chemical

TAK-044

SPE-320

SPE-320_10 mg

TAK-044

Non Antibodies

Proteins

ETB assay / Calcium imaging assay

Lyophilized Powder.

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.

Centrifuge the vial (10,000 × 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.

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.

The product is shipped as a lyophilized powder at room temperature. Upon receipt, store the product at -20°C. Protect from moisture.

Synthetic peptide

EDNRA, EDNRB

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.

Alomone Labs

Endothelin receptors

A Non-Selective Antagonist of Endothelin Receptors

A Non-Selective Antagonist of Endothelin Receptors

927 Da

X = D-(2-thienyl)glycine Tryptophan and aspartic acid-4 are in the D-isomer. Aspartic acid-2 is modified with the group α-amino-γ-oxo-4-phenyl-1-piperazinebutanoyl.

C45H51N9O11S

0.5 - 1 µM

TAK-044 is a non-selective endothelin receptor antagonist1.

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.

1-2 Business Days

Israel/IL

≥98% (HPLC)

157380-72-8

Lyophilized

Contact Alomone Labs for technical support and product customization

DDDXLWS-OH

No

12352202

yes

no

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]-11-thiophen-2-yl-1,4,7,10,13,16-hexazacyclooctadec-2-yl]acetic acid