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Auranofin

Cat. No. M3178
Auranofin Structure
Synonym:

SKF39162

Size Price Availability Quantity
10mM*1mL in DMSO USD 80  USD80 In stock
5mg USD 50  USD50 In stock
10mg USD 70  USD70 In stock
50mg USD 255  USD255 In stock
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Quality Control & Documentation
Biological Activity

Auranofin is an inhibitor of thioredoxin reductase (TrxR) (IC50 = 20 nM; Ki = 4 nM for the NADPH-reduced form of human cytosolic TrxR). Auranofin induced the mitochondrial permeability transition via inhibition of mitochondrial TrxR. Auranofin also exhibits anti-inflammatory and immunosuppressive activities. Auranofin inhibits 5-lipoxygenase at high concentrations and stimulates LTA hydrolase at low concentrations.

Chemical Information
Molecular Weight 678.48
Formula C20H34AuO9PS
CAS Number 34031-32-8
Solubility (25°C) DMSO ≥ 50 mg/mL (Need ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Kim NH, et al. Immunology. Auranofin blocks interleukin-6 signalling by inhibiting phosphorylation of JAK1 and STAT3.

[2] Rigobello MP, et al. Br J Pharmacol. Induction of mitochondrial permeability transition by auranofin, a gold(I)-phosphine derivative.

[3] Gromer S, et al. J Biol Chem. Human placenta thioredoxin reductase. Isolation of the selenoenzyme, steady state kinetics, and inhibition by therapeutic gold compounds.

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