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Home / Proteins & Peptide / Proteins

TAK-044

SKU : BHP21300118

A Non-Selective Antagonist of Endothelin Receptors

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Alomone Labs

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Mfr.No.	SPE-320, SPE-320_10 mg, SPE-320_25 mg, SPE-320_5 mg
Description	A Non-Selective Antagonist of Endothelin Receptors
Reconstitution	Centrifuge the vial (10,000 x g for 5 minutes) before adding solvent 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. Gently tap, tilt, and roll the vial to aid dissolution. Avoid vigorous vortexing; light vortexing for up to 3 seconds is acceptable if needed. Soluble in DMSO. Prepare a concentrated stock solution by dissolving the lyophilized peptide in DMSO first (e.g., at a concentration between 100-1000x of the final working concentration). Once the peptide is completely dissolved in DMSO, slowly dilute the solution into the working buffer (or water) to the desired final working concentration. Centrifuge all product preparations before use. Avoid multiple freeze-thaw cycles to maintain biological activity. It is recommended to keep the DMSO concentration as low as possible. For cell assays, a final concentration of 0.1%0.5% DMSO (v/v) is considered safe. For other experiments, a 5% DMSO (v/v) concentration is recommended.
Molecular Formula	C45H51N9O11S
Background	TAK-044 is a synthetic peptide that acts as a non-selective ET-B (endothelin B) and ET-A (endothelin A) receptor antagonist, receptors that belong to the G-protein coupled receptor (GPCR) superfamily. In a study conducted on rats the compound showed high inhibitory effects on the extension of myocardial infarct size after coronary artery occlusion-reperfusion1. TAK-044 inhibits radiolabelled ET-1 binding from the rabbit ventricular and cerebellar preparation with an IC50 value of 3.8 nM and 130 nM, respectively1.Endothelin receptors include two subtypes: ET-A and ET-B. ET-A receptors are predominantly detected in peripheral tissues, especially in vascular smooth muscle tissues to mediate vasoconstriction. They are also present in several regions of the brain. ET-B receptors play an important role in regulating renal function and blood pressure and are expressed in sensory nerves. They are mainly present in medium- and large-sized cell bodies of human trigeminal ganglia2,3.
Biological Activity	TAK-044 is a non-selective endothelin receptor antagonist1.
Formulation	Lyophilized Powder.
Molecular Weight	927 Da
Solubility	Centrifuge the vial before adding solvent (10,000 x g for 5 minutes). The lyophilizate 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. Soluble in DMSO. Prepare a concentrated stock solution by dissolving the lyophilized peptide in DMSO first (e.g., at a concentration between 100-1000x of the final working concentration). Once the peptide is completely dissolved in DMSO, slowly dilute the solution into the working buffer (or water) to the desired final working concentration. Centrifuge all product preparations before use. It is recommended to keep the DMSO concentration as low as possible. For cell assays, a final concentration of 0.1%0.5% DMSO (v/v) is considered safe. For other experiments, a 5% DMSO (v/v) concentration is recommended.
Source	Synthetic peptide
Concentration	0.5 - 1 uM
Form	Lyophilized
Notes	Bioassay Tested: yes Steril endotoxin free: no Chemical Name: 2-[(2R,5S,8S,11S,14S,17R)-8-(carboxymethyl)-17-(1H-indol-3-ylmethyl)-14-(2-methylpropyl)-3,6,9,12,15,18-hexaoxo-5-[2-oxo-2-(4-phenylpiperidin-1-yl)ethyl
Cas Number	157380-72-8
UNSPSC Code	12352202
Lead Time	1-2 Business Days
Modifications	X = D-(2-thienyl)glycine Tryptophan and aspartic acid-4 are in the D-isomer. Aspartic acid-2 is modified with the group alpha-amino-gamma-oxo-4-phenyl-1-piperazinebutanoyl.

Gene Id	EDNRA, EDNRB
Sequence	DDDXLWS-OH
Target	Endothelin receptors

Country Of Origin	Israel/IL
Purity	>=98% (HPLC)
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: Store the reconstituted solution at -20°C for the shortest time possible. Avoid multiple freeze-thaw cycles. We do not recommend storing the product in working solutions for longer than a day.

Applications	ETB assay, Calcium imaging assay

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Combination SKU	Supplier No.	Size	Your price	Quantity
BHP21300118-1	SPE-320_10 mg	10 mg	$459		Add to Cart
BHP21300118-2	SPE-320_25 mg	25 mg	$912		Add to Cart
BHP21300118-3	SPE-320_5 mg	5 mg	$287		Add to Cart

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