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Guanfu base A
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.
Catalog No. T8182Cas No. 1394-48-5
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Purity:99.85%
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Guanfu base A
Catalog No. T8182Alias Guan-fu base ACas No. 1394-48-5
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.
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose. | Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $81 | In Stock | |
| 5 mg | $193 | In Stock | |
| 10 mg | $289 | In Stock | |
| 25 mg | $489 | In Stock | |
| 50 mg | $698 | In Stock | |
| 100 mg | $968 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| 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 does not inhibit mouse or rat CYP2Ds and shows no inhibition of human recombinant 2C8, 2C19, CYP1A2, 2A6, 3A4, or 3A5, but demonstrates slight inhibition of 2B6 and 2E1. It is a potent inhibitor of CYP2D6 with an IC50 of ~0.46 μM in HLM (Dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (Bufuralol 5 μM)[1]. Additionally, Guanfu base A inhibits HERG channel current in a concentration-, voltage-, and time-dependent manner with an IC50 of 1.64 mM, shifts the activation curve negatively, and accelerates channel inactivation without affecting 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]. |
| Alias | Guan-fu base A |
| Molecular Weight | 429.5 |
| Formula | C24H31NO6 |
| Cas No. | 1394-48-5 |
Storage & Solubility Information
| Storage | store at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
| Solubility Information | DMSO: 10 mM | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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