Pegtarazimod
Based on 1 Customer Validation
Pegtarazimod (RLS-0071) is a dual-target anti-inflammatory peptide that exerts its effects by simultaneously regulating the complement system and neutrophil-associated inflammatory pathways. Pegtarazimod reduces ROS production both in vitro and in vivo, and decreases the level of neutrophil elastase, a marker of neutrophil extracellular traps (NETs), in vivo, thereby alleviating inflammatory responses. Pegtarazimod significantly improves the survival rate of mice in multiple in vivo models of acute graft-versus-host disease (aGVHD). Pegtarazimod inhibits the activation of the C1 complex, reduces the herpes zoster-like spread of herpes simplex virus type 1 skin infection, and improves the survival rate of infected mice. Pegtarazimod can be used in research related to acute graft-versus-host disease, acute pulmonary diseases, and skin herpes simplex virus type 1 infection.
For research use only. We do not sell to patients.
- Purity : 98.79%
- CAS No.: 2056232-82-5
- Formula: C122H224N20O46S2
- Molecular Weight:2771.32
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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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
Pegtarazimod reduces reactive oxygen species (ROS) production in an unspecified in vitro cell system[1].
Pegtarazimod (0.3-2.8 mg/mL) inhibits classical complement pathway activation in spiked normal human plasma in a dose-dependent manner, with 40% inhibition at 0.3 mg/mL and over 80% inhibition at 2.8 mg/mL[2].
Pegtarazimod (0.3-22 mg/mL; 30 min (neutrophil incubation at room temperature); 2 h (CCK-8 dye incubation at 37 °C)) increases the survival of purified human neutrophils ex vivo in a dose-dependent manner[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Pegtarazimod (14.4 mM (40 mg/mL); topical; twice daily; 14 days) formulated in HEC gel significantly reduces vesicle formation and promotes complete lesion healing by day 12 in ACVR-HSV-1-infected BALB/cJ mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/cJ (5-6-week-old female; HSV-1 scratch-inoculated)[3]
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Dosage:14.4 mM (40 mg/mL)
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Administration:topical; twice daily; 14 days
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Result:Achieved a 53.3% survival rate over 14 days.
Significantly reduced vesicle formation on days 9-14 post-infection.
Promoted lesion healing starting on day 9.
Significantly reduced averaged infection scores across 14 days.
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Animal Model:BALB/cJ (5-6-week-old female; ACVR-HSV-1 scratch-inoculated)[3]
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Dosage:14.4 mM (40 mg/mL)
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Administration:topical; twice daily; 14 days
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Result:Significantly reduced vesicle and erosion formation compared to DMSO-treated animals on days 3, 4, and 8-12 post-infection.
Significantly decreased vesicle formation compared to acyclovir-treated animals from days 7-12 post-infection.
Promoted complete healing of infected vesicles by day 12.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 2056232-82-5
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Appearance Solid
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Molecular Weight 2771.32
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Formula C122H224N20O46S2
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Synonyms
RLS-0071
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Sequence
Ile-Ala-Leu-Ile-Leu-Glu-Pro-Ile-Cys-Cys-Gln-Glu-Arg-Ala-Ala-{PEG24 acid}
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Sequence Shortening
IALILEPICCQERAA-{PEG24 acid}
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Shipping
Room temperature in continental US; may vary elsewhere.
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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 : 50 mg/mL (18.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (0.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (0.90 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Purity & Documentation
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 |
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| DMSO | 1 mM | 0.3608 mL | 1.8042 mL | 3.6084 mL | 9.0210 mL |
| 5 mM | 0.0722 mL | 0.3608 mL | 0.7217 mL | 1.8042 mL | |
| 10 mM | 0.0361 mL | 0.1804 mL | 0.3608 mL | 0.9021 mL | |
| 15 mM | 0.0241 mL | 0.1203 mL | 0.2406 mL | 0.6014 mL |
Pegtarazimod Related Classifications
HY-P10868 Related Classifications
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