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ALG1001 (Risuteganib; Luminate)

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ALG1001 (Risuteganib; Luminate)
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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
Molecular FormulaC22H39N9O11S
CAS No.1307293-62-4
Storage-20℃ for 3 years in powder formrr
-80℃ for 2 years in solvent
Solubility In VitroDMSO: >10 mMrr
Water: >10 mMrr
Ethanol: N/A
SMILES CodeO=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
SynonymsLuminate; H-Gly-Arg-Gly-(L-Ala(SO3))-Thr-Pro-OH; ALG1001; ALG-1001; ALG 1001; Risuteganib; developed by Allegro Ophthalmics
ProtocolIn VitroIn 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,
In VivoALG-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 modelMurine
These protocols are for reference only. InvivoChem does not independently validate these methods.
Preparing Stock Solutions
Solvent volume to be added Mass (the weight of a compound)
Mother liquor concentration 1mg5mg10mg20mg
1mM1.5682 mL7.8411 mL15.6822 mL31.3644 mL
5mM0.3136 mL1.5682 mL3.1364 mL6.2729 mL
10mM0.1568 mL0.7841 mL1.5682 mL3.1364 mL
20mM0.0784 mL0.3921 mL0.7841 mL1.5682 mL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid concentration mg/mL) ,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
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