CU-CPT9a

Catalog No.S9730 Batch:S973001

Technical Data

Formula	C₁₇H₁₅NO₂
Molecular Weight	265.31	CAS No.	2165340-32-7
Solubility (25°C)*	In vitro	DMSO	53 mg/mL (199.76 mM)
		Ethanol	10 mg/mL (37.69 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

CU-CPT9a is a potent and specific antagonist of Toll-like receptor 8 (TLR8) with IC50 of 0.5 nM.

Targets

TLR8 ^[1]
(Cell-free assay)

0.5 nM

In vitro

PBMC treatment with R848 or RNA-40 induces IL-6 production, and this activation is suppressed by CU-CPT9a in a dose-dependent manner. A dose-dependent suppression of IL-6 production by CU-CPT9a is also observed when cells are stimulated with violacein. Previous addition of CU-CPT9a only blocks IL-1β stimulated by R848 and has no effect on violacein-induced IL-1β stimulation.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines Human PBMCs Concentrations 0.02 μmol/L, 0.2 μmol/L, 2 μmol/L, 20 μmol/L Incubation Time 1 h Method Human PBMCs are cultured (50 μL of 6 × 10⁶ live cells/mL) in a 96-well plate. Cells are treated with different concentrations of CU-CPT9a (0.02, 0.2, 2 and 20 μmol/L) or medium as a negative control and are incubated for 1 h at 37 °C, 5% CO2. After this, cells are treated with violacein (30 and 15 μmol/L), R848 (1 μmol/L), LPS (50 ng/mL) or RNA-40 (5 μg/mL). After incubating for 20 h, the culture supernatants are collected and used to measure the concentration of IL-6 or IL-1β by ELISA according to the manufacturer’s instructions.

Cell Assay:^{^[2]}

Cell lines
Human PBMCs
Concentrations
0.02 μmol/L, 0.2 μmol/L, 2 μmol/L, 20 μmol/L
Incubation Time
1 h
Method
Human PBMCs are cultured (50 μL of 6 × 10⁶ live cells/mL) in a 96-well plate. Cells are treated with different concentrations of CU-CPT9a (0.02, 0.2, 2 and 20 μmol/L) or medium as a negative control and are incubated for 1 h at 37 °C, 5% CO2. After this, cells are treated with violacein (30 and 15 μmol/L), R848 (1 μmol/L), LPS (50 ng/mL) or RNA-40 (5 μg/mL). After incubating for 20 h, the culture supernatants are collected and used to measure the concentration of IL-6 or IL-1β by ELISA according to the manufacturer’s instructions.

References

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SHIPPING AND STORAGE
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