BQ-123 trifluoroacetate

Mfr.No.	B-186, B-186_10 mg, B-186_25 mg, B-186_5 mg, B-186_50 mg
Description	BQ-123 trifluoroacetate (#B-186) is a highly pure, synthetic, and biologically active compound.
Molecular Formula	C33H43F3N6O9.
Synonyms	Synthetic
Background	BQ-123 is a cyclic pentapeptide that acts as potent and selective antagonist of endothelin A (ET-A) receptors. BQ-123 exhibits a 1000-fold selectivity for ET-A receptors over ET-B receptors. It antagonizes endothelin-1 radioligand binding to ET-A and ET-B receptors with IC50 values of 22 nM and 18 uM, respectively1.Studies show that BQ-123 prevents production of TNF-alpha and IL-6 in skeletal muscle of LPS-treated rat and enhances antioxidant defense1,2.There are two subtypes of endothelin receptor: ET-A and ET-B. They are widely distributed in vascular and nonvascular tissues. ET-A receptors are predominantly expressed in peripheral tissues, especially in vascular smooth muscle where they mediate vasoconstriction. They are also detected in several regions of the brain. The ET-A receptor has high affinity for endothelin-1 and endothelin-2 and relatively low affinity for endothelin-3, while the ET-B receptor has high affinity for all endothelin isopeptides3.
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
Sequence	Cyclo (D-trp-D-asp-L-pro-D-val-L-leu).
Concentration	10 nM - 10 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 (50 uM - 1 mM). For long-term storage in solution, we recommend preparing a stock solution by dissolving the product in sterile water 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	136553-81-6
Molecular Weight	724.74
Modifications	Supplied as trifluoroacetate salt.
Solubility	Soluble in DMSO. Centrifuge all products before use (10000 x g 5 min).
Target	ET-A receptors
Activity	BQ-123, a cyclic peptide, is a potent and selective antagonist of ET-A endothelin receptors, exhibiting a 1000-fold selectivity for ET-A over ET-B receptors (inhibiting endothelin-1 radioligand binding to ET-A and ET-B with IC50 of 22 nM and 18 uM, respectively). In vitro, BQ-123 inhibits endothelin-1 induced contractions of porcine coronary artery with KB of 40 nM1.
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: 2-((3R,6R,9S,12R,15S)-6-(1H-indol-3-ylmethyl)-9-(2-methylpropyl)-2,5,8,11,14-pentaoxo-12-propan-2-yl-1,4,7,10,13-pentazabicyclo(13.3.0)octadecan-3-yl) trifluoroacetate.

Purity	>98%
Form	Lyophilized powder.
Storage	Storage After Reconstitution: Store the reconstituted solution for the shortest time possible at -20°C. We do not recommend storing the product in working solution for longer than one day. Avoid multiple freeze-thaw cycles. Storage before Reconstitution: The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture. Storage of solutions: Up to three months at -20°C.

Product Manual	SDS

Reference	Moreland, S. (1994) Cardiovasc. Ther. 12, 48. Kowalczyk, A. et al. (2016) Oxid. Med. Cell Longev. 2016, 2356853. Saeki, T. et al. (1991) Biochem. Biophys. Res. Commun. 179, 286. Moreland, S. (1994) Cardiovasc. Ther. 12, 48.

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Combination SKU	Supplier No.	Size	Your price
BHB21300063-1	B-186_10 mg	10 mg	$337	Add to Cart
BHB21300063-2	B-186_25 mg	25 mg	$588	Add to Cart
BHB21300063-3	B-186_5 mg	5 mg	$235	Add to Cart
BHB21300063-4	B-186_50 mg	50 mg	$808	Add to Cart

BQ-123 trifluoroacetate

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