Pegtarazimod
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.
- CAS No.: 2056232-82-5
- Formula: C122H224N20O46S2
- Molecular Weight:2771.32
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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
- 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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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
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pegtarazimod Related Classifications
HY-P10868 Related Classifications
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