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Guanfu base A

Name: Guanfu base A
Brand: TargetMol
SKU: T8182
Price: 57 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T8182Cas No. 1394-48-5

Alias Guan-fu 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.

Guanfu base A

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Purity: 99.85%

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.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$57	-	In Stock
5 mg	$135	-	In Stock
10 mg	$202	-	In Stock
25 mg	$342	-	In Stock
50 mg	$489	-	In Stock
100 mg	$678	-	In Stock
200 mg	$918	-	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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.

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Batch Information

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Purity:99.85%

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

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].
Synonyms	Guan-fu base A

Chemical Properties

Molecular Weight	429.5
Formula	C₂₄H₃₁NO₆
Cas No.	1394-48-5
Smiles	[H][C@@]12CC34CC(=C)[C@]5([H])[C@@H](O)[C@@]3([H])[C@@]36C[C@H](C[C@@](C)(CN1C3[C@@]4(O)[C@@H]5OC(C)=O)[C@@]26[H])OC(C)=O
Relative Density.	1.43 g/cm3 (Predicted)

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/Shipping at ambient temperature.

Solubility Information

DMSO: 10 mM, Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.66 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.3283 mL	11.6414 mL	23.2829 mL	116.4144 mL
5 mM	0.4657 mL	2.3283 mL	4.6566 mL	23.2829 mL
10 mM	0.2328 mL	1.1641 mL	2.3283 mL	11.6414 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc