2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. Asivatrep

Asivatrep  (Synonyms: PAC-14028)

Cat. No.: HY-12777 Purity: 95.16%
COA Handling Instructions

Molarity Calculator

Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.

For research use only. We do not sell to patients.

Asivatrep Chemical Structure

Asivatrep Chemical Structure

CAS No. : 1005168-10-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 454 In-stock
Solution
10 mM * 1 mL in DMSO USD 454 In-stock
Solid
1 mg USD 180 In-stock
5 mg USD 420 In-stock
10 mg USD 600 In-stock
50 mg USD 1800 In-stock
100 mg USD 2520 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Asivatrep Related Antibodies

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

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TRPC TRPM TRPV TRPA TRPML

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Asivatrep (PAC-14028) is a potent and selective transient receptor potential vanilloid type I (TRPV1) antagonist.

In Vitro

Asivatrep (PAC-14028) could prevent barrier damages, accelerate skin barrier recovery and suppress pruritus, showing a potential for the treatment of atopic dermatitis. It could suppress serum IgE increase, epidermal infiltration of inflammatory cells and mast cell degranulation associated with atopic dermatitis[1]. Asivatrep (PAC-14028) shows efficacies against diverse disease models including visceral pain, inflammatory bowel disease, and inflammatory pain[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Asivatrep Related Antibodies
In Vivo

Asivatrep (PAC-14028) shows a plasma half-life of 2.1 h in rats while it is extended slightly to 3.8 h in minipigs. Oral bioavailability at 10 mg/kg dose is determined to be 52.7% and 64.2% in rats and minipigs, respectively suggesting that Asivatrep (PAC-14028) is relatively well-absorbed through oral route[1]. Asivatrep (PAC-14028) 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 increase, and the accelerated barrier recovery from tape-stripping-induced barrier damages in hairless mice[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

491.47

Formula

C21H22F5N3O3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@@H](C1=CC(F)=C(NS(=O)(C)=O)C(F)=C1)C)/C=C/C2=CC=C(C(F)(F)F)N=C2CCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (101.74 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0347 mL 10.1736 mL 20.3471 mL
5 mM 0.4069 mL 2.0347 mL 4.0694 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (5.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 95.16%

COA (246 KB) RP-HPLC (206 KB)

Handling Instructions (2659 KB)
References
Animal Administration
[1]

Rats: 1 mg of Asivatrep (PAC-14028) is dissolved in 10 mL of methanol to obtain a concentration of 100 μg/mL. Male Sprague-Dawley rats/minipigs are given intravenously Asivatrep (PAC-14028) at a single dose of 1 mg/kg, orally PAC-14028 at a single dose of 10 mg/kg as a suspension in 1% methylcellulose and 0.5% Tween80, or topically a single or multiple doses of 10 mg/kg as 1% Asivatrep (PAC-14028) solution (gel form) in 68% PEG400 vehicle. For the topical application, dorsal area is shaved and painted with designated dose of Asivatrep (PAC-14028) formulation. Occlusive dressing is placed on the applied region for 6 h to withhold licking or scratching the area. Blood samples are collected from the retroorbital sinus or jugular vein into heparinized tubes at designated times after drug administration. Blood samples are centrifuged immediately, and the plasma is collected and store for analysis[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0347 mL 10.1736 mL 20.3471 mL 50.8678 mL
5 mM 0.4069 mL 2.0347 mL 4.0694 mL 10.1736 mL
10 mM 0.2035 mL 1.0174 mL 2.0347 mL 5.0868 mL
15 mM 0.1356 mL 0.6782 mL 1.3565 mL 3.3912 mL
20 mM 0.1017 mL 0.5087 mL 1.0174 mL 2.5434 mL
25 mM 0.0814 mL 0.4069 mL 0.8139 mL 2.0347 mL
30 mM 0.0678 mL 0.3391 mL 0.6782 mL 1.6956 mL
40 mM 0.0509 mL 0.2543 mL 0.5087 mL 1.2717 mL
50 mM 0.0407 mL 0.2035 mL 0.4069 mL 1.0174 mL
60 mM 0.0339 mL 0.1696 mL 0.3391 mL 0.8478 mL
80 mM 0.0254 mL 0.1272 mL 0.2543 mL 0.6358 mL
100 mM 0.0203 mL 0.1017 mL 0.2035 mL 0.5087 mL
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Asivatrep Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Asivatrep1005168-10-4PAC-14028PAC14028PAC 14028TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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