1. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  2. Fatty Acid Synthase (FASN) Apoptosis Interleukin Related Toll-like Receptor (TLR) NOD-like Receptor (NLR) Caspase
  3. Xelafaslatide

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.

For research use only. We do not sell to patients.

Custom Peptide Synthesis

Xelafaslatide

Xelafaslatide Chemical Structure

CAS No. : 2040964-58-5

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Description

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[1].

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.

Apoptosis Analysis[1]

Cell Line: murine A20 B lymphoma cells
Concentration: 15 μM, 30 μM, 60 μM, 125 μM
Incubation Time: 4 h (with mFasL-VP); overnight (with 3H-thymidine)
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

Xelafaslatide (2 μg/1 μL; intravitreal administration; single dose) achieves complete neuroprotection of retinal ganglion cells and optic nerve axons, inhibits retinal microglial activation, and blocks the induction of glaucoma-related inflammatory genes in a microbead-induced mouse glaucoma model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J wild-type (8-week-old, glaucoma model induced by anterior chamber injection of 15-μm polystyrene microbeads)[1]
Dosage: 2 μg per 1 μL
Administration: intravitreal; single dose (day 0, prior to microbead injection)
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.
Molecular Weight

1461.66

Formula

C71H100N18O16

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

His-His-Ile-Tyr-Leu-Gly-Ala-Val-Asn-Tyr-Ile-Tyr-NH2

Sequence Shortening

HHIYLGAVNYIY-NH2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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)

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.6842 mL 3.4208 mL 6.8415 mL
5 mM 0.1368 mL 0.6842 mL 1.3683 mL
View the 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.

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  • Dilution Calculator

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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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (1.71 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: 99.88%

References

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
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
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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Xelafaslatide
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