STING agonist-12

Names

[ CAS No. ]:
2259624-71-8

[ Name ]:
STING agonist-12

Biological Activity

[Description]:

STING agonist-12 (Compound 53) is a potent, orally active human STING activator with an EC50 of 185 nM[1].

[Related Catalog]:

Research Areas >> Inflammation/Immunology

Signaling Pathways >> Immunology/Inflammation >> STING

[Target]

EC50: 185 nM (STING)[1]

[In Vitro]

STING agonist-12 (Compound 53) (10 μM) shows excellent pan-polymorph activity across the panel of STING proteins (92%, 107% and 92% against R232, H232 and HAQ, respectively) in HEK293T cells[1]. STING agonist-12 is not active at mouse STING[1].

[In Vivo]

STING agonist-12 (Compound 53) (5 mpk for i.v.; 10 mpk for p.o.) is well-absorbed with a short terminal half-life[1]. Animal Model: Balb/c mice (n=3)[1] Dosage: 5 or 10 mpk Administration: Lateral tail vein or oral gavage (Pharmacokinetic Analysis) Result: Pharmacokinetic profile of STING agonist-12 (Compound 53) in mouse[1]. Route DOSE (mpk) AUC (ng/mL*h) T1/2 (h) Cmax (ng/mL) Vd (mL/kg) F (%) IV 5 1215 1.41 1867 2689 NA PO 10 2090 NA 1723 NA 86

[References]

[1]. Pryde DC, et al. The discovery of potent small molecule activators of human STING. Eur J Med Chem. 2021 Jan 1;209:112869.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₅H₁₉ClF₄N₂O₂

[ Molecular Weight ]:
490.88

Related Compounds

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