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H-151

Cat. No. M10126
H-151 Structure
Synonym:

H151

Size Price Availability Quantity
5mg USD 55  USD55 In stock
10mg USD 80  USD80 In stock
50mg USD 280  USD280 In stock
100mg USD 450  USD450 In stock
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Quality Control & Documentation
Biological Activity

H-151 is a highly potent, selective and covalent antagonist of STING, reduces TBK1 phosphorylation and suppresses human STING palmitoylation. H-151 (0.02-2 μM) reduces IFNβ luciferase reporter measurements of HEK293T cells. H-151 (0.5 μM; 2 h) inhibits the phosphorylation of TBK1 in THP-1 cells.

Chemical Information
Molecular Weight 279.34
Formula C17H17N3O
CAS Number 941987-60-6
Solubility (25°C) DMSO ≥ 100 mg/mL
Storage -20°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yanhong Pan, et al. Br J Pharmacol. The STING antagonist H-151 ameliorates psoriasis via suppression of STING/NF-κB-mediated inflammation

[2] Simone M Haag, et al. Nature. Targeting STING with covalent small-molecule inhibitors

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Keywords: H-151, H151 supplier, STING, inhibitors, activators


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