Cart
sales@molnova.com
Philanthotoxin 74 dihydrochloride
CAS No. 1227301-51-0
Philanthotoxin 74 dihydrochloride( PhTx 74 dihydrochloride | PhTx-74 HCl )
Catalog No. M26786 CAS No. 1227301-51-0
Philanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 134 | Get Quote |
|
| 100MG | Get Quote | Get Quote |
|
| 200MG | Get Quote | Get Quote |
|
| 500MG | Get Quote | Get Quote |
|
| 1G | Get Quote | Get Quote |
|
Biological Information
-
Product NamePhilanthotoxin 74 dihydrochloride
-
NoteResearch use only, not for human use.
-
Brief DescriptionPhilanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.
-
DescriptionPhilanthotoxin 74 dihydrochloride is an antagonist of AMPAR with IC50s of 263 and 296 nM for GluR3 and GluR1.(In Vitro):Philanthotoxin 74 dihydrochloride inhibits the two major subtypes of GluA2R-containing AMPARs, GluA1/A2R and GluA2R/A3 in the micromolar concentration range, when these are coexpressed with γ-2 in oocytes. Philanthotoxin 74 dihydrochloride (500 μM) fully inhibits GluA1/A2R receptors and produces 10% inhibition at GluA2R/A3 receptors. Philanthotoxin 74 dihydrochloride (100 and 500 μM) displays a pronounced channel block (> 80%) of GluA1/A2R but minimal block (less than 10%) of GluA2R/A3. Philanthotoxin 74 dihydrochloride inhibits these receptors nonselectively, with IC50 values of about 30 μM, in both the presence and absence of γ-2.
-
In VitroPhilanthotoxin 74 in the micromolar concentration range displays selective inhibition between the two major subtypes of GluA2R-containing AMPARs, GluA1/A2R and GluA2R/A3, when these are coexpressed with γ-2 in oocytes. Philanthotoxin 74 is reported to fully inhibit GluA1/A2R receptors when applied at a concentration of 500 μM while producing 10% inhibition at GluA2R/A3 receptors. Philanthotoxin 74, when tested at concentrations of 100 and 500 μM, displays pronounced channel block (more than 80%) of GluA1/A2R but minimal block (less than 10%) of GluA2R/A3. Oocytes expressing GluA2R alone that homomeric GluA2R is virtually inert to philanthotoxin 74 in the 0.1-300 μM concentration range, displaying less than 5% inhibition at the maximum tested concentration of 300 μM. Philanthotoxin 74 inhibits these receptors nonselectively, with IC50 values of about 30 μM, in both the presence and absence of γ-2.
-
In Vivo——
-
SynonymsPhTx 74 dihydrochloride | PhTx-74 HCl
-
PathwayNeuroscience
-
TargetGluR
-
Recptor——
-
Research Area——
-
Indication——
Chemical Information
-
CAS Number1227301-51-0
-
Formula Weight507.54
-
Molecular FormulaC24H44Cl2N4O3
-
Purity>98% (HPLC)
-
SolubilityIn Vitro:?DMSO : 100 mg/mL (197.03 mM)
-
SMILESOC(C=C1)=CC=C1C[C@H](NC(CCC)=O)C(NCCCCCCCNCCCCN)=O.Cl.Cl
-
Chemical Name——
Shipping & Storage Information
-
Storage(-20℃)
-
ShippingWith Ice Pack
-
Stability≥ 2 years
Reference
-
(S)-MCPG
(S)-MCPG ((+)-MCPG) is a class I/II metabotropic glutamate receptors (mGluRs) antagonist that blocks spatial learning and long-term enhancement of the dentate gyrus in vivo in rats, and can be used to study neurological disorders.
-
Valiglurax
Valiglurax (VU2957), also known as VU0652957 and VU2957, is a potent, selective, CNS penetrant, and orally bioavailable mGlu4 PAM. VU2957 possessed attractive in vitro and in vivo pharmacological and DMPK properties across species.
-
Basimglurant
Basimglurant is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM). In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation (IC50 of 5.9 nM).
