>>Signaling Pathways>> GPCR/G protein>> ETA Receptors>>Asterric Acid

Asterric Acid (Synonyms: Dimethylosoic Acid,RES-1214-1,TAN 1415A)

Catalog No.GC16216

ETA receptor inhibitor

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Asterric Acid Chemical Structure

Cas No.: 577-64-0

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5mg
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Sample solution is provided at 25 µL, 10mM.

Description of Asterric Acid

IC50: 10 μM for ET-1 binding to the ETA receptor ofA10 cells

Asterric Acid is an ETA receptor inhibitor.

Endothelin (ET), a potent vasoconstrictor/pressor peptide consisting of 21 amino acid residues, was first isolated from the cultures of porcine aortic endothelial cells. Analyses of a human genomic library reveals three forms of ET (ET-1, ET-2 and ET-3) with more than 70% homology with one another. In various organs, high affinity and specific receptors for ET have been found, which have been classfied as receptors ETA and ETB. ET-1 has potent and long-lasting vasoconstrictive activity, as a result of binding to the ETA receptor.

In vitro: Previous study asterric acid isolated as an active substance from the culture filtrate of a fungus, Aspergillus sp. Asterric acid had also been reported as a metabolite of a fungus. It was found that asterric acid had the property of inhibiting ET-1 binding to the ETA receptor of A10 cells, but it showed no inhibitory activity against ANP and A II binding at 10 mM, which indicated that asterric acid displayed as a specific inhibitor of ET-1 binding [1].

In vivo: Up to now, there is no animal in vivo data reported.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[1] Ohashi, H. ,Akiyama, H.,Nishikori, K., et al. Asterric acid, a new endothelin binding inhibitor. Journal of Antibiotics 45, 1684-1685 (1992).

Chemical Properties of Asterric Acid

Cas No. 577-64-0 SDF
Synonyms Dimethylosoic Acid,RES-1214-1,TAN 1415A
Chemical Name 2-(2-carboxy-3-hydroxy-5-methylphenoxy)-5-hydroxy-3-methoxy-benzoic acid, 1-methyl ester
Canonical SMILES CC1=CC(O)=C(C(O)=O)C(OC2=C(OC)C=C(O)C=C2C(OC)=O)=C1
Formula C17H16O8 M.Wt 348.3
Solubility Soluble in ethanol;Soluble in DMSO;Soluble in dimethyl formamide Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Asterric Acid

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1 mg 5 mg 10 mg
1 mM 2.8711 mL 14.3554 mL 28.7109 mL
5 mM 0.5742 mL 2.8711 mL 5.7422 mL
10 mM 0.2871 mL 1.4355 mL 2.8711 mL
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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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3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 29 reference(s) in Google Scholar.)

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