规格 | 价格 | 库存 | 数量 |
---|---|---|---|
10 mM * 1 mL in DMSO |
|
||
500μg |
|
||
1mg |
|
||
5mg |
|
||
10mg |
|
||
25mg |
|
||
Other Sizes |
|
靶点 |
STING
|
---|---|
体外研究 (In Vitro) |
SP23表现出最高的STING降解效果,DC50为3.2μM。蛋白质印迹分析证实,SP23通过蛋白酶体依赖性途径PROTAC机制诱导STING降解。此外,STING/TBK1/NF-κB信号通路在THP-1细胞中下调。[1]
|
体内研究 (In Vivo) |
SP23在顺铂-AKI小鼠模型中表现出高的体内抗炎功效,并在体内有效保护小鼠肾脏免受顺铂诱导的损伤。从机制上讲,SP23在体内抑制STING信号通路的下游信号,这与体外实验的结果一致。SP23在AKI小鼠模型中也显示出良性毒性特征。[1]
|
酶活实验 |
酶联免疫吸附测定法。从小鼠眼球血样中收集培养基上清液和血清。根据产品手册,通过酶联免疫吸附测定试剂盒(B Neobioscience)测定小鼠和人IFN-β、CXCL10和IL-6的水平。[1]
|
细胞实验 |
细胞毒性(MTT)测定。使用MTT法评估新合成的化合物SP21-23对各种正常细胞系的细胞毒性,包括人正常肝细胞(LO2)、人胚胎肾细胞(HEK293A)和小鼠神经干细胞(C17.2)。将细胞以5000个细胞/孔的密度接种到96孔板中。在用指定浓度的化合物SP21-23处理后,加入MTT(在PBS中为5mg/mL),并将细胞再孵育4小时。用微孔板读取器在570nm的波长下检测细胞活力。[1]
|
动物实验 |
In Vivo Anti-inflammatory Efficacy Study.
Eight-week-old C57BL/6J male mice were purchased from Guangzhou Southern Medical University Experimental Animal Technology Development Co, certificate number: 110324201104674226. All experimental procedures were approved by Ethical Committee at SMU (Southern Medical University) and implemented accordingly. After 24 h of diurnal circulation and free diet and water, mice were randomly assigned to the following four groups: control group and cisplatin induction model group (25 mg/kg), low-dose treatment group (SP23, 30 mg/kg), and high-dose treatment group (SP23, 60 mg/kg). Mice were pretreated with SP23 administered intraperitoneally 1 h prior to cisplatin injection and administered continuously at the same time each day. Seventy-two hours after cisplatin treatment, all mice were euthanized, blood samples and heart, liver, and kidney tissues were collected. One sample from each tissue in each group was randomly selected and fixed in 4% paraformaldehyde for histological examination, and the remaining tissues were immediately frozen in liquid nitrogen and stored at -80°C. Urea nitrogen (BUN) and creatinine concentrations were determined at the Guangzhou Huayin Medical Laboratory Center using a serum biochemical auto-analyzer. Renal imaging was monitored by the Small Animal Magnetic Resonance Imaging System (PharmaScan70/16, USA) at the Southern Medical University Experimental Center.[1] Pharmacokinetic Study in Male SD Rats. Male SD rats (300-360 g) were purchased from Liaoning Changsheng Biotechnology Co., Ltd. Diet was prohibited for 12 h before the experiment but water was freely available. Blood samples (0.5 mL) were collected from the tail vein into heparinized 1.5 mL polythene tubes at 0.0833, 0.25, 0.5, 1, 2, 3, 4, 6, 8, 12, 24, 36, and 48 h after oral (20 mg/kg) or intravenous (2 mg/kg) administration of compound SP23. Waters Acquity UPLC (Waters Corp., Milford, MA, USA) was used for the separation of SP23 and internal standard compound. The effective separation of SP23 and internal standard compound was achieved on Acquity UPLC BEH C18 column (50 × 2.1 mm, 1.7 μm, Waters Corporation, Milford, MA, USA) used at a