product summary
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company name :
Alomone Labs
product type :
chemical
product name :
RQ 00203078
catalog :
R-170
more info or order :
image
image 1 :
Alomone Labs R-170 image 1
Alomone Labs 5 7-Dichlorokynurenic acid nonohydrate inhibits NMDA (NR1+NR2A) channels expressed inXenopusoocytes. - A. Time course of NMDA currents that were elicited by stimulation with 10 M glutamate and 10 M Glycine every 50 sec while membrane potential was held at -80 mV. 5 and 20 M5 7-Dichlorokynurenic acid monohydrate(#D-191) applied for 2.5 min each as indicated inhibited the current amplitude in a reversible manner. B. superimposed current traces taken from the experiment described in A.
product information
CAT :
R-170
SKU :
R-170_10 mg
Product Name :
RQ 00203078
Group Type :
Non Antibodies
Product Type :
S. Molecules
Storage After Reconstitution :
The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.
Shipping and storage :
Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C
Product Page - Scientific background :
RQ 00203078 is a synthetic compound that acts as a potent and highly selective TRPM8 channel blocker with IC50 values of 8.3 nM and 5.8 nM for human and rat TRPM8 respectively. The compound shows very little inhibitory action against TRPV1, TRPA1, TRPV4 and TRPM2 channel. It is orally available and may be a useful tool for assessing the potential therapeutic use of TRPM81,2.TRPM8 is a Ca2+-permeable, nonselective cation channel that is activated by temperatures in the range of 8-28°C and by chemical agonists such as menthol and icilin. The channel is specifically expressed in temperature-sensing trigeminal and dorsal root ganglion neurons. TRPM8 gene is up-regulated in prostate cancer and other malignancies1,3.
Supplier :
Alomone Labs
Target :
TRPM8 channel
Long Description :
RQ 00203078 (#R-170) is a highly pure, synthetic, and biologically active compound.
Short Description :
A Potent and Selective Blocker of TRPM8 Channels
MW :
554.84
Source :
Synthetic
Molecular formula :
C21H13ClF6N2O5S.
Effective Concentration :
1 nM - 1 µM.
Activity :
RQ 00203078 is a potent and selective TRPM8 antagonist, shown to inhibit menthol-evoked human and rat TRPM8-mediated calcium influx with IC50 of 8.3 nM and 5.8 nM, respectively, while being highly selective over hTRPV4, h/rTRPV1, h/rTRPA1 and TRPM21,2.
Reconstitution and Solubility :
Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity
Solubility :
Up to 100 mM in DMSO. Centrifuge all products before use (10000 x g 5 min).
Storage of solutions :
Up to three months at -20°C.
Lead Time :
1-2 Business Days
Country of origin :
Israel/IL
Applications key :
Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.
Purity :
>99%
CAS No :
1254205-52-1
Form :
Lyophilized powder.
Comment :
Contact Alomone Labs for technical support and product customization
UNSPSC :
41116134
Bioassay Tested :
Yes
Chemical Name :
4-[[3-chloro-5-(trifluoromethyl)pyridin-2-yl]-[[4-(trifluoromethoxy)phenyl]methyl]sulfamoyl]benzoic acid.
more info or order :
company information
Alomone Labs
Jerusalem BioPark (JBP), Hadassah Ein Kerem
P.O. Box 4287
Jerusalem 9104201
info@alomone.com
http://www.alomone.com
972 2 531 8002
headquarters: Israel