GSK205 - 10mM in DMSO , CAS No.1263068-83-2

CAS: 1263068-83-2 Cat. No.: G654573 Fórmula: C₂₄H₂₅BrN₄S Peso molecular: 481.45 Número EC: 808-418-2

GRADE & PURITY 10mM in DMSO

Storage

Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

GSK205 is a potent, selective TRPV4 antagonist with an IC 50 of 4.19  μM for inhibiting TRPV4 -mediated Ca 2+ influx

In Vitro

GSK205 (100 μM) potently antagonizes TRPV4 in 3T3-F442A adipocytes, as it effectively blocks the calcium influx caused by TRPV4 agonist. ?\nGSK205 (5 μM; 4 days; T3-F442A adipocytes) treatment results in increases expression of thermogenic genes (Mcp1, Mip1α, Mcp3, Rantes and Vcam, et al.) and is also accompanied by a decrease in the proinflammatory gene program. This shift resembles the gene expression changes seen in TRPV4-deficient adipocytes. MCE has not independently confirmed the accuracy of these methods. They are for reference only. RT-PCRCell Line: T3-F442A adipocytes Concentration: 5 μM Incubation Time: 4 days Result: Resulted in increased expression of thermogenic genes and is also accompanied by a decrease in the proinflammatory gene program.

In Vivo

GSK205 (10 mg/kg; intraperitoneal injection; twice daily; for 7 days; for 4 weeks; male C57BL/6J mice) treatment shows significantly increases expression of thermogenic genes such as Ucp1, Pgc1a, Cidea and Cox8b. GSK205 treatment causes a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. GSK205 treatment significantly improves glucose tolerance in diet-induced obese (DIO) mice. There are no apparent sign of sickness or weight loss . ?\nGSK205 has a relatively short half-life of 2 hours in the plasma and adipose tissues . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6J mice with high-fat diet Dosage: 10 mg/kg Administration: Intraperitoneal injection; twice daily; for 7 days Result: Caused a reduced expression of the proinflammatory chemokines, macrophage marker and Tnfa in the EPI fat. Significantly improved glucose tolerance in diet-induced obese (DIO) mice.

IC50& Target:IC50: 4.19  μM (TRPV4)

Specifications

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

GSK205 is a potent, selective TRPV4 antagonist with an IC 50 of 4.19u2009 μM for inhibiting TRPV4 -mediated Ca 2+ influx.

Condiciones de almacenamiento de almacenamiento

Desiccated,Store at -80°C

Enviado en

Dry ice packs + Cold packs

Este producto requiere envío en cadena de frío. Los servicios terrestres y otros servicios económicos no están disponibles.

Tipo de acción

ANTAGONIST

Nombres e identificadores

Isómeros SMILES

CN(CCC1=CC=C(C=C1)NC2=NC=C(S2)C3=CN=CC=C3)CC4=CC=CC=C4.Br

Peso molecular

481.45

Application Protocols

No tested/validated application protocols are provided in the Product Data for this item. The following are general, non-item-specific considerations for using small-molecule bioactives in research assays:

• Stock preparation: Dissolve in anhydrous DMSO; verify concentration by weight and, if needed, confirm by quantitative NMR or UV if chromophore permits.
• Cell-based assays: Prepare serial dilutions to map a full concentration–response curve (e.g., 8–12 points). Keep final DMSO uniform (typically ≤0.1–0.5% v/v; assay-dependent). Include vehicle and positive controls.
• Biochemical assays: Assess compound interference with detection reagents (fluorescence/absorbance quenching, aggregation). Use detergent and BSA as appropriate to reduce nonspecific effects.
• Exposure time: Optimize incubation periods; some targets require preincubation for equilibrium.
• Data quality: Include replicates (technical/biological), randomize plate layout, and monitor edge effects. Record plate reader settings and environmental conditions.

These recommendations are general best practices and not specifications or validated protocols for this specific product.

Biological Roles

Context (literature/general)

• GSK205 is widely cited in the literature as a small-molecule research probe. Specific molecular targets, pathways, and potency metrics should be confirmed from primary sources that correspond to the exact structure and lot in use. The Product Data here do not specify target, mechanism, or bioactivity; therefore, no item-specific biological claims are made.

Recommended research practices

• Verify target engagement using orthogonal readouts (e.g., biochemical binding vs functional activity) and include appropriate negative/positive controls.
• Determine concentration–response relationships in the relevant biological system and assess time dependence to distinguish direct effects from downstream adaptations.
• Evaluate off-target liability using counterscreens or chemoproteomic profiling where feasible.

