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Asivatrep

Name: Asivatrep
Brand: TargetMol
SKU: T16426
Rating: 4.5 (1 reviews)

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Catalog No. T16426Cas No. 1005168-10-4

Alias PAC-14028, PAC14028

Asivatrep (PAC14028) is a selective and potent antagonist of transient receptor potential vanilloid subtype 1 (TRPV1) for the study of atopic dermatitis.

Asivatrep

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Purity: 95.13%

Catalog No. T16426Alias PAC-14028, PAC14028Cas No. 1005168-10-4

Asivatrep (PAC14028) is a selective and potent antagonist of transient receptor potential vanilloid subtype 1 (TRPV1) for the study of atopic dermatitis.

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$347	6-8 weeks	6-8 weeks
25 mg	$1,140	6-8 weeks	6-8 weeks
50 mg	$1,490	6-8 weeks	6-8 weeks
100 mg	$1,990	6-8 weeks	6-8 weeks
1 mL x 10 mM (in DMSO)	$375	6-8 weeks	6-8 weeks

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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:95.13%

Appearance:Oil

Color:Transparent

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COA

Product Introduction

Bioactivity

Description	Asivatrep (PAC14028) is a selective and potent antagonist of transient receptor potential vanilloid subtype 1 (TRPV1) for the study of atopic dermatitis.
In vitro	Asivatrep has demonstrated significant efficacy in several disease models, including visceral pain, inflammatory bowel disease, and inflammatory pain. Asivatrep has potential in the treatment of atopic dermatitis due to its ability to prevent damage to the skin barrier, accelerate barrier recovery, and inhibit itching.Asivatrep also reduces elevated serum levels of IgE, inhibits inflammatory cell infiltration in the epidermis, and degranulation of mast cells in atopic dermatitis.Asivatrep has been shown to be effective in preventing damage to the skin barrier, accelerating barrier recovery, and inhibiting itching. [2]
In vivo	Pharmacokinetically, Asivatrep has a plasma half-life of 2.1 hours in rats and is slightly prolonged to 3.8 hours in minipigs. In addition, oral bioavailability was 52.7% in rats and 64.2% in minipigs, demonstrating good oral absorption. [1] Asivatrep was able to inhibit capsaicin-induced calcium influx into keratinocytes at submicromolar concentrations, suggesting a potent TRPV1 antagonism. In vivo, Asivatrep blocked capsaicin-induced increase in blood perfusion and accelerated the recovery of skin barrier damage induced by tape stripping (in hairless mice). [3]
Synonyms	PAC-14028, PAC14028

Chemical Properties

Molecular Weight	491.48
Formula	C₂₁H₂₂F₅N₃O₃S
Cas No.	1005168-10-4
Smiles	C(CC)C1=C(/C=C/C(N[C@H](C)C2=CC(F)=C(NS(C)(=O)=O)C(F)=C2)=O)C=CC(C(F)(F)F)=N1
Relative Density.	1.381 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 40 mg/mL (81.39 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.07 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	2.0347 mL	10.1734 mL	20.3467 mL	101.7335 mL
5 mM	0.4069 mL	2.0347 mL	4.0693 mL	20.3467 mL
10 mM	0.2035 mL	1.0173 mL	2.0347 mL	10.1734 mL
20 mM	0.1017 mL	0.5087 mL	1.0173 mL	5.0867 mL
50 mM	0.0407 mL	0.2035 mL	0.4069 mL	2.0347 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