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Asivatrep

Catalog No. T16426 CAS 1005168-10-4

Synonyms: PAC-14028

Asivatrep is an effective and selective transient receptor potential vanilloid type I antagonist.

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Asivatrep, CAS 1005168-10-4

Pack Size	Availability	Price/USD
5 mg	6-8 weeks	$ 347.00
25 mg	6-8 weeks	$ 1,140.00
50 mg	6-8 weeks	$ 1,490.00
100 mg	6-8 weeks	$ 1,990.00
1 mL * 10 mM (in DMSO)	6-8 weeks	$ 375.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Asivatrep is an effective and selective transient receptor potential vanilloid type I antagonist.
In vitro	Asivatrep displays efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain. Asivatrep could prevent barrier damages, accelerate skin barrier recovery, and inhibit pruritus, displaying a potential for the treatment of atopic dermatitis. It could inhibit serum IgE increase, epidermal infiltration of inflammatory cells, and mast cell degranulation associated with atopic dermatitis[1][2].
In vivo	Asivatrep displays a plasma half-life of 2.1 h in rats while it is extended slightly to 3.8 h in minipigs. Asivatrep could inhibit capsaicin-evoked calcium influx in keratinocytes at sub-micromolar concentrations. This potent TRPV1 antagonistic activity in keratinocytes is manifested in vivo as the blockade of capsaicin-induced blood perfusion increases, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice. Oral bioavailability at 10 mg/kg dose is determined to be 52.7% and 64.2% in rats and minipigs, respectively showing that Asivatrep is relatively well-absorbed through oral route[1][3].

Synonyms	PAC-14028
Molecular Weight	491.47
Formula	C21H22F5N3O3S
CAS No.	1005168-10-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 50 mg/mL (101.74 mM), Sonication is recommended.

References and Literature

1. Park YH, et al. Oral and topical pharmacokinetic studies of a novel TRPV1 antagonist, PAC-14028 in rats and minipigs using liquid chromatography/tandem mass spectrometric method. J Pharm Biomed Anal. 2012 Mar 5;61:8-14. 2. Lim KM, et al. Development of PAC-14028, a novel transient receptor potential vanilloid type 1 (TRPV1) channel antagonist as a new drug for refractory skin diseases. Arch Pharm Res. 2012 Mar;35(3):393-6. 3. Yun JW, et al. TRPV1 antagonist can suppress the atopic dermatitis-like symptoms by accelerating skin barrier recovery. J Dermatol Sci. 2011 Apr;62(1):8-15.

Dose Conversion

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

In vivo Formulation Calculator (Clear solution)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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An example of a molarity calculation using the molarity calculator
What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
Enter 197.13 into the Molecular Weight (MW) box
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The answer of 19.713 mg appears in the Mass box

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An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
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The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

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Molecule Formula

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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.

Keywords

Asivatrep 1005168-10-4 Others PAC-14028 PAC14028 PAC 14028 inhibitor inhibit

Products are chemical reagents for research use only and are not intended for human use. We do not sell to patients.