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Coptisine chloride is an effective and non-competitive IDO inhibitor with Ki value of 5.8 μM and IC50 value of 6.3 μM. Coptisine chloride is an effective H1N1 neuraminidase (NA-1) inhibitor with IC50 of 104.6 μg/mL, which can be used for influenza A virus (H1N1) infection.
Coptisine (12.5, 25, 50 μM) upregulates the expression of pH2AX and p21, reduces expression of cyclin B1, cdc2, and cdc25C, and induces G2/M arrest and apoptosis of A549 cells in a concentration-dependent manner. Coptisine (12.5, 25, 50 μM) also induces mitochondrial dysfunction and activates caspases activities in A549 cells. Furthermore, Coptisine (50 μM) increases ROS levels in a time-dependent manner (0.5, 1, 2, 4, 12, and 24 h).
Coptisine (23.35, 46.7, 70.05 mg/kg, p.o.) dose-dependently decreases the levels of TC, TG, and LDL-c and increases HDL-c content in serum of hamsters to different degree, slows down weight gain induced by the HFHC diet, and raises the level of cholesterol and TBA in feces dose-dependently in hamsters. Coptisine (70.05 mg/kg, p.o.) suppresses HMGCR protein expression level and induces the protein expression of SREBP-2, LDLR, and CYP7A1 involved in cholesterol metabolism.
| Molecular Weight | 355.77 |
| Formula | C19H14ClNO4 |
| CAS Number | 6020-18-4 |
| Solubility (25°C) | DMSO 8 mg/mL |
| Storage | 4°C, dry, sealed |
| Related IDO Products |
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| (S)-LY-3381916
(S)-LY-3381916 is an active S-isomer of LY-3381916. (S)-LY-3381916 binds to IDOL with an IC50 value less than 1.5 µΜ. LY-3381916 is a potent, selective and brain penetrated inhibitor of Indoleamine 2,3-Dioxygenase 1 (IDO1) activity, binds to apo-IDO1 lacking heme rather than mature heme-bound IDO1. |
| IDO2-IN-1
IDO2-IN-1 is an orally active and potent Indoleamine 2,3-dioxygenase 2 (IDO2) inhibitor with an IC50 value of 112 nM. IDO2-IN-1 can be used for the research of inflammatory autoimmunity. |
| IDO1/2-IN-1
IDO1/2-IN-1 is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. |
| IDO1/2-IN-1 hydrochloride
IDO1/2-IN-1 hydrochloride is the first potent IDO1/IDO2 dual inhibitor with IC50s of 28 nM and 144 nM for IDO1 and IDO2, respectively. |
| IDO-IN-18
IDO-IN-18 is an IDO inhibitor. |
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