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SGA360 

Cat. No. M30473
SGA360  Structure
Size Price Availability Quantity
5mg USD 168  USD168 In stock
10mg USD 270  USD270 In stock
25mg USD 540  USD540 In stock
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Quality Control & Documentation
Biological Activity

SGA360 suppress inflammatory SAA1 signaling in an AHR-dependent manner through a mechanism that does not require AHR binding to its cognate response element (partial antagonist).

Chemical Information
Molecular Weight 362.35
Formula C19H17F3N2O2
CAS Number 680611-86-3
Form Solid
Solubility (25°C) DMSO 250 mg/mL (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] Gijs Rikken, et al. Biochem Pharmacol. Lead optimization of aryl hydrocarbon receptor ligands for treatment of inflammatory skin disorders

[2] Gulsum E Muku, et al. Toxicol Sci. Selective Ah Receptor Ligands Mediate Enhanced SREBP1 Proteolysis to Restrict Lipogenesis in Sebocytes

[3] Gulsum E Muku, et al. Lab Invest. Ligand-mediated cytoplasmic retention of the Ah receptor inhibits macrophage-mediated acute inflammatory responses

[4] Ellen H van den Bogaard, et al. J Invest Dermatol. Genetic and pharmacological analysis identifies a physiological role for the AHR in epidermal differentiation

[5] Kayla J Smith, et al. J Pharmacol Exp Ther. Identification of a high-affinity ligand that exhibits complete aryl hydrocarbon receptor antagonism

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  Catalog
Abmole Inhibitor Catalog




Keywords: SGA360  supplier, inhibitors, activators


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