chemical

FR 139317

F-180

F-180_10 mg

FR 139317

Non Antibodies

S. Molecules

https://www.uniprot.org/uniprotkb/P0C1Z0/entry

The reconstituted solution can be stored at 4°C for up to 1 week. For longer periods (up to 6 months), small aliquots should be stored at -20°C. We do not recommend storing the product in working solutions for longer than a few days. Avoid multiple freeze-thaw cycles.

Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C

FR 139317 is a synthetic linear tripeptide that acts as a potent, competitive and highly selective antagonist of endothelin A (ET-A) receptors. FR 139317 can be used as a useful tool to investigate the physiological properties of ET-A receptor and to explore its role in diseases1,2. FR139317 inhibits the specific binding of radio labeled endothelin 1 to porcine aortic microsomes in a concentration-dependent, monophasic manner with an IC50 value of 0.53 nM2.Endothelin receptors include two subtypes: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. The ET-A receptor has a high specificity towards endothelin-1 and endothelin-2. It is expressed in vascular smooth muscle cells and mediates vasoconstriction3.

Alomone Labs

ET-A receptors

FR 139317 (#F-180) is a highly pure, synthetic, and biologically active compound.

A Selective Antagonist of Endothelin A Receptors

604.75

Synthetic

C33H44N6O5.

1 nM - 1 µM.

FR 139317 is a potent and selective antagonist of ET-A receptors, inhibiting Endothelin-1 radioligand binding to ET-A and ET-B with Ki of 1 nM and 7.3 µM, respectively1. in vitro, FR 139317 shifted Endothelin-1-induced contractile response curve to the right with pA2 of 7.2 in isolated rabbit aorta2.

Centrifuge the vial before adding solvent (10,000 x g for 5 minutes) to spin down all the powder to the bottom of the vial. The lyophilized product may be difficult to visualize. Add solvent directly to the centrifuged vial. Tap the vial to aid in dissolving the lyophilized product. Tilt and gently roll the liquid over the walls of the vial. Avoid vigorous vortexing. Light vortexing for up to 3 seconds is acceptable if needed. The product is soluble in pure water at high micromolar concentrations (100 µM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in double-distilled water (ddH2O) at a concentration between 100-1000x of the final working concentration. Divide the stock solution into small aliquots and store at -20°C. Before use, thaw the relevant vial(s) and dilute to the desired working concentration in your working buffer. Centrifuge all product preparations before use. It is recommended to prepare fresh solutions in working buffers just before use. Avoid multiple freeze-thaw cycles to maintain biological activity

Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).

Up to three months at -20°C.

1-2 Business Days

Israel/IL

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

>99%

142375-60-8

Lyophilized powder.

Contact Alomone Labs for technical support and product customization

41116134

Yes

(2R)-2-[[(2R)-2-[[(2S)-2-(azepane-1-carbonylamino)-4-methylpentanoyl]amino]-3-(1-methylindol-3-yl)propanoyl]amino]-3-pyridin-2-ylpropanoic acid.