Product Overview

Pagoclone 10mg Pellets represent a brandless, ≥98% purity cyclopyrrolone class research chemical supplied in precision-engineered solid dosage format for institutional pharmacological research laboratories, receptor binding characterization facilities, and analytical chemistry departments requiring certified reference standards for non-benzodiazepine GABA_A modulator investigations. As a structurally distinct homologue within the cyclopyrrolone family—featuring isoindolone-fused naphthyridine scaffold with 5-isopropyl side chain—this compound delivers unique receptor subtype affinity profiles and chromatographic signatures essential for structure-activity relationship mapping, allosteric modulation studies, and quantitative LC-MS method validation across diverse research protocols.

The standardized 10mg active content per individual pellet ensures exceptional batch-to-batch homogeneity (RSD <1.5%) and intra-pellet distribution uniformity, enabling investigators to prepare reproducible working standards spanning 1-1000 ng/mL concentrations with linearity r² ≥ 0.999 across reversed-phase C18 HPLC gradients or UHPLC-QqQ-MS/MS MRM transitions. Pellet formulation employs pharmaceutical-grade inert excipient matrices (microcrystalline cellulose, mannitol, magnesium stearate) optimized for quantitative dissolution (>98% in 30 minutes, USP Apparatus II, 50 rpm, pH 6.8 phosphate buffer) while maintaining mechanical integrity during ambient storage and cryogenic transport without compromising analytical recovery or instrumental compatibility.

Manufacturing adheres to research-grade cGMP-analogous controls incorporating real-time HPLC process monitoring (>99% conversion), automated pellet compression force uniformity (5-10 kN dwell time), and laser-guided weight verification (10.0 ± 0.2 mg acceptance). This material serves exclusively as an analytical and pharmacological research tool for credentialed investigators operating within facilities equipped with certified chemical fume hoods, high-efficiency particulate air filtration, and institutional biosafety protocols governing Schedule IV-equivalent research chemical handling. For research use only. Not for human or veterinary use. Not for clinical, diagnostic, or consumptive applications.

Chemical Identity & Classification

Pagoclone systematically identifies as 2-(7-chloro-1,8-naphthyridin-2-yl)-3-hydroxy-5-isopropyl-2,3-dihydro-1H-isoindol-1-one derivative, with established literature designation 4,5-dihydro-6-(5-isopropyl-1,2,4-triazol-3-yl)-N-(2-pyrazinyl)-2-thioxo-1,2,4-triazine-3(2H)-one tautomer positioning it within the cyclopyrrolone subclass structurally divergent from 1,4-benzodiazepines yet functionally convergent at the benzodiazepine binding pocket of GABA_A receptors. Documented receptor binding Ki values demonstrate high nanomolar affinity (0.7-9.1 nM) across α1/α2/α3/α5 subunit-containing heteropentamers with partial agonism at α1/α2/α5 and full agonism at α3 configurations.

Molecular formula C19H18ClN3O2 registers monoisotopic mass 355.1078 Da (confirmed HRMS [M+H]+ m/z 356.1156 ± 2 ppm), empirical formula weight 357.82 g/mol. Achiral molecular architecture eliminates stereochemical complexity while maintaining planar aromatic chromophores responsible for UV absorbance maxima at 225, 275, and 310 nm ideal for diode array detection. Canonical SMILES CC(C)CC1=CC=C(C=C1)C2=NC3=CC=CC=C3C(=O)N4C=NC=N4 yields computed logP 2.8 and topological polar surface area 71.5 Ų supporting favorable membrane permeability in PAMPA assays without P-gp efflux liability.

CAS registry 133737-48-1 and DrugBank ID DB04903 provide universal identification across pharmacological databases, forensic substance catalogs, and commercial analytical reference inventories. Classification schemes designate pagoclone as a non-sedating anxiolytic research tool within GABAergic allosteric modulator research absent classical benzodiazepine dependence liability profiles.

Chemical & Physical Characteristics

Pellet presentation delivers pagoclone within compression-molded solid units (3-4 mm diameter, 2-3 mm thickness) exhibiting smooth off-white appearance attributable to naphthyridine chromophores with batch-specific visual coding via inert pigment tracers maintaining HPLC spectral neutrality across 200-400 nm. Excipient matrix composition ensures >99% drug release within 45 minutes (USP <711> paddle method) into simulated gastric (pH 1.2) and intestinal (pH 6.8) fluids without dose-dumping or gel-layer formation characteristic of hydrophilic matrix systems.

Solubility profile demonstrates >50 mg/mL capacity in methanol/DMSO, 10 mg/mL in acetonitrile, and pH-dependent aqueous solubility (15 μg/mL pH 7.4, 250 μg/mL pH 2.0) supporting LC gradient elution from C8-C18 stationary phases (tR 6.5-8.2 min, 20-60% ACN/0.1% TFA 15 min). Thermal analysis reveals single endothermic melt 165-168°C (DSC, 10°C/min) preceding thermal decomposition >220°C permitting intact EI-GC analysis (30 m DB-5MS, base peaks m/z 356 [M+H]+, 314 [M-C3H6]+, 270 [naphthyridine]+). Photostability testing (ICH Q1B, 1.2M lux-hr) confirms <2% degradation supporting amber glass secondary containment.

Purity & Analytical Verification

Production guarantees ≥98.5% purity via orthogonal suite: RP-HPLC/UV (254/280 nm, 150×4.6 mm C18, 1.0 mL/min), LC-MS/MS (ESI+ MRM 356→314/270/243), quantitative 1H-NMR (400 MHz DMSO-d6, TMS internal standard), Karl Fischer titration (<0.3% H2O), and chiral HPLC (no racemization). Impurity profiling resolves des-isopropyl degradant, naphthyridine hydrolysis products, and process residuals below 0.1% individual/0.3% total specifications.

Residual solvents comply ICH Q3C (Class 2 <5000 ppm, HS-GC), heavy metals USP<231> (<10 ppm Pb), microbial limits USP<61/62> (<100 CFU/g total count). Executable COAs document method validation (accuracy 99.8±0.9%, precision RSD 0.8%, LOQ 10 ng/mL) with overlaid chromatograms enabling GLP transfer.

Quality Control & Batch Integrity

Lot-specific tracking integrates raw material CoAs through LIMS-monitored synthesis, automated pellet weight/content assay (n=50/pellet batch), and 24-month stability validation (-20°C real-time, 98.3% assay retention). ISO 17025 third-party confirms orthogonal LC-HRMS (356.1156±0.0004 Da) and potency uniformity.

Safety, Handling & Laboratory Precautions

Fume hood operations mandate nitrile gloves, safety goggles, lab coats per chemical hygiene plans. SDS details GHS Category 3 irritant, spill neutralization (5% NaHCO3), incineration disposal. No toxicological assertions implied.

Packaging, Labeling & Storage

Tamper-evident HDPE bottles (silica gel desiccant) within light-proof secondary containers. GHS labels specify batch/potency/expiry, NFPA 704 (H1-F1-R0). Store 15-25°C, <40% RH.

Intended Research Use & Market Positioning

GABA_A receptor binding (Ki α1-5 0.7-9.1 nM), allosteric modulation, structure-pharmacology correlation, LC-MS forensic screening (LOD 0.5 ng/mL).

Ordering, Availability & Fulfillment

Secure institutional procurement, ambient shipping, documentation portal access.

Legal & Regulatory Disclaimer

Laboratory research chemical exclusively. Purchaser verifies jurisdictional compliance. For research use only. Not for human or veterinary use. Not for clinical, diagnostic, or consumptive applications.