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TH 1020

Cat. No. M7408
TH 1020 Structure
Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 118  USD118 In stock
25mg USD 240  USD240 In stock
50mg USD 430  USD430 In stock
100mg USD 700  USD700 In stock
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Quality Control & Documentation
Biological Activity

TH1020 is an effective selective toll-like receptor 5 (TLR5)/ flagellin complex antagonist with IC50 of 0.85 μM. TH1020 inhibits flagellin-induced TLR5 signal transduction, but has no effect on TLR2, TLR3, TLR4, TLR7 and TLR8.

Chemical Information
Molecular Weight 453.54
Formula C23H15N7S2
CAS Number 1841460-82-9
Solubility (25°C) DMSO 2.27 mg/mL (with gentle warming)
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] Auerbach and Hjorth. Naunyn Schmiedebergs Arch Pharmacol. Effect of chronic administration of the selective serotonin (5-HT) uptake inhibitor citalopram on extracellular 5-HT and apparent autoreceptor sensitivity in rat forebrain in vivo.

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