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AM-2099 Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5754503

MBS5754503 is an inhibitor targeting AM-2099. AM-2099 is a voltage-gated sodium channel Nav1.7 inhibitor (IC50: 0.16uM). More details

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

Product Overview

Online Datasheet in PDF
Product Name
AM-2099, Inhibitor
Full Product Name
AM-2099
Product Gene Name
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
466.46
Solubility
DMSO: 150mg/mL (321.57mM)
(<1mg/ml refers to the product slightly soluble or insoluble)
Formula
C19H13F3N4O3S2
SMILES
COC1=CC(C(F)(F)F)=CC=C1C2=NC=NC3=CC(S(=O)(NC4=NC=CS4)=O)=CC=C32
CAS Number
1443373-17-8
Target & IC50
human Nav1.7: ic50 0.16uM
mouse Nav1.7: ic50 0.18uM
rat Nav1.7: ic50 3.5uM
In Vitro
AM-2099 demonstrates a dose-dependent increase in plasma exposure with a concomitant dose-dependent reduction in scratching bouts compared to vehicle-treated animals, with a statistically significant reduction observed at the 60mg/kg dose[1]. AM-2099 demonstrates a favorable pharmacokinetic profile in rat and dog. In rats AM-2099 shows low total clearance and moderate Vdss and half-life. However, when dosed in dogs AM-2099 shows very low clearance, a low Vdss and long halflife (18 h).

Structure of AM-2099, inhibitor

AM-2099 Inhibitor – Cat# MBS5754503

Product References and Citations for AM-2099, inhibitor

Marx IE, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067.
Marx IE, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067.

Other Notes

Small volumes of AM-2099, 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.
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