| Field | Specification |
|---|---|
| Mfr No | |
| Activity | |
| Cas No. | |
| Concentration | |
| Form | Lyophilized |
| Formulation | |
| Gene ID | |
| Molecular Weight | |
| Product Type | |
| Purity | |
| Reconstitution | |
| 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 |
| Storage | |
| Target |
Overview
TAK-044 is a research-grade protein/peptide reagent (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) used in research settings. It is commonly applied as a tool reagent related to Endothelin receptors biology and/or assay development. It is supplied in Lyophilized format to support flexible downstream use in RUO workflows. Researchers commonly pair it with applications such as ETB assay, Calcium imaging assay.
Key elements and design rationale
- Molecular identity: CAS: 157380-72-8, MW: 927 Da, Formula: C45H51N9O11S.
- Source / origin: Synthetic peptide.
- Quality attributes: Purity: ≥98% (HPLC); Bioassay tested: Yes; Sterile / endotoxin-free: No.
Modifications
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.
When used as a biochemical or pharmacological tool, results are best interpreted relative to the experimental system (species, expression level, and assay readout) and with appropriate negative and competition-style controls where relevant. This product is intended for research use only.
Biological 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.
Research relevance and current trends
- Using high-specificity ligands, toxins, and engineered peptides to dissect closely related receptor/channel subtypes and signaling microdomains.
- Pairing labeled (e.g., fluorescent) proteins/peptides with advanced imaging to map surface expression, trafficking, and nanoscale organization.
- Increasing emphasis on reproducibility through standardized characterization (identity, purity, and lot QC) and transparent reporting of reagent attributes.
Common research applications
- ETB assay: commonly used to compare signal, binding, or functional readouts across conditions without implying a specific protocol.
- Calcium imaging assay: commonly used to compare signal, binding, or functional readouts across conditions without implying a specific protocol.
Across these use cases, changes in signal or functional readout are generally interpreted as evidence of differences in target abundance, accessibility, or engagement, but alternative explanations (matrix effects, off-target interactions, or assay artifacts) should be considered.
Notes for experimental interpretation
- Assay context matters: binding assays, functional modulation, and detection workflows can yield different readouts even for the same target system.
- Target complexity: closely related family members, splice variants, and post-translational modifications can influence apparent specificity and potency.
- Matrix and sample effects: buffer composition, detergents, and biological matrices may alter stability or apparent activity; interpret with appropriate controls.
- Control concepts: include negative controls and orthogonal validation (e.g., genetic perturbation or alternative reagents) to support robust interpretation.
Can’t Find What You’re Looking For? We can help you source the best match or customize a recombinant protein solution for your study. Options may include species (human/mouse/rat), protein region/domain (full-length vs fragment), tag or label (His/GST/FLAG/biotin/fluorescent), expression system (E. coli/HEK293/insect), purity grade, formulation (buffer, carrier-free, glycerol-free), activity/functional validation (binding or enzymatic assays), endotoxin level (low-endotoxin for cell-based work), mutants/variants (point mutations, isoforms), and bulk or custom packaging. Click Talk to a Scientist to submit a request form, email us at support@biohippo.com, or explore our Research Services for additional support. Our team will be in contact with you shortly.
Nakamichi, K.
et al. (1992) Biochem. Biophys. Res. Commun.182, 144.
Watanabe. T.
et al. (1995) Br. J. Pharmacol.114, 949.
Saeki, T.
et al. (1991) Biochem. Biophys. Res. Commun.179, 286.
Xie, C. and Wang, D.H.
(2009) Hypertension54, 1298.
