规格 | 价格 | 库存 | 数量 |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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体外研究 (In Vitro) |
在完全发育的脂肪细胞中,BVT 2733(100 μM;24 小时)与 PA (100 μM) 共同处理可降低 MCP-1 表达 [3]。 Elisa 检查了 J774.1 巨噬细胞培养基中炎症蛋白(MCP-1、IL-6)的水平,发现 BVT 2733(50-100 μM;24 小时)可降低炎症蛋白的水平 [3]。
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体内研究 (In Vivo) |
口服 BVT-2733(100 毫克/千克;每天两次;两周)可降低 CIA 小鼠的抗 CII 水平和关节炎的严重程度,以及 TNF-α、IL-1β、IL-6 和 IL-6 的水平。他们的血清中有 17 个[2]。与对照小鼠相比,BVT 2733(口服;100 mg/kg;剂量[09:00和17:00小时);过去 4 周)显示体重减轻,胰岛素敏感性和葡萄糖耐量改善。此外,它还抑制与炎症相关的基因的表达,例如肿瘤坏死因子α (TNF-α)、单核细胞趋化蛋白1 (MCP-1) 以及进入人体脂肪组织的巨噬细胞的数量[3]。
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细胞实验 |
RT-PCR[3]
细胞类型:分化脂肪细胞 测试浓度: 100 μM 孵育时间: 24 hrs (hrs (小时)) 实验结果: MCP-1 mRNA 水平下调。 |
动物实验 |
Animal/Disease Models: Collagen-induced arthritis (CIA) mice [2]
Doses: 100 mg/kg Route of Administration: Oral; twice (two times) daily; 2 weeks Experimental Results: diminished synovial inflammation and joint destruction. Animal/Disease Models: C57BL/6J mice [3] Doses: 100 mg/kg Route of Administration: po (po (oral gavage)) Take the drug (09:00 and 17:00); Results in the past 4 weeks: Improved metabolic homeostasis in diet-induced obese mice and inhibits inflammation of adipose tissue. |
参考文献 |
[1]. 11β-hydroxydehydrogenase 1 (11β-HSD1) Inhibitor in Development
[2]. Zhang L, et al. 11β-Hydroxysteroid dehydrogenase 1 inhibition attenuates collagen-induced arthritis. Int Immunopharmacol. 2013 Nov;17(3):489-94. [3]. Wang L, et al. BVT.2733, a selective 11β-hydroxysteroid dehydrogenase type 1 inhibitor, attenuates obesity and inflammation in diet-induced obese mice. PLoS One. 2012;7(7):e40056. |
分子式 |
C17H21CLN4O3S2
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分子量 |
428.95
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精确质量 |
428.07436
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CAS号 |
376640-41-4
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相关CAS号 |
376640-41-4
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SMILES |
CN1CCN(C(CC2=CSC(NS(=O)(C3=CC=CC(Cl)=C3C)=O)=N2)=O)CC1
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InChi Key |
YDPRNGAPPNPYQQ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C17H21ClN4O3S2/c1-12-14(18)4-3-5-15(12)27(24,25)20-17-19-13(11-26-17)10-16(23)22-8-6-21(2)7-9-22/h3-5,11H,6-10H2,1-2H3,(H,19,20)
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化学名 |
3-chloro-2-methyl-N-(4-(2-(4-methylpiperazin-1-yl)-2-oxoethyl)thiazol-2-yl)benzenesulfonamide
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别名 |
BVT-2733 BVT 2733 BVT2733 BVT.2733
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO : ~50 mg/mL (~116.56 mM)
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.83 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 1 mg | 5 mg | 10 mg | |
1 mM | 2.3313 mL | 11.6564 mL | 23.3127 mL | |
5 mM | 0.4663 mL | 2.3313 mL | 4.6625 mL | |
10 mM | 0.2331 mL | 1.1656 mL | 2.3313 mL |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
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)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
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 ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。