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CU-CPT-8m

Cat. No. M9746
CU-CPT-8m Structure
Synonym:

CU-CPT8m

Size Price Availability Quantity
5mg USD 120  USD120 In stock
10mg USD 200  USD200 In stock
25mg USD 350  USD350 In stock
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Quality Control & Documentation
Biological Activity

CU-CPT8m is an antagonist of toll-like receptor 8 (TLR8) with Kd of 220 nM and IC50 of 67 nM in assay. Treatment of 1 μM CU-CPT-8m completely abolishes the elevation of TNF-α and IL-8 mRNA levels induced by R848. CU-CPT-8m inhibits R848-induced TNF-α production in the differentiated THP-1 monocytes cells in a dose-dependent manner with an IC50 of 90±10 nM, which is in good agreement with its IC50 value determined in HEK-Blue TLR8 cells.

Chemical Information
Molecular Weight 252.27
Formula C14H12N4O
CAS Number 125079-83-6
Solubility (25°C) DMSO ≥ 22 mg/mL
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] Shuting Zhang, et al. Nat Chem Biol. Small-molecule inhibition of TLR8 through stabilization of its resting state

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