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

Asivatrep (Synonyms: PAC-14028)

Cat. No.: HY-12777 Purity: 95.14%
Handling Instructions

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
10 mM * 1 mL in DMSO USD 454 In-stock
Estimated Time of Arrival: December 31
1 mg USD 180 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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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].

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

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].

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.

1005168-10-4

SMILES

O=C(N[[email protected]@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 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (101.74 mM; Need ultrasonic)

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
10 mM 0.2035 mL 1.0174 mL 2.0347 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
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

Purity: 95.14%

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Keywords:

AsivatrepPAC-14028PAC14028PAC 14028TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

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