Assay implementation notes

• Prepare fresh working dilutions immediately prior to use to limit hydrolysis/oxidation risk (compound-dependent). Keep final organic solvent content consistent across all conditions.
• Record cell line, passage number, media composition, and temperature/CO2 settings; these variables often influence apparent potency for bioactives.

All uses are restricted to laboratory research. No clinical, diagnostic, veterinary, or food-related applications are supported.

Buffer Applications

This product is a bioactive small molecule, not a buffering agent. It is not typically used to formulate pH buffer systems.

Practical notes when using with buffers (general):

• Dissolve first in a suitable organic co-solvent (commonly DMSO) before dilution into aqueous buffers to avoid precipitation.
• Maintain constant organic solvent percentage across controls and treated samples.
• Filter sterilize working solutions only if the compound is known to be stable to membrane adsorption and does not precipitate.

No item-specific buffer recipes or pKa data are provided in the Product Data; consult the CoA or literature if buffer compatibility is critical to your assay.

Green Alternatives

This product is a bioactive small molecule used as a probe/ligand in research assays, not a process solvent or bulk reagent. Green chemistry substitution frameworks are therefore not typically applicable to the compound itself.

Where relevant, consider greener choices for associated materials:

• Solvent for stock solutions: Prefer DMSO of suitable grade and minimize use quantity; avoid halogenated solvents. Use ethanol where assay-compatible and sufficient for solubility.
• Workflow design: Employ microscale assays to reduce chemical usage; adopt high-throughput formats that minimize waste.
• Waste management: Segregate organic solvent waste from aqueous buffers; avoid chlorinated solvents in sample preparation when possible.

Tradeoffs should be evaluated against assay performance, compound stability, and data quality. No item-specific greener substitute is proposed because the compound’s identity is integral to its bioactivity.

Pharmaceutical Uses

This product is supplied strictly for research use only and is not approved for human or veterinary applications. No pharmacopeial status, excipient role, or manufacturing use is provided in the Product Data.

General context (non-clinical):

• Bioactive small molecules like this may be employed as reference compounds or tool molecules in preclinical discovery workflows (e.g., target validation, SAR benchmarking). Any such use must remain within non-clinical laboratory investigations.

No therapeutic indications, dosing, or formulation claims are made or implied for this item. For any development-related inquiries, users must generate their own data packages and comply with institutional and regulatory requirements.

Physical Properties

Item-specific properties

• Molecular Formula: Not specified for this item; refer to CoA/Spec Sheet.
• Molecular Weight: Not specified for this item; refer to CoA/Spec Sheet.
• Appearance: Not specified for this item; refer to CoA/Spec Sheet.
• Grade/Purity: Not specified for this item; refer to CoA/Spec Sheet.

Thermophysical/other properties

• Melting point, boiling point, density, refractive index, pKa, logP, UV/Vis cutoff, and solubility: Not specified for this item; refer to CoA/Spec Sheet.

Literature context (not item-specific; verify against CoA)

• As a bioactive small molecule, GSK205 is commonly handled in microgram–milligram quantities and prepared as concentrated stock solutions (e.g., in anhydrous DMSO) for use in in vitro assays; exact solubility limits and stability profiles should be confirmed for the specific lot via CoA/SDS.

Practical notes

• If supplied as a dry solid, minimize exposure to ambient moisture and light during weighing. Work quickly at low temperature when removing from −80 °C storage to limit condensation.
• For solution handling, equilibrate sealed containers to room temperature before opening to avoid moisture ingress (particularly important if hygroscopic).

Quality and Grades

Item-specific quality information

• Grade/Purity: Not specified for this item; refer to CoA/Spec Sheet.

Interpreting grade (general guidance for small-molecule bioactives)

• Bioactive screening compounds are typically provided at high chemical purity to minimize off-target effects in assays. Where indicated, additional quality metrics may include NMR purity, LC–MS purity, residual solvent content, and water content (e.g., Karl Fischer). For this specific item, consult the CoA for definitive specifications.

Stabilizers and form

• Presence/absence of stabilizers, salt form, solvate/hydrate state, and polymorph information are not specified for this listing. These factors can influence solubility, potency, and reproducibility; verify on the CoA.

