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Cat #: V0194 CAS #: 1307293-62-4 Purity ≥ 99%
Description: ALG1001 (discontinued, also known as Risuteganib and Luminate, developed by Allegro Ophthalmics) is a potent and selective small peptide with a sequence of Gly-Arg-Gly-Cya-Thr-Pro. It is an anti-integrin that acts as an inhibitor of angiogenesis and a modulator of integrin α2ß1, αV-ß 3, αV-ß 5. ALG-1001 is a first-in-class integrin peptide therapy which met the primary endpoint of vision non-inferiority to bevacizumab, an anti-vascular endothelial growth factor therapy (anti-VEGF), with 12-week durability in a population of patients with mostly chronic diabetic macular edema (DME). ALG1001's potency relies on anti-angiogenesis and vitreolysis to induce posterior vitreous detachment as well as vitreous liquefaction. ALG1001 was shown to be effective at regressing and inhibiting new blood vessel formation, as well as reducing vascular leakage to maintain and restore vision. ALG-1001 seems to be a strong player with different mechanisms of action that benefit patients who have been receiving chronic anti-VEGF therapy and those who are treatment naïve.
References: US 20130129621 A1 20130523; WO 2012154894 A2 20121115; Nebbioso M, et al. Therapeutic Approaches with Intravitreal Injections in Geographic Atrophy Secondary to Age-Related Macular Degeneration: Current Drugs and Potential Molecules. Int J Mol Sci. 2019 Apr 4;20(7). pii: E1693.
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Molecular Weight (MW) | 637.666 |
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Molecular Formula | C22H39N9O11S |
CAS No. | 1307293-62-4 |
Storage | -20℃ for 3 years in powder formrr |
-80℃ for 2 years in solvent | |
Solubility In Vitro | DMSO: >10 mMrr |
Water: >10 mMrr | |
Ethanol: N/A | |
SMILES Code | O=C(O)[C@H]1N(C([C@H]([C@H](O)C)NC([C@H](CS(=O)(O)=O)NC(CNC([C@H](CCCNC(N)=N)NC(CN) =O)=O)=O)=O)=O)CCC1 |
Synonyms | Luminate; H-Gly-Arg-Gly-(L-Ala(SO3))-Thr-Pro-OH; ALG1001; ALG-1001; ALG 1001; Risuteganib; developed by Allegro Ophthalmics |
Protocol | In Vitro | In vitro activity: ALG1001 (also known as Luminate, developed by Allegro Ophthalmics) is small peptide that acts as an inhibitor of angiogenesis and a modulator of integrin α2ß1, αV-ß 3, αV-ß 5. ALG-1001 is a first-in-class integrin peptide therapy which met the primary endpoint of vision non-inferiority to bevacizumab, an anti-vascular endothelial growth factor therapy (anti-VEGF), with 12-week durability in a population of patients with mostly chronic diabetic macular edema (DME). ALG1001's potency relies on anti-angiogenesis and vitreolysis to induce posterior vitreous detachment as well as vitreous liquefaction. ALG1001 was shown to be effective at regressing and inhibiting new blood vessel formation, as well as reducing vascular leakage to maintain and restore vision. ALG-1001 seems to be a strong player with different mechanisms of action that benefit patients who have been receiving chronic anti-VEGF therapy and those who are treatment naïve. Kinase Assay: ALG-1001 binds to the retinal pigment epithelium for several months. Cell Assay: ALG-1001 reduced vascular leakage. Other investigations have shown that the formulation affects only stressed retinal cells and has an anti-inflammatory effect, |
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In Vivo | ALG-1001 appeared to have 4 times more anti-angiogenic activity compared with aflibercept (Eylea, Regeneron Pharmaceuticals) in a murine model of retinopathy of prematurity. | |
Animal model | Murine |
Solvent volume to be added | Mass (the weight of a compound) | |||
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Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
1mM | 1.5682 mL | 7.8411 mL | 15.6822 mL | 31.3644 mL |
5mM | 0.3136 mL | 1.5682 mL | 3.1364 mL | 6.2729 mL |
10mM | 0.1568 mL | 0.7841 mL | 1.5682 mL | 3.1364 mL |
20mM | 0.0784 mL | 0.3921 mL | 0.7841 mL | 1.5682 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.