SW033291
(Synonyms: 2-(丁基亚磺酰基)-4-苯基-6-(2-噻吩基)噻吩并[2,3-B]吡啶-3-胺) 目录号 : GC14441
SW033291是15-羟基前列腺素脱氢酶（15-PGDH）的小分子抑制剂，15-PGDH是一种催化PGE2氧化和失活的酶。
Cas No.:459147-39-8
Sample solution is provided at 25 µL, 10mM.
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SW033291 is a small molecule inhibitor of 15-hydroxyprostaglandin dehydrogenase (15-PGDH), an enzyme that catalyzes the oxidation and inactivation of PGE2 [1]. SW033291 was to promote tissue regeneration and prevent kidney and liver injury by upregulating PGE2 levels [2-3]. SW033291 is commonly used to promote tissue regeneration and repair [4].
In Muscle-derived stem cells (MDSCs), SW033291 (20, 50, 100, 500, 1000nM; 24h) increased the production of PGE2 by MDSCs both in GM and DM, and MDSCs were well-tolerated to SW033291 in various concentrations with strong proliferation potential [5]. In marrow mesenchymal stem cells (BMSCs), GelMA ICC combined with SW033291 (1μM; 5d) were able to regulate the M2 macrophage polarization in the co-culture with BMSCs system [6].
In mouse model of liver ischemia-reperfusion, SW033291 (5mg/kg; ip; 72h) increases PGE2 levels in liver tissue and improves liver injury after hepatic ischemia-reperfusion [3]. In T2DM mouse model, SW033291 (5mg/kg; ip; 10 weeks) improves abnormal glucose and lipid metabolism [7]. In T2DM mouse model, SW033291 (5mg/kg; ip; 10 weeks) improved impaired glucose tolerance and insulin resistance [8].
References:
[1]. Cheng H, Huang H, Guo Z, et al. Role of prostaglandin E2 in tissue repair and regeneration. Theranostics. 2021 Aug 13; 11(18): 8836.
[2]. Miao S, Lv C, Liu Y, et al. Pharmacologic blockade of 15-PGDH protects against acute renal injury induced by LPS in mice. Frontiers in physiology. 2020 Mar 13; 11: 138.
[3]. Xie M, He R, Wang H, et al. Effects of small molecule inhibitor SW033291 on hepatic ischemia-reperfusion injury in mice. Biochemical and biophysical research communications. 2022 Jul 30; 615: 70-74.
[4]. Zhang Y, Desai A, Yang SY, et al. Inhibition of the prostaglandin-degrading enzyme 15-PGDH potentiates tissue regeneration. Science. 2015 Jun 12; 348(6240): aaa2340.
[5]. Dong Y, Li Y, Zhang C, et al. Effects of SW033291 on the myogenesis of muscle-derived stem cells and muscle regeneration. Stem cell research & therapy. 2020 Dec; 11: 1-7.
[6]. Jiang Q, Bai G, Liu X, et al. 3D GelMA ICC scaffolds combined with SW033291 for bone regeneration by modulating macrophage polarization. Pharmaceutics. 2021 Nov 16; 13(11): 1934.
[7]. Liang M, Wang L, Wang W. The 15-hydroxyprostaglandin dehydrogenase inhibitor SW033291 ameliorates abnormal hepatic glucose metabolism through PGE2–EP4 receptor–AKT signaling in a type 2 diabetes mellitus mouse model. Cellular Signalling. 2023 Aug 1; 108: 110707.
[8]. Wang W, Liang M, Wang L, et al. 15-Hydroxyprostaglandin dehydrogenase inhibitor SW033291 ameliorates hepatic abnormal lipid metabolism, ER stress, and inflammation through PGE2/EP4 in T2DM mice. Bioorganic chemistry. 2023 Aug 1; 137: 106646.
