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TZA-2 TZ Peptide Analog

TZA-2 TZ Peptide Analog

Research use only. Laboratory and investigational purposes — not for human or animal consumption.

Net quantity

15 mg 40 mg 60 mg

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FOR RESEARCH USE ONLY — Molecular Research Profile

TZA-2 TZ — Molecular Research Profile

TZA-2 TZ is a synthetic peptide analog designed for dual-receptor engagement of the glucose-dependent insulinotropic polypeptide receptor (GIPR; UniProt P48546) and glucagon-like peptide-1 receptor (GLP-1R; UniProt P43220), incorporating a fatty-acid acylation chain to extend apparent half-life in cell-culture media and backbone modifications conferring measurable resistance to dipeptidyl peptidase-4 (DPP-IV) in cell-free enzymatic assays.

Molecular Architecture

Backbone
GIP-derived peptide scaffold with position-specific substitutions to modulate dual GIPR/GLP-1R engagement; single molecular entity confirmed by HPLC-MS at ≥99%
Lipidation
C20 fatty diacid conjugated via γGlu linker at a specified lysine residue; enables albumin-binding in serum assay matrices (class Kd ~1–10 µM for acyl-HSA interactions)
Molecular weight
~4,700–4,900 Da (linker-configuration dependent); confirmed by ESI-MS at expected m/z
Secondary structure
N-terminal amphipathic α-helix (residues 1–~15) consistent with Class B1 GPCR engagement model; no disulfide bonds
Modifications
C-terminal –NH₂ amide; DPP-IV–resistant N-terminal substitutions; acyl chain for albumin-mediated diffusion retardation in serum matrices

Receptor Binding and Signaling Mechanics

TZA-2 TZ is characterized in dual-receptor assay formats against GIPR and GLP-1R, both Class B1 (secretin-family) GPCRs. The binding mechanism follows the two-domain model: the N-terminal peptide segment docks to the receptor extracellular domain (ECD) while the C-terminal helix engages the transmembrane bundle. In published dual-agonist pharmacophore work, GIPR engagement drives full cAMP accumulation while GLP-1R engagement may show partial agonism relative to native GLP-1(7-36)NH₂ in transfected cell assays — a profile researchers use to separate GIPR-dominant from GLP-1R-dominant signaling in the same compound.

Intracellular signaling cascade:

  1. GIPR activation → Gαs dissociation → adenylyl cyclase (AC) stimulation → cAMP ↑ (HTRF cAMP assay in GIPR-overexpressing CHO or HEK293)
  2. GLP-1R activation → Gαs → AC → cAMP ↑ (same assay format in GLP-1R transfectants; compare Emax vs. native GLP-1 reference)
  3. cAMP → PKA holoenzyme dissociation → CREB Ser133 phosphorylation
  4. β-arrestin-2 recruitment measurable by BRET or PathHunter split-enzyme assay at each receptor individually
  5. Run GIPR and GLP-1R assays in separate wells — do not infer dual-receptor potency from a single-receptor plate

In Vitro Research Profile

Primary assay
cAMP accumulation in GIPR- and GLP-1R-overexpressing CHO-K1 or HEK293 cells run as separate receptor panels; HTRF or AlphaScreen cAMP kit; 30-min stimulation at 37°C
Secondary assay
β-arrestin-2 recruitment via BRET in U2OS cells transfected with individual receptor constructs; characterizes biased agonism vs. native GIP or GLP-1 reference agonists
Reference agonists
GIP(1-42) or GIP(1-30)NH₂ (GIPR); GLP-1(7-36)NH₂ (GLP-1R); include in every dose-response run
Concentration range
0.01–100 nM for full dose-response at each receptor; vehicle DMSO ≤0.1% v/v in assay wells
Stability (PBS)
Assess by RP-HPLC (C18 column) at 0, 4, 24, 72 h at 37°C in PBS pH 7.4; acylation extends apparent half-life in 50% human serum relative to unmodified peptide in peptidase assay
Known limitations
Published EC50 data specific to TZA-2 TZ formulation not yet in indexed literature; researchers should run full concentration-response at GIPR and GLP-1R separately in their certified cell lines

Research Use Only — Regulatory Notice

All compounds on this page are sold exclusively for in vitro laboratory research. They are not approved by the FDA, DEA, or any regulatory agency for human or animal use, therapeutic application, clinical investigation, or consumption of any kind. Binding affinities, IC50/EC50 values, and signaling cascade descriptions referenced herein derive from published in vitro and cell-based literature and do not constitute efficacy or safety claims. Researchers are responsible for complying with all applicable institutional, local, and federal regulations governing the handling and use of research chemicals.

Batch specifications

Compound
TZA-2 TZ Peptide Analog
Net quantity
60 mg
Form
Lyophilized powder
HPLC purity
≥99%
Current lot
DP-TZA2-060
Testing panel
HPLC · Mass Spec · LAL Endotoxin
Storage
2–8°C, protected from light

Lot Documentation & Testing

Each lot is tested by HPLC (purity), mass spectrometry (identity confirmation), and LAL endotoxin assay prior to release. COA documentation is pending finalization — lot number is reserved and testing is underway. QR-linked COA will be published to the vial and the COA library when the batch is released.

Description

FOR RESEARCH USE ONLY. Not for human consumption, medical use, or therapeutic application of any kind.

A synthetic peptide analog studied in vitro as a dual agonist of the GIP receptor (GIPR) and glucagon-like peptide-1 receptor (GLP-1R). In cell-based assays using lines recombinantly expressing GIPR or GLP-1R, it has been characterized for stimulation of cAMP accumulation at each receptor, with published dual-agonist work examining relative potency across these in vitro systems.

Research Specifications

  • Purity: 99%+ (HPLC — Freedom Diagnostics)
  • Testing: HPLC · Mass Spectrometry · LAL Endotoxin
  • Form: Lyophilized powder
  • Storage: 2–8°C, protected from light

Why Researchers Choose This Catalog

  • Third-party verified purity — every batch, not sampled
  • Mass spectrometry confirmation of identity
  • Endotoxin-screened (LAL method)
  • QR code on each vial will link to the published Freedom Diagnostics certificate when the batch COA is released
  • Lot-numbered inventory with corresponding batch documentation
FOR RESEARCH USE ONLY — NOT FOR HUMAN CONSUMPTION

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