column temperature of 40 °C. The mobile phase consisted of a mixture of solvent A (acetonitrile) and solvent B (formic acid/ ultrapure water, 1:1000, v/v). The linear gradient program for the mobile phase was set as follows: 0 min 10% A; 0.5 min 30% A; 1 min 95% A; 2 min 95% A; 2.3 min 10% A. The flow rate of the mobile phase was 0.4 mL/min and the injection volume was 2 μL. The XEVO TQD triple quadrupole mass spectrometer was equipped with an electrospray ionization (ESI) source; multiple reaction monitoring (MRM) mode was selected for quantitation. The Mass Lynx 4.1 software (Waters Corp.) was used for data acquisition. Mass spectral data were obtained in positive electrospray mode (ESI+) in MRM mode. |
参考文献 |
分子式 |
C34H33N7O10
|
---|---|
分子量 |
699.666727781296
|
精确质量 |
699.23
|
元素分析 |
C, 58.37; H, 4.75; N, 14.01; O, 22.87
|
CAS号 |
2762552-74-7
|
外观&性状 |
Light yellow solid
|
LogP |
2.9
|
tPSA |
242Ų
|
SMILES |
C(NCCCCCCNC1=CC=CC2=C1C(=O)N(C1CCC(=O)NC1=O)C2=O)(=O)/C=C/C(NC1=CC=C(NC(C2=CC=C([N+]([O-])=O)O2)=O)C=C1)=O
|
InChi Key |
TXNQXRGOKABDOB-FOCLMDBBSA-N
|
InChi Code |
InChI=1S/C34H33N7O10/c42-26(15-16-27(43)37-20-8-10-21(11-9-20)38-32(46)25-13-17-29(51-25)41(49)50)36-19-4-2-1-3-18-35-23-7-5-6-22-30(23)34(48)40(33(22)47)24-12-14-28(44)39-31(24)45/h5-11,13,15-17,24,35H,1-4,12,14,18-19H2,(H,36,42)(H,37,43)(H,38,46)(H,39,44,45)/b16-15+
|
化学名 |
(E)-N-[6-[[2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindol-4-yl]amino]hexyl]-N'-[4-[(5-nitrofuran-2-carbonyl)amino]phenyl]but-2-enediamide
|
HS Tariff Code |
2934.99.9001
|
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)
|
溶解度 (体外) |
DMSO : ~100 mg/mL (~142.92 mM)
|
---|---|
溶解度 (体内) |
注意: 如下所列的是一些常用的体内动物实验溶解配方,主要用于溶解难溶或不溶于水的产品(水溶度<1 mg/mL)。 建议您先取少量样品进行尝试,如该配方可行,再根据实验需求增加样品量。
注射用配方
注射用配方1: DMSO : Tween 80: Saline = 10 : 5 : 85 (如: 100 μL DMSO → 50 μL Tween 80 → 850 μL Saline)(IP/IV/IM/SC等) *生理盐水/Saline的制备:将0.9g氯化钠/NaCl溶解在100 mL ddH ₂ O中,得到澄清溶液。 注射用配方 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (如: 100 μL DMSO → 400 μL PEG300 → 50 μL Tween 80 → 450 μL Saline) 注射用配方 3: DMSO : Corn oil = 10 : 90 (如: 100 μL DMSO → 900 μL Corn oil) 示例: 以注射用配方 3 (DMSO : Corn oil = 10 : 90) 为例说明, 如果要配制 1 mL 2.5 mg/mL的工作液, 您可以取 100 μL 25 mg/mL 澄清的 DMSO 储备液,加到 900 μL Corn oil/玉米油中, 混合均匀。 View More
注射用配方 4: DMSO : 20% SBE-β-CD in Saline = 10 : 90 [如:100 μL DMSO → 900 μL (20% SBE-β-CD in Saline)] 口服配方
口服配方 1: 悬浮于0.5% CMC Na (羧甲基纤维素钠) 口服配方 2: 悬浮于0.5% Carboxymethyl cellulose (羧甲基纤维素) 示例: 以口服配方 1 (悬浮于 0.5% CMC Na)为例说明, 如果要配制 100 mL 2.5 mg/mL 的工作液, 您可以先取0.5g CMC Na并将其溶解于100mL ddH2O中,得到0.5%CMC-Na澄清溶液;然后将250 mg待测化合物加到100 mL前述 0.5%CMC Na溶液中,得到悬浮液。 View More
口服配方 3: 溶解于 PEG400 (聚乙二醇400) 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 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 | 1.4292 mL | 7.1462 mL | 14.2925 mL | |
5 mM | 0.2858 mL | 1.4292 mL | 2.8585 mL | |
10 mM | 0.1429 mL | 0.7146 mL | 1.4292 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) 。