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Cat.No.S8185
| Cell Lines | Assay Type | Concentration | Incubation Time | Formulation | Activity Description | PMID |
|---|---|---|---|---|---|---|
| CHO | Function assay | Displacement of [I125]amyloid beta (1 to 40) from human RAGE domain V expressed in CHO cells, Ki=0.025μM | 28482155 | |||
| CHO | Function assay | Inhibition of HMGB1 binding to human RAGE domain V expressed in CHO cells, Ki=0.148μM | 28482155 | |||
| CHO | Function assay | Inhibition of S110B binding to human RAGE domain V expressed in CHO cells, Ki=0.23μM | 28482155 | |||
| Click to View More Cell Line Experimental Data | ||||||
|
In vitro |
DMSO
: 66 mg/mL
(201.31 mM)
Ethanol : 66 mg/mL Water : Insoluble |
|
In vivo |
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Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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| Molecular Weight | 327.85 | Formula | C20H22ClNO |
Storage (From the date of receipt) | |
|---|---|---|---|---|---|
| CAS No. | 945714-67-0 | Download SDF | Storage of Stock Solutions |
|
|
| Synonyms | N/A | Smiles | C1CCC(CC1)N(CC2=CC=CC=C2)C(=O)C3=CC=C(C=C3)Cl | ||
| Targets/IC50/Ki |
RAGE
|
|---|---|
| In vitro |
FPS-ZM1 blocks Aβ binding to the V domain of RAGE and inhibited Aβ40- and Aβ42-induced cellular stress in RAGE-expressing cells in vitro. It blocks binding of other ligands to RAGE as well, such as S100B, AGE, and HMGB1, which have been suggested to contribute to RAGE-mediated long-term tissue damage in models of diabetes, immune/inflammatory disorders, and AD.
|
| In vivo |
FPS-ZM1 is nontoxic to mice and readily crossed the blood-brain barrier (BBB). It effectively controls progression of an Aβ-mediated brain disorder and the related neurovascular and cognitive dysfunction in 17-month-old APPsw/0 mice with fully developed Aβ and amyloid pathology by blocking RAGE actions at the BBB and in brain. Also, this compound blocks RAGE-dependent BACE1 expression and activity in brain of 17-month-old APPsw/0 mice.
|
References |
| Methods | Biomarkers | Images | PMID |
|---|---|---|---|
| Immunofluorescence | AGE-2 / AGEE-3 cathepsin B Caspase-1 |
|
29430285 |
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