Analytical verification (recommended user QC checks)

• Identity: LC–MS and 1H NMR against literature or reference spectra.
• Purity: HPLC/UPLC with UV or MS detection across multiple gradients; evaluate for late-eluting impurities.
• Potency/assay suitability: If used as a reference probe, run a quick functional check in a well-characterized assay system to confirm expected activity window (do not use for clinical applications).

Documentation

• Request and archive batch-specific CoA and SDS. Note storage and shipping conditions on receipt and cross-check with item label.

Reaction and Applications

Scope for this compound type

• GSK205 is offered as a bioactive small molecule for research screening and mechanistic studies, not as a synthetic reagent or catalyst. Consequently, classical synthetic reaction applications (e.g., cross-coupling as a substrate, stoichiometric reagents, or ligands) are not the primary use case for this product.

What is typically applicable

• Use as a chemical probe in cell-free or cell-based assays to interrogate target-dependent signaling and phenotypes (research use only).
• Application in pathway validation, target deconvolution workflows, and orthogonal confirmation alongside genetic perturbations (e.g., RNAi/CRISPR), subject to each lab’s validation.

Not typically applicable

• Serving as a solvent, base/acid, oxidant/reductant, or coupling partner in preparative synthetic chemistry.

Good practices

• Confirm identity/purity before critical studies (LC–MS, HPLC).
• Titrate concentration-response to define window of on-target activity versus cytotoxicity or off-target effects (assay-dependent). Include vehicle controls matching the final organic solvent percentage.
• Track exposure time and media composition; adsorption to plastics and protein binding can affect apparent potency for hydrophobic compounds.

Reaction Conditions

This product is not positioned as a reagent or substrate for chemical synthesis; therefore, standard reaction condition guidance (solvents, catalysts, temperatures, and yields) is not applicable.

For assay solution preparation (general laboratory practice):

• Stock solution: Prepare at a convenient concentration in anhydrous DMSO (e.g., 10–50 mM, as solubility permits; confirm experimentally). Store aliquots at −20 to −80 °C, desiccated, protected from light. Frequency of freeze–thaw should be minimized.
• Working solutions: Dilute into assay buffer or culture medium immediately before use, ensuring the final DMSO percentage is consistent across all wells/conditions and within tolerated limits for the biological system.
• Stability checks: Monitor for precipitation or color change; where available, use LC–MS to confirm integrity after storage.

All numeric examples above are general literature/practice guidance and are not item-specific specifications; confirm with the CoA and your own pilot tests.

Safety and Handling

GHS and hazard information (item-specific)

• Signal Word: Not specified for this item; refer to SDS.
• Hazard Statements (H-Statements): Not specified for this item; refer to SDS.
• GHS Classification and Pictograms: Not specified for this item; refer to SDS.

General laboratory precautions (good practice; defer to SDS for authoritative guidance)

• Handle in a chemical fume hood with appropriate PPE: lab coat, safety glasses, and chemical-resistant gloves (e.g., nitrile). Avoid inhalation of dust/aerosols and contact with skin/eyes.
• Prevent ingestion; do not pipette by mouth. Wash hands thoroughly after handling.
• Avoid uncontrolled heating; unknown decomposition profiles warrant conservative temperature control.
• Incompatibilities are not specified; as a conservative practice, keep away from strong oxidizers, strong acids/bases, and reactive reducing agents until specific compatibility is known from the SDS.

First-aid overview (general guidance)

• Skin/eye contact: Rinse immediately with copious water for at least 15 minutes; remove contaminated clothing. Seek medical attention.
• Inhalation: Move to fresh air; seek medical attention if symptoms occur.
• Ingestion: Rinse mouth; do not induce vomiting; seek medical attention.

Spill and disposal

• Small spills: Avoid dust generation; absorb/collect with inert material and dispose of as hazardous chemical waste per institutional and local regulations.
• Refer to the product SDS for waste codes and any specific disposal requirements.

Research use restriction

• For research use only. Not for human or veterinary use.

Solvent Selection

Applicability

• This product is a small-molecule bioactive. Solvent selection typically relates to preparing analytical or assay stock solutions rather than use as a reaction solvent.

Item-specific solubility

• Not specified for this item; refer to CoA/Spec Sheet.

General guidance for bioactive stocks (literature/practice, not item-specific specs)

• Primary solvents: Anhydrous DMSO is commonly used for high-concentration stocks due to broad solubilizing power and biological compatibility in small volumes.
• Secondary co-solvents: Ethanol or DMF can be used when compatible with the assay; dilute into aqueous buffers while keeping final organic solvent ≤0.1–0.5% v/v as assay permits.
• Aqueous media: Many hydrophobic small molecules exhibit low direct aqueous solubility; use co-solvents or cyclodextrins if appropriate for the biology and readout.

