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| | 1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]- Basic information |
| Product Name: | 1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]- | | Synonyms: | 1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-;STING agonist-4;TMEM173,STING agonist-4,MPYS,Inhibitor,STING agonist 4,STING,Stimulator of Interferon Genes,inhibit,ERIS,STING agonist4,MITA;diABZI STING Agonist-2;1H-Benzimidazole-5-carboxamide, 1,1′-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]- (ACI);1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-1H-benzimidazole-5-carboxamide;1-{4-[5-carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-amido)-1H-1,3-benzodiazol-1-yl]butyl}-2-(1-ethyl-3-methyl-1H-pyrazole-5-amido)-1H-1,3-benzodiazole-5-carboxamide;STING agonist-4, 10 mM in DMSO | | CAS: | 2138300-40-8 | | MF: | C34H38N12O4 | | MW: | 678.74 | | EINECS: | | | Product Categories: | | | Mol File: | 2138300-40-8.mol | ![1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]- Structure](CAS/20200331/GIF/2138300-40-8.gif) |
| | 1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]- Chemical Properties |
| density | 1.48±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO: slightly soluble | | form | A solid | | pka | 11.97±0.43(Predicted) | | color | White to gray | | InChIKey | ICZSAXDKFXTSGL-UHFFFAOYSA-N | | SMILES | C(N1C(NC(C2N(CC)N=C(C)C=2)=O)=NC2=CC(C(N)=O)=CC=C21)CCCN1C(NC(C2N(CC)N=C(C)C=2)=O)=NC2=CC(C(N)=O)=CC=C21 |
| | 1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]- Usage And Synthesis |
| Uses | STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function[1]. | | Biological Activity | STING agonist-4 is a stimulator of receptor agonists of the interferon gene (STING) with an apparent inhibition constant IC50 of 20 nM, It is a compound containing two symmetrically related aminobenzimidazoles (ABZI ) based compounds. | | in vitro | STING agonist-4 (Compound 2) (0.3-30 μM; 2 hours) causes phosphorylation of IRF3 and STING that is inhibited by the TBK1 inhibitor BX795 and induces dose-dependent secretion of IFN-β with an EC 50 of 3.1 μM. STING agonist-4 (Compound 2) (0.001 nM-1 μM) inhibits binding of full-length STING to the solid support with an apparent dissociation constant (K d < /sub> ) of approximately 1.6 nM. It (Compound 2) (0-100 μM) is 18-fold more potent than cGAMP (an endogenous STING ligand), with an EC 50 of 53.9 μM. STING agonist-4 (Compound 2) (3 μM; 4 hours) promotes production of interferon γ-induced protein 10 (IP-10), IL-6 and TNF-α by a mechanism that is dependent on STING-mediated activation of TBK1. Cell Viability Assay | Cell Line: | Human peripheral blood mononucl ear cells (PBMCs) | | Concentration: | 0.3 μM, 1 μM, 3 μM, 10 μM and 30 μM | | Incubation Time: | 2 hours | < td class="col1"> Result: | Caused phosphorylation of IRF3 and STING and induced secretion of IFN-β. | | | target | IC50: 20 nM (STING agonist-4) | | References | [1] Ramanjulu JM et al. Design of amidobenzimidazole STING receptor agonists with systemic activity. Nature. 2018 Dec;564(7736):439-443. DOI:10.1038/s41586-018-0705-y |
| | 1H-Benzimidazole-5-carboxamide, 1,1'-(1,4-butanediyl)bis[2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]- Preparation Products And Raw materials |
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