Dihydromunduletone - 10mM in DMSO , CAS No.674786-20-0

CAS: 674786-20-0 Cat. No.: D655745 分子式: C₂₅H₂₈O₆ 分子量: 424.49 PubChem CID: 3492326

GRADE & PURITY 10mM in DMSO

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

概要

Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) ( GPR56 and GPR114/ADGRG5 ) antagonist with an IC 50 of 20.9 μM for GPR56 , but not inhibit GPR110 or class A GPCRs

In Vitro

Assays are initiated by the addition of [ 35 S]GTPγS, and the rates of aGPCR-stimulated G protein activation ([ 35 S]GTPγS binding to Gα) are measured with or without the influence of added compounds. Dihydromunduletone (DHM) inhibits the kinetics of GPR56 7TM-stimulated G13 GTPγS binding to varying degrees. Dihydromunduletone is the best inhibitory compound and reduced the rate at which GPR56 7TM activated G13 >75% (from 0.18 to 0.04 minute −1 ). At a concentration of Dihydromunduletone (DHM) that maximally inhibits GPR56 (50 μM), the rate of GPR114 7TM-stimulated Gs activity is also inhibited dramatically. When Dihydromunduletone (50 μM) is applied to the GPR110 7TM, it fails to inhibit GPR110 stimulation of Gq GTPγS binding. Cells transfected with GPR56 A386M 7TM are incubated with increasing concentrations of Dihydromunduletone. P7 peptide agonist is added, and SRE-luciferase activity is measured. Dihydromunduletone inhibits the P7 peptide-induced luciferase activity in a concentration-dependent manner. Cells are also treated with a fixed concentration of 3 µM Dihydromunduletone and then stimulated with an increasing concentration of P7 peptide agonist. Dihydromunduletone treatment blunts P7 peptide activation at each concentration. In conclusion, Dihydromunduletone antagonizes synthetic-peptide agonist and tethered-peptide agonist-mediated aGPCR activation in isolated membranes and HEK293T cell-based assays, but it does not inhibit basal receptor signaling. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

IC50& Target:IC50: 20.9 μM (GPR56), ,GPR114

Specifications

仕様と純度

10mM in DMSO

生化学的・生理学的メカニズム

Dihydromunduletone (DHM) is a rotenoid derivative and a selective, potent adhesion G protein-coupled receptor (aGPCR) ( GPR56 and GPR114/ADGRG5 ) antagonist with an IC 50 of 20.9 μM for GPR56 , but not inhibit GPR110 or class A GPCRs.

保管条件

Store at -80°C

入荷

Dry ice packs + Cold packs

この製品は冷冷この冷このこの製品の運送が必要です。地上およびその他の経済サービスは利用できません。

名前と識別子

異性体SMILES

CC1(C=CC2=C(O1)C=CC(=C2OC)CC(=O)C3=C(C=C4C(=C3)CC(C(O4)(C)C)O)O)C

代替CAS番号

674786-20-0

PubChem CID

3492326

MeSH用語

dihydromunduletone

分子量

424.49

よくある質問

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 674786-20-0, the molecular formula is C25H28O6, and the molecular weight is 424.49 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.