Xelafaslatide
Based on 1 Customer Validation
Xelafaslatide (ONL-1204) is a Fas receptor antagonist. Xelafaslatide blocks the Fas receptor signaling pathway and inhibits downstream apoptosis and inflammatory pathways. Xelafaslatide suppresses neuroinflammation and microglial activation in glaucoma models, protects retinal ganglion cells and prevents axonal degeneration. Xelafaslatide is applicable to relevant research on glaucoma.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.02%
- CAS. Nr.: 2040964-58-5
- Formel: C71H100N18O16
- Molecular Weight:1461.66
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Speicherung:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
IL-6 |
IL-1β |
Caspase 8 |
TLR4 |
NLRP3 |
In Vitro
Xelafaslatide (15-125 μM; 4 h-overnight) dose-dependently blocks FasL-mediated apoptosis of murine A20 B lymphoma cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:murine A20 B lymphoma cells
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Concentration:15 μM, 30 μM, 60 μM, 125 μM
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Incubation Time:4 h (with mFasL-VP); overnight (with 3H-thymidine)
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Result:Inhibited mFasL-induced apoptosis of A20 cells in a dose-dependent manner.
Significantly increased cell survival at all tested concentrations relative to vehicle-treated mFasL-VP-exposed cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J wild-type (8-week-old, glaucoma model induced by anterior chamber injection of 15-μm polystyrene microbeads)[1]
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Dosage:2 μg per 1 μL
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Administration:intravitreal; single dose (day 0, prior to microbead injection)
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Result:Achieved RGC density equivalent to saline-injected control mice, fully preventing microbead-induced RGC loss.
Attained optic nerve axon density equivalent to saline-injected control mice, fully preventing microbead-induced axon loss.
Preserved a quiescent, dendritic morphology in Iba1+ retinal microglia (ganglion cell layer/inner plexiform layer), with significantly longer microglial cell processes compared to vehicle-treated microbead-injected mice.
Abrogated the microbead-induced upregulation of multiple inflammatory and glial activation genes (including GFAP, Caspase-8, TNFα, IL-1β, IL-18, IL-6, MIP-1α, MIP-1β, MIP-2, MCP1, IP10, C3, C1Q, TLR4, and NLRP3), with gene expression levels equivalent to saline-injected controls.
Chemical Information
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CAS. Nr. 2040964-58-5
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Appearance Solid
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Molecular Weight 1461.66
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Formel C71H100N18O16
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Color White to off-white
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Synonyms
ONL-1204
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Sequence
His-His-Ile-Tyr-Leu-Gly-Ala-Val-Asn-Tyr-Ile-Tyr-NH2
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Sequence Shortening
HHIYLGAVNYIY-NH2
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (68.42 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 12.5 mg/mL (8.55 mM; Need ultrasonic)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Research Protocol for Neurological Diseases
PINK1/Parkin-mediated mitophagy pathway is a mitochondrial quality-control signaling axis in which mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, activates Parkin recruitment and E3 ubiquitin ligase activity, promotes ubiquitination of outer mitochondrial membrane proteins, recruits selective autophagy adaptors, and drives lysosomal degradation of damaged mitochondria. In neurological disease research, this pathway is experimentally important because neurons, especially dopaminergic neurons, are highly dependent on mitochondrial integrity, and defective mitochondrial turnover can lead to mitochondrial dysfunction, oxidative stress, impaired neuronal survival, α-synuclein accumulation, and neuroinflammatory damage-associated signals. The genetic disease link is strongest in Parkinson’s disease because mutations in PRKN/parkin cause autosomal recessive juvenile parkinsonism, mutations in PINK1 cause hereditary early-onset Parkinson’s disease, and Drosophila studie
Reinheit & Dokumentation
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Data Sheet (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.6842 mL | 3.4208 mL | 6.8415 mL | 17.1038 mL |
| 5 mM | 0.1368 mL | 0.6842 mL | 1.3683 mL | 3.4208 mL | |
| DMSO | 10 mM | 0.0684 mL | 0.3421 mL | 0.6842 mL | 1.7104 mL |
| 15 mM | 0.0456 mL | 0.2281 mL | 0.4561 mL | 1.1403 mL | |
| 20 mM | 0.0342 mL | 0.1710 mL | 0.3421 mL | 0.8552 mL | |
| 25 mM | 0.0274 mL | 0.1368 mL | 0.2737 mL | 0.6842 mL | |
| 30 mM | 0.0228 mL | 0.1140 mL | 0.2281 mL | 0.5701 mL | |
| 40 mM | 0.0171 mL | 0.0855 mL | 0.1710 mL | 0.4276 mL | |
| 50 mM | 0.0137 mL | 0.0684 mL | 0.1368 mL | 0.3421 mL | |
| 60 mM | 0.0114 mL | 0.0570 mL | 0.1140 mL | 0.2851 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Keywords
- Xelafaslatide
- 2040964-58-5
- ONL-1204
- ONL1204
- ONL 1204
- Fatty Acid Synthase (FASN)
- Apoptosis
- Interleukin Related
- Toll-like Receptor (TLR)
- NOD-like Receptor (NLR)
- Caspase
- retinal ganglion cell
- chemokines
- pro-inflammatory genes
- axon degeneration
- inflammasome pathway mediators
- retinal microglia
- complement cascade components
- Toll-like receptor pathway mediators
- cytokines
- Fas receptor
- Inhibitor
- inhibitor
- inhibit