store at low temperature,keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 97.00 | |
5 mg | In stock | $ 233.00 | |
10 mg | In stock | $ 345.00 | |
25 mg | In stock | $ 582.00 | |
50 mg | In stock | $ 832.00 | |
100 mg | In stock | $ 1,150.00 | |
500 mg | In stock | $ 2,290.00 |
Description | Guanfu base A is a potent noncompetitive CYP2D6 inhibitor (Ki: 1.20 μM in HLMs; Ki: 0.37 μM for rCYP2D6). It also inhibits HERG channel current. |
Targets&IC50 | CYP2D6:0.37 μM (Ki, cell free) |
In vitro | Guanfu base A has no inhibitory activity on mouse or rat CYP2Ds. Guanfu base A does not exhibit any inhibition activity on human recombinant 2C8, 2C19, CYP1A2, 2A6, 3A4, or 3A5, but shows slight inhibition of 2B6 and 2E1. Guanfu base A is a potent inhibitor of CYP2D6, with an IC50 recorded at ~0.46 μM in HLM (Dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (Bufuralol 5 μM)[1]. Guanfu base A inhibits HERG channel current in concentration-, voltage-, and time-dependent manners with an IC50 of 1.64 mM. Guanfu base A shifts the activation curve in a negative direction and accelerated channel inactivation but shows no effect on the inactivation curve [2]. |
In vivo | Beagle dogs administered Dextromethorphan (2 mg/mL) intravenously following a pretreatment with Guanfu base A injection exhibited diminished CYP2D metabolic activity. This was evidenced by the maximum concentration (Cmax) of dextrorphan being one-third compared to the saline-treated group and the area under the plasma concentration-time curve being half of that observed in the saline-treated group [1]. |
Source |
Synonyms | Guan-fu base A |
Molecular Weight | 429.5 |
Formula | C24H31NO6 |
CAS No. | 1394-48-5 |
store at low temperature,keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mM
You can also refer to dose conversion for different animals. More
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Guanfu base A 1394-48-5 Angiogenesis JAK/STAT signaling Membrane transporter/Ion channel Metabolism Tyrosine Kinase/Adaptors HER P450 Potassium Channel inhibit Inhibitor KcsA Guan-fu base A inhibitor