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AVN-101

Name: AVN-101
Brand: TargetMol
SKU: T26690
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T26690Cas No. 1061354-48-0

AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.

AVN-101

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Purity: 99.61%

Catalog No. T26690Cas No. 1061354-48-0

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$73	In Stock	In Stock
10 mg	$123	In Stock	In Stock
25 mg	$228	In Stock	In Stock
50 mg	$372	In Stock	In Stock
100 mg	$619	In Stock	In Stock
200 mg	$877	In Stock	-
1 mL x 10 mM (in DMSO)	$98	In Stock	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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Purity:99.61%

Appearance:Solid

Color:White

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COA HNMR HPLC LCMS

Product Introduction

Bioactivity

Description	AVN-101 is a highly potent 5-HT7 receptor antagonist with a Ki value of 153 pM. AVN-101 also exhibits considerable affinity for histamine H1 (Ki value of 0.58 nM) and adrenergic α2A, α2B and α2C (Ki values of 0.41-3.6 nM) receptors. AVN-101 has shown good oral bioavailability and brain-blood barrier permeability, low toxicity and reasonable efficacy in animal models of central nervous system diseases.
Targets&IC50	5-HT2C receptor:1.17 nM (Ki), α2B-adrenoceptor:0.41 nM (Ki), α2:0.41-3.6 nM(Ki), H1:0.58 nM(Ki), 5-HT7:153 pM(Ki), 5-HT2B receptor:10.6 nM (Ki), α1D-adrenoceptor:30.2 nM (Ki), α1A-adrenoceptor:18.9 nM (Ki), α2C-adrenoceptor:3.55 nM (Ki), α2A-adrenoceptor:1.77 nM (Ki), α1B-adrenoceptor:9.4 nM (Ki), 5-HT1A receptor:61 nM (Ki), 5-HT6 receptor:2.04 nM (Ki), 5-HT2A receptor:1.56 nM (Ki), 5-HT1B receptor:720 nM (Ki)
In vitro	METHODS: The ability of AVN-101 to block hERG channels was tested in single-cell patch clamp experiments using HEK cells stably expressing hERG potassium channels and measuring potassium currents. RESULTS Both AVN-101 and M1 blocked hERG channels with an IC50 score of 0.58 μM. [2]
In vivo	METHODS: AVN-101 (5 mg/kg) was evaluated in Wistar rats when administered by oral (PO) and intravenous (I.v) routes. AVN-101 was detected in plasma using LC-MS/MS. RESULTS The bioavailability of AVN-101 in rats (calculated based on AUC0 ⟶240 values) was 26.3% when injected intraperitoneally and 8.5% when administered orally. However, it should be noted that the drug elimination rate determined in the in vivo experiments, Kel = 0.0121 min-1 (i.v.), was significantly slower than that observed in rat microsomes (Kel = 0.335 min-1). [1]

Chemical Properties

Molecular Weight	340.89
Formula	C₂₁H₂₅ClN₂
Cas No.	1061354-48-0
Smiles	Cl.CN1CCC2=C(C1)C1=CC(C)=CC=C1N2CCC1=CC=CC=C1
Relative Density.	no data available

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 60 mg/mL (176.01 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9335 mL	14.6675 mL	29.3350 mL	146.6749 mL
5 mM	0.5867 mL	2.9335 mL	5.8670 mL	29.3350 mL
10 mM	0.2933 mL	1.4667 mL	2.9335 mL	14.6675 mL
20 mM	0.1467 mL	0.7334 mL	1.4667 mL	7.3337 mL
50 mM	0.0587 mL	0.2933 mL	0.5867 mL	2.9335 mL
100 mM	0.0293 mL	0.1467 mL	0.2933 mL	1.4667 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