Login / Register Order My Items
Contact Us
800.227.0627
Contact Us Quote Order Login / Register

Peptidomimetics Synthesis Service

Backbone-modified and constrained peptidomimetics, peptoids/foldamers, functional handles, purification, QC & COA, and scale-up—backed by 45+ years of peptide manufacturing expertise.

Custom peptidomimetic peptide synthesis with scale-aware route design, purification strategy, and analytical control.

Request a Quote Talk to a chemist
Overview Capabilities at a glance Vs modified peptides Options Strategy guide Quote specs QC Scale-up Contact

Overview: Peptidomimetics synthesis

Peptidomimetics are engineered molecules designed to reproduce the binding and biological function of peptides while overcoming key limitations of native sequences—most notably protease instability, short half-life, and insufficient conformational control. Because small structural changes can generate closely related impurities or isomers, successful peptidomimetics synthesis requires deliberate route selection, purification strategy, and analytical planning.

Bio-Synthesis delivers custom peptidomimetic peptide synthesis backed by more than 45 years of peptide manufacturing experience. We focus on chemistries that remain robust and reproducible across development stages—from early feasibility through multi-gram supply—rather than one-off, definition-level builds.

Large scale ready N-methylation Macrocycles Constraints Peptoids / foldamers ISO 90001:2015 / ISO 13485:2016 45+ Years of Expertise U.S. Facilities (Texas)
Why choose Bio-Synthesis
  • 45+ years of peptide and modified-peptide manufacturing expertise
  • Manufacturing-first design: route, purification, and analytics planned together
  • Scale-aware execution: mg feasibility through multi-gram production
  • Close-variant control: analytics selected for isomers and related impurities
  • COA with every lot and documentation options for regulated planning
What “click-ready” means in practice

Most scale issues trace back to route choices that work once at mg scale but break under higher loading or tighter impurity control.

  • Route discipline: chemistries chosen for reproducibility and purification compatibility
  • Behavior-first controls: aggregation/solubility handled early, not at the end
  • Purification stability: methods selected to hold resolution as load increases
  • Documentation options: RUO through regulated planning
Best fit: discovery & SAR programs, lead optimization, tool compounds, and projects that anticipate tighter specifications or future scale-up.

Related: Peptide Modifications, Macrocyclic Peptides, Stapled Peptides, Click Chemistry Peptides. If your sequence is challenging, see difficult peptide synthesis.

Capabilities at a glance

Click chemistry vs other conjugation methods

Fast-scanning matrix for buyers. If you’re unsure which option fits your goal, jump to Strategy guide or send your sequence/structure for feasibility review.

Capability What we offer Best fit for Notes (scale & QC)
Peptoids
N-substituted glycine oligomers Hybrid designs
Protease stability, scaffold exploration Routes and analytics selected to control close analogs and maintain reproducibility at higher loads.
Macrocycles
Head-to-tail Side-chain Conformational bias
Potency, selectivity, PPI targeting Constraint chemistry drives impurity profile; we plan purification to hold resolution during scale-up.
N-methylation
Site-defined N-methyl Non-natural residues
Stability; permeability optimization (project-dependent) We design routes to minimize closely related variants and verify identity with appropriate MS/HPLC.
Constraints
Lactam Thioether Disulfide Staples/bridges*
Conformational control, potency *Project-dependent; feasibility and analytics confirmed during review.
Functional handles
Azide/Alkyne DBCO/BCN Biotin Fluorophores Isotopes
Assays, conjugation, standards Handle placement is verified by LC–MS; QC can be aligned to downstream conjugation success.

Need click-ready handles? See Click Chemistry Peptides.

Peptidomimetics vs modified peptides

Modified peptide (typical)

Standard peptide backbone with targeted changes for function, labeling, or stability.

  • Labels/handles (azide/alkyne, dyes, biotin), linkers
  • Selected non-natural residues or terminal caps
  • Simple cyclization or disulfides
Peptidomimetic (typical)

Engineered to preserve activity while deliberately changing structure for drug-like performance.

  • Backbone edits (e.g., site-defined N-methylation; project-dependent isosteres)
  • Conformational constraints (macrocycles, staples/bridges)
  • Alternative scaffolds (peptoids, β-peptides, hybrid backbones)
Practical rule: if the design increases synthetic or purification complexity enough to affect lot-to-lot reproducibility or scale-up, treat it as a peptidomimetic program and plan route + analytics accordingly.

Designed for reproducibility and scale

Manufacturing-first, not definition-first

We plan route, purification, and analytics together—so the design remains reproducible and scalable beyond a first-pass mg batch.

Decision logic (property-first)

We match the peptidomimetic approach to the dominant limitation (stability, conformation, selectivity, scale) to reduce rework and delays.

QC aligned to close variants

Peptidomimetics often generate close analogs/isomers. We select analytics to distinguish these and support consistent lot release.

Note: Many vendors can “make peptidomimetics.” The differentiator is whether the route and purification strategy are engineered to hold performance as specifications tighten and scale increases.

Peptidomimetic options we provide

Expand each category to see representative classes, typical design goals, and best-fit use cases.

Backbone-modified peptides stability / conformation
Best fit: stability Also used: permeability (project-dependent) Scale-aware routes

Backbone modification can reduce protease susceptibility and bias conformational preference. We plan routes and analytics to control closely related variants.

  • Site-defined N-methylation
  • Non-natural amino acids (D-amino acids, bulky/functional residues)
  • Backbone disruption / turn-inducers (project-dependent)
  • Selected amide isosteres (project-dependent; feasibility-driven)
Constrained peptidomimetics potency / selectivity
Best fit: conformational control Macrocycles PPI targeting

Constraints stabilize bioactive shape and can improve potency/selectivity. The constraint chemistry drives impurity profile and scale-up robustness.

  • Head-to-tail cyclization
  • Side-chain cyclization (lactam, thioether, disulfide)
  • Stapled/bridged architectures (project-dependent)
  • Macrocyclic designs for conformational bias
Peptoids & foldamer-like scaffolds alternate backbones
Peptoids β-peptides (project-dependent) Hybrid designs

Alternative backbones can improve stability and tune structure. We align synthesis and purification to your performance goals and scale expectations.

  • Peptoids (N-substituted glycine oligomers)
  • β-peptides (project-dependent; feasibility-driven)
  • Hybrid backbones (mixed peptide/peptoid regions)
Functional handles & labeling (optional) assays / conjugation
Azide/alkyne DBCO/BCN Biotin / dyes / isotopes

Handles can be incorporated at defined sites to support downstream conjugation, imaging, or quantitation. If conjugation success is critical, we align QC to the intended chemistry.

  • Click-ready: azide, alkyne, DBCO, BCN
  • Labels: biotin, fluorophores, isotopes
  • Linkers: cleavable and non-cleavable (project-dependent)

Strategy guide (fast decisions)

Successful peptidomimetics design is driven by the dominant limitation of the native peptide. We select strategies using a property-first framework:

  • Protease instability: backbone modification, non-natural residues, site-defined N-methylation
  • Loss of bioactive conformation: cyclization, macrocyclization, side-chain constraints
  • Selectivity/potency limitations: conformational control and scaffold refinement
  • Future scale requirements: routes and purification methods compatible with increased batch size
Manufacturing reality: peptidomimetics synthesis is not only a design challenge—it is a manufacturing challenge. We focus on approaches that succeed beyond the first batch.

QC & typical deliverables

Standard QC
  • Analytical HPLC/UPLC purity profile
  • Identity confirmation (LC–MS)
  • Certificate of Analysis (COA)
Scale-ready controls
  • Analytics chosen for close variants / isomers
  • Purification approach that holds under higher loading
  • Method notes to support repeat lots
Optional add-ons

Project-dependent add-ons can be aligned to your analytical needs.

  • HRMS (as needed)
  • Aliquoting / formulation preferences
  • Documentation options for regulated planning

Large-scale peptidomimetics production

How we scale without surprises
  • Route discipline: reproducible chemistries, scale-compatible steps
  • Purification stability: methods that hold resolution under higher loading
  • Behavior-first controls: aggregation/solubility addressed early
  • Lot-to-lot consistency: controlled parameters documented

Example (anonymized): a constrained peptidomimetic progressed from a first-pass mg feasibility batch to multi-gram supply by locking the constraint-formation step early and selecting a purification method that held resolution under higher loading.

