diABZI STING agonist-1 trihydrochloride
- Product Name
- diABZI STING agonist-1 trihydrochloride
- CAS No.
- 2138299-34-8
- Chemical Name
- diABZI STING agonist-1 trihydrochloride
- Synonyms
- di-ABZI;STING?agonist?diABZ;diABZI STING agonist-1;diABZI STING agonist-1 3HCl;STING agonist-1 trihydrochloride;diABZI STING Agonist-1 (hydrochloride);diABZI STING Agonist 3 (hydrochloride);diABZI STING agonist-1 trihydrochloride;STING agonist-1(compound 3)trihydrochloride;inhibit,diABZI STING agonist1 trihydrochloride,MPYS,diABZI STING agonist-1 trihydrochloride,ERIS,STING,Inhibitor,MITA,Stimulator of Interferon Genes,TMEM173,diABZI STING agonist 1 trihydrochloride
- CBNumber
- CB84818416
- Molecular Formula
- C42H52ClN13O7
- Formula Weight
- 886.41
- MOL File
- 2138299-34-8.mol
diABZI STING agonist-1 trihydrochloride Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: 50 mg/ml
- form
- A crystalline solid
- color
- White to yellow
N-Bromosuccinimide Price
- Product number
- 28054
- Product name
- diABZI STING Agonist 3 (hydrochloride)
- Packaging
- 1mg
- Price
- $299
- Updated
- 2024/03/01
- Product number
- 28054
- Product name
- diABZI STING Agonist 3 (hydrochloride)
- Packaging
- 5mg
- Price
- $743
- Updated
- 2024/03/01
- Product number
- 28054
- Product name
- diABZI STING Agonist 3 (hydrochloride)
- Packaging
- 500μg
- Price
- $158
- Updated
- 2024/03/01
- Product number
- A629825
- Product name
- 1-[(2E)-4-[5-(Aminocarbonyl)-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-methoxy-1H-benzimidazol-1-yl]-2-buten-1-yl]-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-[3-(4-morpholinyl)propoxy]-1H-benzimidazole-5-carboxamideHydrochloride(1:3)
- Packaging
- 1mg
- Price
- $360
- Updated
- 2021/12/16
- Product number
- 1582EN
- Product name
- 1-[(E)-4-[5-Carbamoyl-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-(3-morpholin-4-ylpropoxy)benzimidazol-1-yl]but-2-enyl]-2-[(2-ethyl-5-methylpyrazole-3-carbonyl)amino]-7-methoxybenzimidazole-5-carboxamide;trihydrochloride
- Packaging
- 1mg
- Price
- $430
- Updated
- 2021/12/16
diABZI STING agonist-1 trihydrochloride Chemical Properties,Usage,Production
Description
diABZI STING agonist-1 is an agonist of the stimulator of interferon genes (STING) pathway. It induces secretion of IFN-β in human peripheral blood mononuclear cells (PBMCs; EC50 = 130 nM). diABZI STING agonist-1 (2.5 mg/kg) increases serum levels of IFN-β, IL-6, TNF, and KC/GROα in wild-type, but not Sting-/-, mice. It inhibits the cytopathic effect of the common cold human coronavirus 229E (HCoV-229E) in infected MRC-5 cells (EC50 = 3 nM). diABZI STING agonist-1 also decreases the level of severe acute respiratory coronavirus 2 (SARS-CoV-2) RNA in primary human bronchial airway epithelial cells in an air-liquid interface assay. It decreases tumor volume and increases survival in a CT26 murine colorectal cancer model when administered at a dose of 3 mg/kg.
Uses
1-[(2E)-4-[5-(Aminocarbonyl)-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-methoxy-1H-benzimidazol-1-yl]-2-buten-1-yl]-2-[[(1-ethyl-3-methyl-1H-pyrazol-5-yl)carbonyl]amino]-7-[3-(4-morpholinyl)propoxy]-1H-benzimidazole-5-carboxamide Hydrochloride (1:3), an amino acid derivatve used in preparation of STING protein.
in vivo
diABZI STING agonist-1 trihydrochloride (subcutaneous injection; 2.5 mg/kg) induces STING-dependent activation of type-I interferon and pro-inflammatory cytokines in vivo[1]. diABZI STING agonist-1 trihydrochloride (intravenous injection; 3 mg/kg) exhibits systemic exposure with a half-life of 1.4 h and achieves systemic concentrations greater than the half-maximal effective concentration (EC50) for mouse STING (200 ng/ml)[1]. diABZI STING agonist-1 trihydrochloride (intravenous injection; 1.5 mg/kg; days 1, 4 and 8; 43 days) results in significant tumour growth inhibition and significantly improves survival (P < 0.001) with 8 out of 10 mice remaining tumor free at the end of the study on day 43[1].
Animal Model: | Wild and Sting?/? C57Blk6 mice[1] |
Dosage: | 2.5 mg/kg |
Administration: | Subcutaneous injection; 2.5 mg/kg |
Result: | Activated secretion of IFNβ, IL-6, TNF, and CXCL1 in wild-type but not Sting?/? mice. |
Animal Model: | Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice[1] |
Dosage: | 3 mg/kg |
Administration: | Intravenous injection; 3 mg/kg |
Result: | Exhibited a half-life of 1.4 hours and achieved systemic concentrations greater than EC50 for mouse STING (200 ng/ml). |
Animal Model: | Syngeneic mouse model of colorectal tumours (CT-26) in BALB/c mice[1] |
Dosage: | 1.5 mg/kg |
Administration: | Intravenous injection; 1.5 mg/kg; 43 days |
Result: | Resulted in significant tumour growth inhibition and improved survival. |
diABZI STING agonist-1 trihydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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