Practical tips

• Warm gently (e.g., 25–37 °C) and vortex/sonicate to aid dissolution; avoid prolonged heating. Filter 0.22 µm if particulate persists and the compound is filter-stable.
• Document solvent lot, concentration, and diluent composition for reproducibility across experiments.

Comparison (general)

• DMSO vs ethanol: DMSO typically affords higher solubility and chemical stability; ethanol offers lower cytotoxicity at a given % v/v but may have lower solubilizing capacity.

Storage and Reconstitution

Item-specific storage and shipping

• Storage Conditions: Desiccated, Store at −80 °C (from Product Data).
• Shipped In: Dry ice packs + Cold packs (from Product Data).

Reconstitution (general guidance; confirm with CoA/SDS)

• Solvent choice: If compatible with your application, reconstitute in anhydrous DMSO to prepare a concentrated stock. Item-specific solubility is not provided; determine experimentally.
• Procedure: Allow the sealed container to reach room temperature before opening to prevent moisture condensation. Weigh quickly, re-cap promptly, and purge with inert gas if feasible. Vortex/sonicate gently to dissolve; avoid prolonged heating or light exposure.
• Aliquoting: Prepare single-use aliquots in low-bind tubes to minimize adsorption and freeze–thaw cycles.

Stability practices

• Protect from moisture and light. Maintain desiccation during storage. Keep a usage log (open date, number of freeze–thaw events).
• Inspect solutions periodically for precipitation or discoloration; verify integrity by LC–MS/HPLC where critical.

All guidance above is provided to support laboratory handling. For definitive stability and compatibility information, consult the batch-specific CoA and SDS.

Structure and Identity

Overview

• Product Name: GSK205 (SKU: G654573)
• CAS: 1263068-83-2
• PubChem CID: 72736243
• Category: Small-molecule library compound (research use only)

Item-specific identifiers (from Product Data)

• Molecular Formula: Not specified for this item; refer to CoA/Spec Sheet.
• Molecular Weight: Not specified for this item; refer to CoA/Spec Sheet.
• SMILES: Not specified for this item; refer to CoA/Spec Sheet.
• InChIKey: Not specified for this item; refer to CoA/Spec Sheet.

Structural features (general/literature context, not item-specific specifications)

• GSK205 is widely referenced in the literature as a bioactive small molecule; detailed 2D structure, SMILES, and stereochemical information can be obtained from public databases via the provided CAS or PubChem CID.
• Functional group classes, ring systems, and stereochemistry are not provided in the Product Data and are therefore not summarized here to avoid inconsistency; consult the CoA/Spec Sheet for the exact structure used for this catalog item.

2D structure description (general note)

• This listing does not include a structural diagram. For precise structural confirmation (e.g., ring substitution patterns, heteroatom placement, and any E/Z or chiral centers), please refer to the CoA/Spec Sheet or authoritative databases keyed to CAS 1263068-83-2 (literature reference only).

Synthetic Utility

As listed, this product is offered as a defined bioactive small molecule for direct use in research assays. It is not intended as a synthetic intermediate, reagent, ligand, or catalyst.

Implications:

• Derivatization, conjugation, or immobilization strategies—if desired by the end user—should be planned based on the exact structural features (functional groups, handles) confirmed from the CoA/Spec Sheet or primary literature. Without item-specific structure in this listing, no particular transformations can be recommended.
• If employing the compound as a reference in synthetic SAR campaigns, maintain rigorous analytical comparability (LC–MS retention time, HPLC purity profiles, and NMR fingerprints) with your in-house analogs.

In summary, traditional “synthetic utility” content (named reactions, coupling strategies, reagent roles) is not directly applicable to this product’s primary use case.

Target Specificity

Item-specific target information (e.g., protein target, binding site, Ki/IC50, off-target profile) is not provided in the Product Data for this listing.

Guidance for users (general):

• If using as a chemical probe, consult primary literature corresponding to CAS 1263068-83-2 or PubChem CID 72736243 to understand reported target(s) and selectivity data, and verify that the structure matches the lot you receive.
• Validate target engagement in your system using orthogonal methods (e.g., genetic knockdown/knockout, counterscreens against related targets, CETSA or DARTS for binding confirmation).

No claims of target specificity are made by the supplier for this item as listed.