1. Immunology/Inflammation
  2. Complement System
  3. Avacincaptad pegol

Avacincaptad pegol  (Synonyms: Izervay)

Cat. No.: HY-148457 Purity: 92.19%
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Avacincaptad pegol (Izervay) is a selective inhibitor targeting complement component C5, and is a pegylated ribonucleic acid aptamer. Avacincaptad pegol inhibits the cleavage of C5 into pro-inflammatory C5a and C5b, which forms the membrane attack complex (C5b-9), thereby reducing inflammatory cell recruitment and retinal cell damage. Avacincaptad pegol can slow the growth of geographic atrophy (GA) lesions and reduce the risk of persistent vision loss. Avacincaptad pegol can be used in research of geographic atrophy associated with age-related macular degeneration (AMD) and has been approved by the FDA.

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

Poly(oxy-1,2-ethanediyl), α-hydro-ω-methoxy-, 5′-ether with RNA ((2′-deoxy-2′-fluoro)C-Gm-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)C-G-(2′-deoxy-2′-fluoro)C-Gm-Gm-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-Am-Gm-Gm-(2′-deoxy-2′-fluoro)C-G-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-Gm-Am-Gm-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-Gm-Am-Gm-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)U-A-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-Gm-(2′-deoxy-2′-fluoro)C-Gm-(3′→3′)-dT) 5′-[6-[[(2,3-dihydroxypropoxy)carbonyl]amino]hexyl hydrogen phosphate] (2:1)

Avacincaptad pegol Chemical Structure

CAS No. : 1613641-69-2

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Based on 1 publication(s) in Google Scholar

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Description

Avacincaptad pegol (Izervay) is a selective inhibitor targeting complement component C5, and is a pegylated ribonucleic acid aptamer. Avacincaptad pegol inhibits the cleavage of C5 into pro-inflammatory C5a and C5b, which forms the membrane attack complex (C5b-9), thereby reducing inflammatory cell recruitment and retinal cell damage. Avacincaptad pegol can slow the growth of geographic atrophy (GA) lesions and reduce the risk of persistent vision loss. Avacincaptad pegol can be used in research of geographic atrophy associated with age-related macular degeneration (AMD) and has been approved by the FDA[1][2].

IC50 & Target

C5

 

In Vitro

Avacincaptad pegol exerts its complement inhibitory activity by specifically binding to complement component C5, inhibiting its cleavage into pro-inflammatory C5a and C5b, which forms the membrane attack complex (MAC), thus blocking the terminal steps of the complement cascade[1].
Avacincaptad pegol can inhibit the damage to retinal pigment epithelial (RPE) cells caused by the complement activation product C5b-9, reduce lysosomal overload and the release of pro-inflammatory factors, maintain the stability of RPE cell function, and is associated with the improvement of pathological processes related to age-related macular degeneration (AMD)[1].

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

In Vivo

In a male cynomolgus monkey (Macaca fascicularis) model, Avacincaptad pegol (1-1.5 mg/eye; intravitreal injection; once every 4 weeks for 4 doses) reduces the area of Ageographic atrophy in a sodium iodate-induced dry age-related macular degeneration model, but doesn't affect retinal or central macular thinning, nor does it induce choroidal neovascularization[2].

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

Animal Model: Cynomolgus macaques (Macaca fascicularis) (male, 2.9-6.6 kg, 3.4-5.0 years old) sodium iodate-induced dry age-related macular degeneration (AMD) with geographic atrophy (GA) model[2]
Dosage: Initial 1.5 mg/eye ubsequent doses adjusted to 1 mg/eye (phosphate-buffered saline)
Administration: 16 weeks
Result: The mean GA area in Avacincaptad pegol-treated eyes (11.4 ± 4.0 mm2) was reduced by approximately 36% compared with vehicle-treated eyes (18.9 ± 6.6 mm2), though the difference was not statistically significant.
Avacincaptad pegol did not alter the thinning of total retinal thickness or central macular thickness induced by sodium iodate. No choroidal neovascularization (CNV) was observed in either the treatment or vehicle group.
Choroidal capillary (CC) leakage under or around the macula was detected in both groups, with no statistically significant difference in the incidence of CC leakage between the two groups.
Clinical Trial
Molecular Weight

52603 (Approximately)

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Poly(oxy-1,2-ethanediyl), α-hydro-ω-methoxy-, 5′-ether with RNA ((2′-deoxy-2′-fluoro)C-Gm-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)C-G-(2′-deoxy-2′-fluoro)C-Gm-Gm-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-Am-Gm-Gm-(2′-deoxy-2′-fluoro)C-G-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-Gm-Am-Gm-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-Gm-Am-Gm-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)U-(2′-deoxy-2′-fluoro)U-A-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)C-(2′-deoxy-2′-fluoro)U-Gm-(2′-deoxy-2′-fluoro)C-Gm-(3′→3′)-dT) 5′-[6-[[(2,3-dihydroxypropoxy)carbonyl]amino]hexyl hydrogen phosphate] (2:1)

SMILES

[Avacincaptad pegol]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Purity & Documentation

Purity: 92.50%

References
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Avacincaptad pegol
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