A GPR75 antagonist
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AAA

Item No. 32733

Technical Information
Formal Name
(20-hydroxyicosa-6Z,15Z-dienoyl)aspartate, disodium salt
CAS Number
3055022-23-3
Molecular Formula
C24H39NO6 • 2Na
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMSO: Slightly solublePBS (pH 7.2): 1 mg/ml
SMILES
OCCCC/C=C\CCCCCCC/C=C\CCCCC(NC(C([O-])=O)CC([O-])=O)=O.[Na+].[Na+]
InChi Code
InChI=1S/C24H41NO6.2Na/c26-19-17-15-13-11-9-7-5-3-1-2-4-6-8-10-12-14-16-18-22(27)25-21(24(30)31)20-23(28)29;;/h8-11,21,26H,1-7,12-20H2,(H,25,27)(H,28,29)(H,30,31);;/q;2*+1/p-2/b10-8-,11-9-;;
InChi Key
JGVHCBALWPPEGB-UJJOPKMPSA-L
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    Product Description

    AAA is an antagonist of G protein-coupled receptor 75 (GPR75).1 It increases basal GPR75 protein levels and inhibits 20-HETE-induced reductions in GPR75 protein levels in PC3 cells. AAA (5 and 10 µM) also reduces 20-HETE-induced phosphorylation of EGFR, NF-κB, and Akt in, and cell migration of, PC3 cells. In vivo, AAA (10 mg/kg per day) reduces systolic blood pressure, albuminuria, renal angiotensin II levels, and cardiac hypertrophy in a Cyp1a1-Ren-2 transgenic rat model of malignant hypertension when administered prior to induction or after establishment of hypertension.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Cárdenas, S., Colombero, C., Panelo, L., et alGPR75 receptor mediates 20-HETE-signaling and metastatic features of androgen-insensitive prostate cancer cells. Biochim. Biophys. Acta Mol. Cell Biol. Lipids 1865(2), 158573 (2020).

    2. Sedláková, L., Kikerlová, S., Husková, Z., et al20-Hydroxyeicosatetraenoic acid antagonist attenuates the development of malignant hypertension and reverses it once established: a study in Cyp1a1-Ren-2 transgenic rats. Biosci. Rep. 38(5), BSR20171496 (2018).