STING agonist-3
(Synonyms: CS-0029879, Diamidobenzimidazole STING Agonist, diABZI-3, EX-A3217, HY-103665, STING Agonist-3) 目录号 : GC37692
A STING agonist
Cas No.:2138299-29-1
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
diABZI STING agonist-3 is an agonist of stimulator of interferon genes (STING).1 It binds to STING (IC50 = 0.32 nM in a FRET assay) and induces STING transcriptional activity in a reporter assay (EC50 = 31.62 nM). diABZI STING agonist-3 increases protein levels of Nod-like receptor protein 3 (NLRP3), IL-1β, and IL-18, but not cGAS or mtDNA, in macrophages.2
1.Charnley, A.K., Darcy, M.G., Dodson, J.W., et al.Heterocyclic amides useful as protein modulators(2017) 2.Ning, L., Wei, W., Wenyang, J., et al.Cytosolic DNA-STING-NLRP3 axis is involved in murine acute lung injury induced by lipopolysaccharideClin. Transl. Med.10(7)e228(2020)
| Cas No. | 2138299-29-1 | SDF | |
| 别名 | CS-0029879, Diamidobenzimidazole STING Agonist, diABZI-3, EX-A3217, HY-103665, STING Agonist-3 | ||
| Canonical SMILES | O=C(N)C1=CC=C(N(C(NC(C2=CC(C)=NN2CC)=O)=N3)C/C=C/CN4C5=C(N=C4NC(C6=CC(C)=NN6CC)=O)C=C(C(N)=O)C=C5OCCCO)C3=C1 | ||
| 分子式 | C37H42N12O6 | 分子量 | 750.81 |
| 溶解度 | DMSO: 125 mg/mL (166.49 mM) | 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。 |
||
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.3319 mL | 6.6595 mL | 13.3189 mL |
| 5 mM | 0.2664 mL | 1.3319 mL | 2.6638 mL |
| 10 mM | 0.1332 mL | 0.6659 mL | 1.3319 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。
Synthesis and Biological Evaluation of Phosphoester and Phosphorothioate Prodrugs of STING agonist 3',3'-c-Di(2'F,2'dAMP)
J Med Chem 2021 Jun 10;64(11):7596-7616.PMID:34019405DOI:10.1021/acs.jmedchem.1c00301.
Cyclic dinucleotides (CDNs) are second messengers that bind to the stimulator of interferon genes (STING) and trigger the expression of type I interferons and proinflammatory cytokines. Here we evaluate the activity of 3',3'-c-di(2'F,2'dAMP) and its phosphorothioate analogues against five STING allelic forms in reporter-cell-based assays and rationalize our findings with X-ray crystallography and quantum mechanics/molecular mechanics calculations. We show that the presence of fluorine in the 2' position of 3',3'-c-di(2'F,2'dAMP) improves its activity not only against the wild type (WT) but also against REF and Q STING. Additionally, we describe the synthesis of the acyloxymethyl and isopropyloxycarbonyl phosphoester prodrugs of CDNs. Masking the negative charges of the CDNs results in an up to a 1000-fold improvement of the activities of the prodrugs relative to those of their parent CDNs. Finally, the uptake and intracellular cleavage of pivaloyloxymethyl prodrugs to the parent CDN is rapid, reaching a peak intracellular concentration within 2 h.