SRI-37330
目录号 : GC68451SRI-37330 是一种具有口服活性的 TXNIP 抑制剂。SRI-37330 降低胰高血糖素的分泌和作用，并阻断肝脏葡萄糖输出。SRI-37330 可用于肥胖和糖尿病的研究。
Cas No.:2322245-42-9
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
SRI-37330 is an orally active TXNIP inhibitor. SRI-37330 decreases glucagon secretion and action and blocks hepatic glucose output. SRI-37330 can be used in the research of obesity and diabetes[1].
SRI-37330 (1 μM, 24 h) inhibits the activity of the human TXNIP promoter in INS-1 cells[1].
SRI-37330 (1 μM, 24 h) inhibits Mrna and protein levels of TXNIP in INS-1 cells[1].
SRI-37330 (5 μM, 24 h) inhibits polymerase II (Pol II) binding to the E-box motif region of the TXNIP promoter[1].
SRI-37330 (5 μM, 24 h) lowers glucagon secretion in TC1-6 cells[1].
SRI-37330 (0-5 μM, 24 h) inhibits glucagon-induced glucose output from primary hepatocytes[1].
RT-PCR[1]
| Cell Line: | INS-1 cells |
| Concentration: | 1 μM |
| Incubation Time: | 24 h |
| Result: | Inhibited endogenous TXNIP mRNA expression with an IC50 of 0.64 μM. |
SRI-37330 (100 mg/kg, p.o., in drinking water, 3 weeks) decreases glucagon secretion and action and blocks hepatic glucose output[1].
SRI-37330 (100 mg/kg, p.o., in drinking water, 3 weeks) is well tolerated in male C57BL/6J mice[1].
SRI-37330 (100 mg/kg, p.o., in drinking water, 3 weeks) reverses obesity- and STZ-induced diabetes and hepatic steatosis in mice[1].
| Animal Model: | C57BL/6J mice[1] |
| Dosage: | 100 mg/kg |
| Administration: | Oral administration (p.o.), in drinking water, 3 weeks. |
| Result: | Lowered serum glucagon levels, inhibited hepatic glucose production and improved glucose homeostasis in mice. |
[1]. Thielen LA, et al. Identification of an Anti-diabetic, Orally Available Small Molecule that Regulates TXNIP Expression and Glucagon Action. Cell Metab. 2020 Sep 1;32(3):353-365.e8.
| Cas No. | 2322245-42-9 | SDF | Download SDF |
| 分子式 | C16H19F3N4O2S | 分子量 | 388.41 |
| 溶解度 | DMSO : 100 mg/mL (257.46 mM; Need ultrasonic) | 储存条件 | Store at -20°C, stored under nitrogen |
| 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 | 2.5746 mL | 12.873 mL | 25.746 mL |
| 5 mM | 0.5149 mL | 2.5746 mL | 5.1492 mL |
| 10 mM | 0.2575 mL | 1.2873 mL | 2.5746 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。
Identification of an Anti-diabetic, Orally Available Small Molecule that Regulates TXNIP Expression and Glucagon Action
Cell Metab 2020 Sep 1;32(3):353-365.e8.PMID:32726606DOI:PMC7501995
Diabetes is characterized by hyperglycemia, loss of functional islet beta cell mass, deficiency of glucose-lowering insulin, and persistent alpha cell secretion of gluconeogenic glucagon. Still, no therapies that target these underlying processes are available. We therefore performed high-throughput screening of 300,000 compounds and extensive medicinal chemistry optimization and here report the discovery of SRI-37330, an orally bioavailable, non-toxic small molecule, which effectively rescued mice from streptozotocin- and obesity-induced (db/db) diabetes. Interestingly, in rat cells and in mouse and human islets, SRI-37330 inhibited expression and signaling of thioredoxin-interacting protein, which we have previously found to be elevated in diabetes and to have detrimental effects on islet function. In addition, SRI-37330 treatment inhibited glucagon secretion and function, reduced hepatic glucose production, and reversed hepatic steatosis. Thus, these studies describe a newly designed chemical compound that, compared to currently available therapies, may provide a distinct and effective approach to treating diabetes.