Basic information Safety Supplier Related

diABZI STING agonist-1 trihydrochloride

Basic information Safety Supplier Related

diABZI STING agonist-1 trihydrochloride Basic information

Product Name:
diABZI STING agonist-1 trihydrochloride
Synonyms:
  • diABZI STING agonist-1 trihydrochloride
  • diABZI STING agonist-1
  • STING agonist-1（compound 3）trihydrochloride
  • STING?agonist?diABZ
  • (E)-1-(4-(5-Carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-(3-morpholinopropoxy)-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-methoxy-1H-benzimidazole-5-carboxamide tris(hydrochloride)
  • diABZI STING Agonist 3 (hydrochloride)
  • STING agonist-1 trihydrochloride
  • 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)
CAS:
2138299-34-8
MF:
C42H52ClN13O7
MW:
886.41
Mol File:
2138299-34-8.mol
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diABZI STING agonist-1 trihydrochloride Chemical Properties

storage temp. 
Store at -20°C
solubility 
DMSO: 50 mg/ml
form 
A crystalline solid
color 
White to yellow
InChIKey
PSJURLIZOBGEGB-HRNDJLQDSA-N
SMILES
C(N1C(=NC2=CC(C(=O)N)=CC(OCCCN3CCOCC3)=C12)NC(C1=CC(C)=NN1CC)=O)/C=C/CN1C(=NC2=CC(C(=O)N)=CC(OC)=C12)NC(C1=CC(C)=NN1CC)=O.Cl
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diABZI STING agonist-1 trihydrochloride Usage And Synthesis

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.

References

[1] JOSHI M. RAMANJULU. Design of amidobenzimidazole STING receptor agonists with systemic activity[J]. Nature, 2018, 564 7736: 439-443. DOI: 10.1038/s41586-018-0705-y
[2] QINGYUAN ZHU . Inhibition of coronavirus infection by a synthetic STING agonist in primary human airway system[J]. Antiviral research, 2021, 187: Article 105015. DOI: 10.1016/j.antiviral.2021.105015
[3] ZILAN SONG. Structure–Activity Relationship Study of Amidobenzimidazole Analogues Leading to Potent and Systemically Administrable Stimulator of Interferon Gene (STING) Agonists[J]. Journal of Medicinal Chemistry, 2021, 64 3: 1649-1669. DOI: 10.1021/acs.jmedchem.0c01900

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