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Asivatrep Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5755325

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

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Product Documentation
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Sample Manual Insert View PDF
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Testing Data View PDF
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Certificate of Analysis (COA) View PDF
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QC Report View PDF
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Material Safety Data Sheet View PDF
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Technical Datasheet View PDF
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Protocol View PDF

Product Overview

Online Datasheet in PDF
Product Name
Asivatrep, Inhibitor
Full Product Name
Asivatrep
Product Synonym Names
PAC-14028
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
491.47
Solubility
DMSO: 50mg/mL (101.74mM) Need ultrasonic
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C21H22F5N3O3S
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
CAS Number
1005168-10-4
Target & IC50
Others
In Vitro
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 10mg/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].

Structure of Asivatrep, inhibitor

Asivatrep Inhibitor – Cat# MBS5755325

Product References and Citations for Asivatrep, inhibitor

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.
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.
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.
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.
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.
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.

Other Notes

Small volumes of Asivatrep, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Asivatrep purchase

MBS5755325 is an inhibitor targeting Asivatrep.
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