SW033291是15-羟基前列腺素脱氢酶（15-PGDH）的小分子抑制剂，15-PGDH是一种催化PGE2氧化和失活的酶 [1]。SW033291通过上调PGE2水平来促进组织再生并预防肾脏和肝脏损伤 [2-3]。SW033291常用于促进组织再生和修复 [4]。
在肌肉来源的干细胞（MDSC）中，SW033291（20、50、100、500、1000nM；24h）可增加肌肉来源的干细胞的GM和DM中的PGE2生成，MDSC对不同浓度的SW033291均具有良好的耐受性，并具有强大的增殖潜力 [5]。在骨髓间充质干细胞（BMSCs）中，GelMA ICC与SW033291（1μM；5d）联合应用，能够在与BMSCs共培养的体系中调节M2巨噬细胞极化 [6]。
在小鼠肝脏缺血再灌注模型中，SW033291（5mg/kg；ip；72h）可提高肝组织中PGE2水平，改善肝脏缺血再灌注后的肝损伤 [3]。在2型糖尿病小鼠模型中，SW033291（5mg/kg；ip；10周）可改善异常的糖脂代谢 [7]。在2型糖尿病小鼠模型中，SW033291（5mg/kg；ip；10周）可改善糖耐量受损和胰岛素抵抗 [8]。
| Cell experiment [1]: | |
Cell lines | Muscle-derived stem cells (MDSCs) |
Preparation Method | Muscle tissue was obtained from the hind limbs of 8-week-old female Sprague Dawley (SD) rats. After mincing, the tissue was treated with 0.1% collagenase, dispase, and trypsin solutions and incubated at 37°C for 24h. Then, the dissociated cells were treated with the serial pre-seeding method as reported, using collagen-coated culture plates and cultured in a humidified atmosphere at 37°C and 5% CO2; MDSCs at passage 6 were used in the experiments. MDSC cells were incubated with SW033291 at concentrations ranging from 20 to 1000nM and then evaluated by senescence-associated β-galactosidase (SAβ-Gal) staining, LIVE/DEAD staining, and Alamar blue assay. |
Reaction Conditions | 20, 50, 100, 500, 1000nM; 24h |
Applications | SW033291 increased the production of PGE2 by MDSCs both in GM and DM with the best response reached approximately 2.8-folds increase, and MDSCs were well-tolerated to SW033291 in various concentrations with strong proliferation potential. |
| Animal experiment [2]: | |
Animal models | Type 2 diabetes mellitus (T2DM) mouse model |
Preparation Method | Seven-week-old male C57BL/6 J mice. After acclimation for 1 week, the mice were randomly divided into three groups, with no significant differences in the fasting blood glucose levels or body weights among the groups. Mice were housed in temperature-controlled (25 ± 2°C) conditions with a 12h dark/light cycle. Water and food were provided ad libitum. Mice in the control group were fed a normal diet. The T2DM mouse model was established using a high-fat diet (protein, 18.1%; fat, 61.6%; carbohydrates, 20.3%; HF60) combined with streptozotocin injections (30mg/kg body weight, dissolved in 0.1M citrate buffer, pH 4.2–4.5) on three consecutive days. SW033291 was dissolved in a vehicle containing 10% ethanol, 5% Cremophor EL, and 85% dextrose-5 water. Mice in the SW033291 group were intraperitoneally injected with SW033291 for 10 weeks. Control and T2DM mice were intraperitoneally injected with the vehicle solution. |
Dosage form | 5mg/kg; ip; 10 weeks |
Applications | SW033291 improves abnormal glucose and lipid metabolism. |
References: | |
| Cas No. | 459147-39-8 | SDF | |
| 别名 | 2-(丁基亚磺酰基)-4-苯基-6-(2-噻吩基)噻吩并[2,3-B]吡啶-3-胺 | ||
| 化学名 | 2-(butylsulfinyl)-4-phenyl-6-(thiophen-2-yl)thieno[2,3-b]pyridin-3-amine | ||
| Canonical SMILES | NC1=C(S(CCCC)=O)SC2=NC(C3=CC=CS3)=CC(C4=CC=CC=C4)=C21 | ||
| 分子式 | C21H20N2OS3 | 分子量 | 412.59 |
| 溶解度 | ≥ 20.65mg/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 | 2.4237 mL | 12.1186 mL | 24.2371 mL |
| 5 mM | 0.4847 mL | 2.4237 mL | 4.8474 mL |
| 10 mM | 0.2424 mL | 1.2119 mL | 2.4237 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。
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