidase (MPO) activity and skin thickness and increased p53 expression and keratinocyte apoptosis. In mice with squamous carcinogenesis, CPSI-1306 slowed tumor growth and reduced p53 foci in non-tumor skin [1]. In ICR mice with streptozotocin (STZ) -induced non-insulin-dependent diabetes mellitus (NIDDM), CPSI 1306 significantly decreased blood glucose levels and reduced the levels of IL-6 and TNF-ɑ, the proinflammatory cytokines. These results suggested that MIF was involved in the pathogenesis of NIDDM [2]. In wild-type C57Bl/6 mice immunized with myelin oligodendrocyte glycoprotein (MOG35–55), which induced experimental autoimmune encephalomyelitis (EAE), CPSI-1306 (1 mg/kg) reduced the inflammation and reduced the severity of disease [3].
References:
[1]. Nagarajan P, Tober KL, Riggenbach JA, et al. MIF antagonist (CPSI-1306) protects against UVB-induced squamous cell carcinoma. Mol Cancer Res, 2014, 12(9): 1292-1302.
[2]. Sanchez-Zamora Y, Terrazas LI, Vilches-Flores A, et al. Macrophage migration inhibitory factor is a therapeutic target in treatment of non-insulin-dependent diabetes mellitus. FASEB J, 2010, 24(7): 2583-2590.
[3]. Kithcart AP, Cox GM, Sielecki T, et al. A small-molecule inhibitor of macrophage migration inhibitory factor for the treatment of inflammatory disease. FASEB J, 2010, 24(11): 4459-4466.
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Animal experiment: |
Mice[1]Six- to 8-wk-old female BALB/c mice and ICR mice are used in the study. Age- and sex-matched ICR mice are deprived of food for 20 h and then injected intraperitoneally with STZ (90 mg/kg). Beginning at 6 h after STZ injection, mice are administered CPSI-1306 (1 or 0.1 mg/kg) or PBS daily in a single oral dose for 30 d[1]. |
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References: [1]. Sanchez-Zamora Y, et al. Macrophage migration inhibitory factor is a therapeutic target in treatment of non-insulin-dependent diabetes mellitus. FASEB J. 2010 Jul;24(7):2583-90. |
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| Cas No. | 1309793-47-2 | SDF | |
| 别名 | 2-(3-(2,4-二氟苯基)-4,5-二氢异恶唑-5-基)-1-吗啉乙酮 | ||
| 化学名 | (S)-2-(3-(2,4-difluorophenyl)-4,5-dihydroisoxazol-5-yl)-1-morpholinoethanone | ||
| Canonical SMILES | FC1=CC(F)=CC=C1C2=NO[C@@H](C2)CC(N3CCOCC3)=O | ||
| 分子式 | C15H16F2N2O3 | 分子量 | 310.3 |
| 溶解度 | <31.03mg/ml 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 | 3.2227 mL | 16.1134 mL | 32.2269 mL |
| 5 mM | 0.6445 mL | 3.2227 mL | 6.4454 mL |
| 10 mM | 0.3223 mL | 1.6113 mL | 3.2227 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。
Quality Control & SDS
- View current batch:
- Purity: >97.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet