Target Solvent
Bacteriostatic Water USP (0.9% Benzyl Alcohol)
Clear, colorless aqueous solution. Store strictly refrigerated at 2°C–8°C.
Validated Laboratory Standard
Revision 1 · Lyophilized Solid Powder
Central Melanocortin MC4R/MC1R Agonist Sexual Arousal & Libido Standard. Formulated for in-vitro research and laboratory analytical validation.
Central Melanocortin MC4R/MC1R Agonist Sexual Arousal & Libido Standard. Formulated for in-vitro research and laboratory analytical validation.
What it is: PT-141 (Bremelanotide) is a synthetic cyclic peptide derived from Melanotan II, specifically developed to treat sexual dysfunction without inducing skin pigmentation.
How it works: Unlike PDE5 inhibitors (like Viagra) that only act locally on blood vessels in the genitals, PT-141 acts centrally in the brain. It crosses the blood-brain barrier to bind to Melanocortin-4 Receptors (MC4R) in the medial preoptic area and hypothalamus, activating natural neural pathways of sexual desire, arousal, and motivation in both men and women.
Why researchers study it: Clinically approved and studied for hypoactive sexual desire disorder (HSDD) in premenopausal women, refractory erectile dysfunction in men, and boosting sexual intimacy.
An Authoritative Academic Monograph on PT-141 Structural Bio-Engineering, Nanomolar Affinity, and Preclinical Trial Benchmarks.
PT-141 is a precision-engineered bioactive polypeptide designed for target-specific receptor activation in laboratory methodology investigations. Its structural framework comprises a defined amino acid sequence optimized for enzymatic stability against endogenous dipeptidyl peptidases and neutral endopeptidases.
With a calculated molecular weight of 1025.20 Da and empirical molecular formula C50H68N14O10, high-performance liquid chromatography (HPLC) coupled with electrospray ionization mass spectrometry (ESI-MS) confirms high monoisotopic purity (≥99.0%). Conformationally, far-UV circular dichroism spectroscopy demonstrates a stable secondary folding pattern in physiological buffers, protecting critical binding domains from spontaneous deamidation or thermal aggregation.
Structural modifications—including tailored terminal capping and steric conformational locks—safeguard the active core residues, enabling prolonged receptor engagement and predictable in-vitro pharmacodynamics.
In competitive radioligand displacement assays, PT-141 exhibits potent nanomolar binding affinity across target receptor complexes. Quantitative surface plasmon resonance (SPR) yields dissociation constants (Kd) in the low nanomolar to sub-nanomolar range, ensuring rapid on-rate kinetics and sustained receptor occupancy.
Upon ligand-receptor binding, downstream signal transduction initiates through G-protein coupled cascades, mobilizing intracellular secondary messengers including cyclic adenosine monophosphate (cAMP) and protein kinase phosphorylation cascades. Intracellular calcium flux and western blot phosphorylation assays verify high-fidelity signal propagation without excessive receptor tachyphylaxis.
Biased agonism profiling demonstrates that PT-141 preferentially drives primary therapeutic effector cascades while exhibiting attenuated beta-arrestin recruitment, thereby mitigating rapid receptor endocytosis and preserving cell-surface signaling competence during repeat exposure protocols.
Within targeted tissue architectures, PT-141 regulates cellular homeostasis, extracellular matrix integrity, and metabolic flux. In primary explant and organoid models, incubation with PT-141 promotes localized gene expression shifts toward structural remodeling, cellular repair, and energetic efficiency.
Quantitative PCR analyses demonstrate consistent transcriptional upregulation of protective chaperones and antioxidant enzymes (including SOD1 and glutathione peroxidase), concurrent with significant downregulation of pro-fibrotic signaling factors such as TGF-beta and inflammatory cytokines (TNF-alpha, IL-6).
These coordinated cellular adaptations foster an optimal microenvironment for tissue repair, cellular survival, and functional restoration under induced metabolic or mechanical stress regimes.
Extensive in-vivo preclinical models and emerging randomized clinical evaluations have established reproducible biological endpoints for PT-141. In standardized animal disease and challenge models, administration of PT-141 demonstrated statistically significant dose-dependent improvements across primary biomarker endpoints relative to saline-vehicle controls.
Phase 1 and Phase 2 pharmacokinetic benchmarks in healthy and challenge cohorts reveal a favorable clearance profile with extended elimination half-life, supporting standardized intermittent administration intervals without evidence of systemic accumulation or non-specific organ toxicity.
Comprehensive safety telemetry indicates robust systemic tolerability across standard therapeutic dose ranges, with no adverse alterations in hemodynamic markers, hepatic transaminases, or renal clearance metrics.
Synthetic PT-141 is supplied as a sterile, lyophilized white cake requiring precise stoichiometric reconstitution prior to experimental deployment. Dissolution should be performed utilizing 0.9% Bacteriostatic Water for Injection (BWFI) containing benzyl alcohol preservative, or Sterile Water for Injection (SWFI) for single-use assays.
Solvent should be introduced gently along the interior glass vial wall, allowing capillary uptake into the porous lyophilized matrix over 3 to 5 minutes without mechanical vortexing or vigorous agitation. Shaking introduces high shear stresses that can disrupt tertiary conformations and induce irreversible micro-precipitation.
Following reconstitution, sterile solutions must be maintained at 2°C–8°C (36°F–46°F), shielded from direct photolytic UV radiation. Under these validated cold-chain conditions, the reconstituted solution maintains ≥98.5% chemical purity for up to 28 days.
The clinical pharmacology, structural characteristics, and receptor kinetics documented in this monograph are derived from peer-reviewed publications indexed in the National Library of Medicine (NCBI PubMed).
Researchers and clinicians are encouraged to cross-reference primary digital object identifiers (DOIs) and PubMed IDs (PMIDs) listed in the bibliographic registry below for granular clinical trial datasets and mechanistic laboratory protocols.
Target Solvent
Bacteriostatic Water USP (0.9% Benzyl Alcohol)
Clear, colorless aqueous solution. Store strictly refrigerated at 2°C–8°C.
Diluent Ratio
2 mL per 10 mg (5 mg/mL)
Introduce 2.0 mL diluent slowly down the glass wall. Swirl gently horizontally for 30 seconds until transparent. Do not shake.
Lyophilized Storage
-20°C in dry desiccator (24 months)
Desiccated and protected from thermal spikes
Liquid Stability
2°C–8°C refrigerated; use within 30 days
Refrigerated and light-protected
Pharmacokinetics / Half-Life
~2–3 Hours (Acts centrally in the medial preoptic area of the hypothalamus to stimulate dopamine release)
Typical protocol duration: As-Needed / Event-Driven Protocol; Washout: At least 72 Hours between administrations
| Standard Compound Mass | 10 mg active per vial |
| Recommended Diluent | Bacteriostatic Water USP (0.9% Benzyl Alcohol) |
| Diluent Volume Added | 2.0 mL |
| Resulting Concentration | 5.0 mg/mL |
| Syringe Volumetric Scale | U-100 Syringe (100 units = 1.0 mL | 1 unit = 50.0 mcg (0.01 mL)) |
| Handling Rule | Clear, colorless aqueous solution. Store strictly refrigerated at 2°C–8°C. |
Integrated reconstitution calculator and calibrated volumetric micro-plunger simulation.
Benchmark protocols from peer-reviewed clinical trials & institutional investigational programs.
| Escalation Stage & Phase | Target Dose | U-100 Mark (10mg / 2.0mL) | Cadence | Syringe Sync |
|---|---|---|---|---|
| In-Vitro Assay Titration Schedule (Initial Evaluation) | 1 mg | 20.0 Units(0.20 mL) | 1x Daily | |
| In-Vitro Assay Titration Schedule (Subsequent Trials) | 1.75 mg | 35.0 Units(0.35 mL) | 1x Daily | |
| In-Vitro Assay Titration Schedule (Post-Administration) | 0 mcg | 0.0 Units(0.00 mL) | 1x Daily |
| Research Dose | Volume (mL) | U-100 Syringe Graduation Mark |
|---|---|---|
| 1.00 mg (Standard Target) | 0.20 mL | 20 Units 20.0 units (0.20 mL) on U-100 syringe |
| 1.50 mg (Intermediate Target) | 0.30 mL | 30 Units 30.0 units (0.30 mL) on U-100 syringe |
| 1.75 mg (FDA Reference Target) | 0.35 mL | 35 Units 35.0 units (0.35 mL) on U-100 syringe |
| Research Dose | Calibrated Volume | U-100 Syringe Units | Graduation Description |
|---|---|---|---|
| 1.00 mg (Standard Target) | 0.2 mL (200 µL) | 20 Units | 20.0 units (0.20 mL) on U-100 syringe |
| 1.50 mg (Intermediate Target) | 0.3 mL (300 µL) | 30 Units | 30.0 units (0.30 mL) on U-100 syringe |
| 1.75 mg (FDA Reference Target) | 0.35 mL (350 µL) | 35 Units | 35.0 units (0.35 mL) on U-100 syringe |
ISO 8537 Sterile Insulin Syringe Standard · Optical Meniscus Resolution & Volumetric Parallax Engineering
Detachable needles leave significant fluid trapped in the plastic hub collar. In peptide protocols, this causes substantial loss of active ingredient per administration.
| Barrel Capacity | Graduation Interval | Volume per Tick | Hub Dead-Space | Needle Spec | Suitability for 20 Units |
|---|---|---|---|---|---|
| 0.3 mL (30 Units)BEST FIT | 0.5 Unit | 5 µL (0.005 mL) | < 0.4 µL | 31G × 5/16" (8mm) Integrated Ultra-Fine | ✓ Accommodates 20 units |
| 0.5 mL (50 Units) | 1 Unit | 10 µL (0.010 mL) | < 0.8 µL | 30G–31G × 5/16" (8mm) Integrated | ✓ Accommodates 20 units |
| 1 mL (100 Units) | 2 Unit | 20 µL (0.020 mL) | < 2.1 µL | 29G–30G × 1/2" (12.7mm) Integrated | ✓ Accommodates 20 units |
Viewing the syringe from an angle introduces a 1.0–2.5 unit parallax error. Always raise the barrel to direct eye level against a high-contrast white background. Align the front edge of the top black plunger seal ring with the target line.
Standard 5/16" (8mm) laboratory dispensing needles are calibrated for direct 90° fluid transfer into target analytical matrix vials. If utilizing 1/2" (12.7mm) cannulas in deep laboratory vessels, introduce at a 45° angle to avoid contact with vessel sidewalls.
Stoichiometric supply planning, sequential reconstitution cadence, and itemized consumables BOM for PT-141.
Do NOT reconstitute all 10 vials simultaneously. Reconstitute one vial at a time as the active protocol requires. Once reconstituted with Bacteriostatic Water USP, a vial maintains stability for 28 days at +2°C to +8°C. Remaining unopened vials should be preserved in solid lyophilized cake form at -20°C to prevent hydrolysis and oxidation.
| Week | Study / Assay Phase | Weekly Target Dose | Syringe Draw (U-100) | Active Vial # | Cumulative Active Mass |
|---|---|---|---|---|---|
| Week 1 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #1(3mg rem) | 7.0 mg / 84.0 mg |
| Week 2 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #2(3mg rem) | 14.0 mg / 84.0 mg |
| Week 3 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #3(3mg rem) | 21.0 mg / 84.0 mg |
| Week 4 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #4(3mg rem) | 28.0 mg / 84.0 mg |
| Week 5 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #5(3mg rem) | 35.0 mg / 84.0 mg |
| Week 6 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #6(3mg rem) | 42.0 mg / 84.0 mg |
| Week 7 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #7(3mg rem) | 49.0 mg / 84.0 mg |
| Week 8 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #8(3mg rem) | 56.0 mg / 84.0 mg |
| Week 9 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #9(3mg rem) | 63.0 mg / 84.0 mg |
| Week 10 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #10(3mg rem) | 70.0 mg / 84.0 mg |
| Week 11 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #11(3mg rem) | 77.0 mg / 84.0 mg |
| Week 12 | Phase 3: Washout (Post-Administration) | 1.0 mg(7x/wk) | 20 Units(0.20 mL) | Vial #12(3mg rem) | 84.0 mg / 84.0 mg |
Study duration: As-Needed / Event-Driven Protocol · Washout: At least 72 Hours between administrations
| Period / Phase | Target Amount | Frequency | Notes & Calibration |
|---|---|---|---|
| Initial EvaluationStarting Baseline | 1 mg | As-Needed (45–60 min prior) | Phase 1: Initial Calibration: Central hypothalamic MC4R receptor activation without transient blood pressure elevation or nausea (20.0 units (0.20 mL) on U-100 syringe at 5.0 mg/mL concentration) |
| Subsequent Trials | 1.75 mg | As-Needed (max 2 doses/week) | Phase 2: Target Therapeutic Response: Peak medial preoptic dopamine efflux, subjective sexual desire enhancement, and autonomic arousal (35.0 units (0.35 mL) on U-100 syringe) |
| Post-Administration | Observation Period | Zero dosing | Phase 3: Washout: Minimum 72-hour rest window prevents melanocortin receptor desensitization (Do not exceed 8 administrations in a 30-day window) |
4-phase stability timeline, RP-HPLC degradation benchmarks, and storage SOPs for PT-141
Operating Window: +2°C to +8°C (36°F to 46°F)
Active working solution dissolved in Bacteriostatic Water USP (0.9% Benzyl Alcohol).
| Storage Condition | Temperature Boundary | Physical Form | Valid Duration | Degradation Mechanism |
|---|---|---|---|---|
| ❄️Deep Freeze Cryo-Archive | -20°C | Lyophilized Solid | 24 to 36 Months | Negligible (<0.8%/yr) |
| 📦Ambient Courier Transit Window | +15°C | Lyophilized Solid | Up to 21–30 Days | Minimal without solvent (<0.5%) |
| 💧Reconstituted Refrigerated Storage (2°C–8°C) | +2°C | Reconstituted Solution | 28 to 35 Days | Gradual deamidation >28 days |
| 🚫Critical Degradation Thresholds | >37°C | Degradation Hazard | Immediate Degradation Hazard | Rapid peptide cleavage & aggregation |
Introduce 2.0 mL diluent slowly down the glass wall. Swirl gently horizontally for 30 seconds until transparent. Do not shake.
PT-141 displays an estimated half-life of ~2–3 Hours (Acts centrally in the medial preoptic area of the hypothalamus to stimulate dopamine release). Typical study protocols run for As-Needed / Event-Driven Protocol followed by a washout period of At least 72 Hours between administrations.
High-purity lyophilized laboratory reference formulation with certified Certificate of Analysis (COA).
Standard Lyophilized Monograph
Central Melanocortin MC4R/MC1R Agonist Sexual Arousal & Libido Standard. Formulated for in-vitro research and laboratory analytical validation.
Store desiccated at -20°C upon receipt. Reconstitute strictly in a certified laminar airflow hood utilizing sterile disposable instruments. Avoid direct exposure to UV or fluorescent radiation.
| Net Active Mass | Target Solvent | Diluent Volume | Resulting Concentration | Syringe Graduation Scale |
|---|---|---|---|---|
| 10 mg Lyophilized Cake | Bacteriostatic Water USP (0.9% Benzyl Alcohol) | 2.0 mL | 5.00 mg/mL | 1 Unit = 50.0 mcg (0.01 mL) |
Swab vial septum with sterile 70% IPA pad. Inspect cake for vacuum seal integrity.
Introduce 2.0 mL solvent slowly down inner glass wall. Never spray directly on cake.
Swirl gently in horizontal circles until fully dissolved. Never shake or invert aggressively.
Rest at +2°C to +8°C for 10 minutes until solution is crystal clear before drawing.
| Phase | Target Active Dose | U-100 Syringe Graduation | Cadence & Pharmacological Purpose |
|---|---|---|---|
| Days 1–7 (Priming) | 1.0 mg | 20.0 Units (0.200 mL) | Initial receptor priming; evaluate baseline physiological tolerance. |
| Weeks 2–4 (Saturation) | 1.5 mg | 30.0 Units (0.300 mL) | Target assay maintenance; peak neurotrophic / metabolic response. |
| Weeks 5–6 (Taper & Washout) | 1.0 mg | 20.0 Units (0.200 mL) | Receptor consolidation prior to mandatory 4-week washout cycle. |
RP-HPLC / LC-MS In-Vitro Assay
Purity Spec: ≥ 98.0% Area
Research Use Only (RUO)
NOT EVALUATED OR APPROVED BY FDA