Scale questions we answer upfront
  • Which salt/form supports shipping, storage, and downstream use?
  • How do we keep yield stable as the batch grows?
  • What impurities become critical as specs tighten?
  • What documentation level matches RUO vs regulated planning?

For broader manufacturing workflows, see Large-Scale Peptide Synthesis.

Quote specifications

For the fastest quote, send the items below. We’ll respond with feasibility notes, a recommended strategy, QC options, and pricing.

Required
  • Sequence or structure (drawing or description)
  • Constraints (cyclization/staple/bridge details)
  • Quantity and purity target
  • Salt/form preference (or ask us to recommend)
Recommended
  • Intended use (screening vs in vivo vs standards)
  • Solubility or formulation constraints
  • Handle/label requirements (click, dye, isotope)
  • Scale plan (if multi-gram is likely later)

FAQ

What is a peptidomimetic?

A peptidomimetic is engineered to reproduce a peptide’s binding/function while improving stability, half-life, and conformational control using non-natural residues, backbone edits, and constraints (e.g., macrocyclization).

Are peptidomimetics harder to synthesize than peptides?

Often yes. Backbone edits/constraints increase steric and purification complexity, and can create closely related variants. Route planning + analytics are key.

What causes most peptidomimetic synthesis failures?

Aggregation, solubility limits during workup/purification, and close impurity profiles (including isomers), especially when scale increases without early planning.

Can you incorporate site-defined N-methylation?

Yes. Share target positions and goals (stability vs permeability). We plan chemistry and QC to minimize close variants and confirm identity by LC–MS/HPLC.

Do you make macrocyclic peptidomimetics?

Yes. Head-to-tail and side-chain cyclization are supported (project-dependent). We design purification to maintain resolution as loading increases.

Do you synthesize peptoids?

Yes—peptoids (N-substituted glycine oligomers) and hybrid backbones are supported with route and analytics planning for reproducibility.

Can you add click-ready handles (azide/alkyne, DBCO/BCN)?

Yes. We install handles at defined sites and verify by LC–MS. QC can be aligned to downstream conjugation performance.

Can you scale peptidomimetics to multi-gram supply?

Yes. We use scale-aware routes and purification approaches designed to remain robust as batch size increases, with documentation options for regulated planning.

How do you control closely related impurities or isomers?

Peptidomimetics often generate closely related analogs or stereochemical variants. We select synthesis routes, purification methods, and analytical techniques specifically to resolve and monitor these species, and align QC criteria to lot-to-lot reproducibility rather than single-batch success.

More FAQ'sAll FAQ's

Contact & quote request

For the fastest quote, send your sequence/structure, constraint details, quantity/purity, intended use, and any analytical or documentation requirements.

Fastest path
Request a Quote Copy quote specs

What happens next: Our technical team reviews your request and replies with a recommended strategy, feasibility notes, and a synthesis/QC plan aligned to your goals and scale expectations.

Fast quote checklist
  • Sequence/structure + modifications
  • Constraints (macrocycle/staple/bridge) and positions
  • Quantity & purity target
  • Intended use (screening / in vivo / standards)
  • Any handle/label requirements (optional)

Recommended reading (peptidomimetics & constraints)

Selected reviews and resources relevant to peptidomimetic design and synthesis.

Related: Macrocyclic Peptides, Stapled Peptides, Peptide Modifications, Ready-made catalog peptides.

Talk to a chemist Request a quote
Peptidomimetics Synthesis Service

Bio-Synthesis designs and synthesizes peptidomimetic peptides and related scaffolds, with scale-aware route selection, purification strategy, analytical QC, and COA—backed by 45+ years of peptide manufacturing expertise.

Related services

Macrocyclic Peptides
Stapled Peptides
Click Chemistry Peptides
Difficult Peptide Synthesis

Get a quote

Quote request form
sales@biosyn.com
+1-972-420-8505

Why Choose Bio-Synthesis

Trusted by biotech leaders worldwide for over 40+ years of delivering high quality, fast and scalable synthetic biology solutions.

Greetings Researchers,

Please be advised that any information, guidelines, writeups, and oral/video/graphic content on our website are intended solely as general guidelines.
It is the researcher's sole responsibility to conduct thorough research on the designs of the products intended for their experiments before submitting
their designs to Biosynthesis for review of production feasibility.
Thank you for your understanding.

Quick Links