- surface antigen (208-215) [Hepatitis B Virus]
- HBcAg [Hepatitis B virus] (18-27)
- Telbivudine
- Merimepodib
- Adefovir Dipivoxil
| GS-9620TLR-7 agonist |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.01%
- COA (Certificate Of Analysis)
- HPLC (Retest)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Description | GS-9620 is a potent and selective orally active small-molecule agonist of Toll-like receptor 7(TLR-7). | |||||
| Targets | TLR-7 | |||||
| IC50 | ||||||
| Cell experiment [1]: | |
Cell lines | Peripheral blood mononuclear cells (PBMCs) or plasmacytoid dendritic cells (pDCs) |
Preparation method | Soluble in DMSO. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | 14 ~ 66 nM |
Applications | In human and cynomolgus monkey PBMCs and/or pDCs, GS-9620 induced interferon (IFN)-alpha and other cytokines, with a minimum effective concentration ranging from 14 to 66 nM in humans and with 5-fold less potency in monkeys. |
| Animal experiment [1]: | |
Animal models | Cynomolgus monkeys |
Dosage form | single doses of 0.1 ~ 2.0 mg, daily doses of 0.1 ~ 1.0 mg for 7 days or every other day doses of 0.05 ~ 1.5 mg for 28 days; p.o. |
Applications | In cynomolgus monkeys, GS-9620 was well tolerated even at the highest oral doses (1.5 mg every other day for 28 days). GS-9620 increased IFN-alpha, immunomodulatory cytokines, chemokines and peripheral blood cell IFN stimulated genes (ISGs) in a dose-dependent manner. In addition, there was no evidence of tachyphylaxis following every other day dosing, and oral administration resulted in limited systemic bioavailability but high oral absorption. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Turnas P, Zheng X, Lu B, et al. 1129 Preclinical characterization of GS-9620, a potent and selective oral TLR7 agonist[J]. Journal of Hepatology, 2011, 54: S446-S447. | |
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| Cas No. | 1228585-88-3 | SDF | Download SDF |
| Synonyms | GS 9620;GS9620 | ||
| Chemical Name | 4-amino-2-butoxy-8-[[3-(pyrrolidin-1-ylmethyl)phenyl]methyl]-5,7-dihydropteridin-6-one | ||
| Canonical SMILES | CCCCOC1=NC2=C(C(=N1)N)NC(=O)CN2CC3=CC(=CC=C3)CN4CCCC4 | ||
| Formula | C22H30N6O2 | M.Wt | 410.51 |
| Solubility | ≥20.55 mg/mL in DMSO, ≥9.9 mg/mL in EtOH with ultrasonic and warming, <2.66 mg/ml="" in="" h2o=""> | Storage | Store at -20°C |
| Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
GS-9620 is an orally active TLR7 agonist with EC50 of 291 nM. [1]Toll-like receptor 7 (TLR7) is a pathogen recognition receptor which plays an important role in the detection of, and the innate immune response to, pathogens. TLR7 signaling is predominantly activated by viral single-stranded RNA and is localized within the endolysosomal compartments of plasmacytoid dendritic cells (pDCs) and B lymphocytes in humans and non-human primates. Activation of pDCs plays an important role in the progress of innate response to viral pathogens and are involved in the majority of type I interferon (IFN) production during the acute phase of an infection by viruses. The induction and secretion of endogenous IFNs, including IFN-α and IFN- β, also induce the development of an efficient adaptive immunological response. Interferons induce the transcription of interferon-stimulated genes (ISGs) which generate an antiviral state within cells, as well as induce the production of other cytokines and chemokines which facilitate intercellular communication and cellular trafficking. GS-9620 could activate TLR7 signaling in immune cells to induce clearance of virus infected cells. [1, 2]GS-9620 selectively induces IFN-α, cytokines and chemokines. The minimum effective concentrations for IFN-α induction were similar in pDCs and in PBMCs from HCV-positive donors. GS-9620 demonstrates an EC50 of 291 nM for human TLR7, which is 30-fold selectivity over TLR8 with EC50 of 9 μM. [1]GS-9620 was administered to HBV infected chimpanzees for 8 weeks with an interval of 1 week. Consequently, serum concentrations of HBV surface antigen and HBV antigen, and the number of HBV antigen–positive hepatocytes, were decreased as hepatocyte apoptosis increased. In a phase 1 clinical trial to evaluate the safety and tolerability of GS-9620, treatment of GS-9620 results in dose dependent increases in select cytokines, chemokines, and ISGs beginning at 2mg and is safe in a single dose up to 12mg. Increases in percentages of immunocytes, like T cells, B cells and NK cells, expressing CD69 were also noted in subjects receiving GS-9620 treatment. [2, 3]References: [1]. Turnas P, Zheng X, Lu B, et al. 1129 Preclinical characterization of GS-9620, a potent and selective oral TLR7 agonist[J]. Journal of Hepatology, 2011, 54: S446-S447.[2]. Lanford R E, Guerra B, Chavez D, et al. GS-9620, an oral agonist of Toll-like receptor-7, induces prolonged suppression of hepatitis B virus in chronically infected chimpanzees[J]. Gastroenterology, 2013, 144(7): 1508-1517. e10.[3]. Lopatin U, Wolfgang G, Kimberlin R, et al. 737 A phase-i, randomized, double-blind, placebo-controlled study to evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of single escalating oral doses of GS-9620 in healthy subjects[J]. Journal of Hepatology, 2011, 54: S296.
