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Home / Biochemicals / Small Molecules

FR 139317

SKU : BHB21300139

A Selective Antagonist of Endothelin A Receptors

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Mfr.No.	F-180, F-180_10 mg, F-180_25 mg, F-180_5 mg, F-180_50 mg
Description	FR 139317 (#F-180) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C33H44N6O5.
Background	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.
Shipping	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
Concentration	1 nM - 1 uM.
Reconstitution	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 uM - 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
Cas Number	142375-60-8
Molecular Weight	604.75
Solubility	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Target	ET-A receptors
Source	Synthetic
Activity	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 uM, respectively1. in vitro, FR 139317 shifted Endothelin-1-induced contractile response curve to the right with pA2 of 7.2 in isolated rabbit aorta2.
Country Of Origin	Israel/IL
UNSPSC Code	41116134
Application	FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay
Lead Time	1-2 Business Days
Notes	Bioassay Tested: Yes Chemical Name: (2R)-2-(((2R)-2-(((2S)-2-(azepane-1-carbonylamino)-4-methylpentanoyl)amino)-3-(1-methylindol-3-yl)propanoyl)amino)-3-pyridin-2-ylpropanoic acid.

Purity	>99%
Form	Lyophilized powder.
Storage	Storage After Reconstitution: 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. Storage of solutions: Up to three months at -20°C.

Product Manual	SDS

Reference	Aramori, I. et al. (1993) Mol. Pharmacol. 43, 127. Peter, M.G. and Davenport, A.P. (1996) Br. J. Pharmacol. 117, 455. Takase, H. et al. (1995) Hypertension 25, 739. Aramori, I. et al. (1993) Mol. Pharmacol. 43, 127. Sogabe, K. et al. (1993) J. Pharmacol. Exp. Ther. 264, 1040.

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHB21300139-1	F-180_10 mg	10 mg	$254		Add to Cart
BHB21300139-2	F-180_25 mg	10 mg	$509		Add to Cart
BHB21300139-3	F-180_5 mg	5 mg	$168		Add to Cart
BHB21300139-4	F-180_50 mg	50 mg	$916		Add to Cart

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