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想用二步酶消法来分离毛乳头细胞，一个毛囊大概有多少个毛乳头细胞？处于生长期的毛囊在显微镜下有什么特点？先谢谢大神们指点
经过无数次的大鼠肝脏插针灌注，忍受过实验结果不理想的打击和折磨，今天终于成功了，特分享些相关图片以鼓励还在奋战中的网友们。
最近在做黄体化颗粒细胞分离培养，但是注射器吸取大卵泡液或者从下颗粒细胞离心时就会凝固成果冻状，大家有碰到过这样的事情么？已经好几次了，一直是这样，大家给支个招吧
我的步骤：
1、16－22天小鼠颈椎脱臼法处死后，75%酒精浸泡30秒消毒，睾丸取出后置预冷PBS，40分钟（路上所需时间）后开始处理。
2、剔除白膜，剪碎睾丸。0.25%胰酶（含edta）1.5ml/个睾丸37°C消化30-50分钟，等体积DMEM/F12含10%FBS终止消化，1000r/MIN离心5分钟，弃上液。
3、加0.1%胶原酶消化30分钟，过200目网筛，1000r/MIN离心5分钟，弃上液。
4、DMEM/F12含10%FBS5ml重悬后转如培养瓶，入孵育箱37°C5%CO2培养。
请教各位，我到底是哪里有问题，是胰酶消化的时间长了吗？
近期根据经验总结了原代肿瘤细胞分离培养的2个关键因素。
1、组织的活性：如果我们取的都是坏死的组织或者结缔组织，我相信任何方法都不可能分离出来活的细胞的。另外，取完的组织要冷藏存放，并且越早分离越好，最好在24h内，最久不要超过48h。
2、组织的消化：在组织消化前，组织剪的越碎越好（1mm3左右为宜），组织的大小决定了组织的消化时间，不同组织消化时间差别较大：例如肺癌在2h-2.5h；食管癌在1个多小时。
希望可以帮到各位研友，另外如果大家有更好的经验可以一起来讨论！
前辈们好，近期老板布置任务需要分离小鼠肝脏细胞，查了好多文献，都没有写胶原酶的cat#,只写sigma订购，想请教下，是否有人做过，可以提供下货号和使用方法吗？十分感谢。另外，文中还提到digitonin，如果有一起用到的话麻烦帮我查看下，谢谢。
我做的临床试验，就想简单检测PBMC细胞的凋亡，上流式检测，有啥检测效果好的步骤推荐一下，谢谢
大概步骤如下：c57小鼠大概六七只，酒精浸泡后不处死取出，迅速打开胸腔取出心脏放入冰PBS冲洗。待心脏取出完毕，冲洗移入有PBS青霉素小瓶中用眼科剪剪成较小组织块。
之后加入0.1％胰酶消化（之前浓度为0.25％，活细胞数量更少。）吹打1min.放入孵箱中3min.弃去上清，加入∥型胶原酶（0.1％）吹打10Min，放入孵箱15Min。取出后加入1ml胰酶。吹打1Min后加入含血清F12培养液终止消化，800转离心5Min。之后取沉淀重悬种板。90Min差速贴壁法纯化心肌细胞。
48h后只有少量（个位数）细胞贴壁，呈三角形。
第一次用0.25％胰酶时离心后有大量鼻涕样物质。
第二次胰酶浓度减小后没有，但细胞沉淀少，且为半透明微白。是不是离心时间不够。
感觉细胞整体状态都不好，几次都没有大量心肌细胞，更不用说观察到心肌细胞搏动。
老师们能不能帮忙分析一下是哪里的原因呢。
有没有比较稳定的小鼠乳鼠心肌细胞分离步骤呢。
希望大神快点出现。
请大神前辈指点指点，已经研三了，实验很不顺利，再这样都要延期的节奏了。请问最近急性分离出来的大鼠心肌细胞很不耐钙，做膜片钳封接不上可能是什么原因造成的？谢谢了！
