CAS NO: | 1307293-62-4 |
规格: | ≥98% |
Molecular Weight (MW) | 751.68 |
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Formula | C22H39N9O11S TFA |
CAS No. | 1307293-62-4 (free base) |
Storage | -20℃ for 3 years in powder form |
-80℃ for 2 years in solvent | |
Solubility (In vitro) | DMSO:>10 mM |
Water: >10 mM | |
Ethanol: | |
Chemical Name | L-Proline, glycyl-L-arginylglycyl-3-sulfo-L-alanyl-L-threonyl- Trifluoroacetic acid |
Synonyms | Luminate; H-Gly-Arg-Gly-(L-Ala(SO3))-Thr-Pro-OH; ALG1001; ALG-1001; ALG 1001 |
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.O=C(O)C(F)(F)F |
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 naive. 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 | |
Formulation & Dosage | |
References | US 20130129621 A1 20130523; WO 2012154894 A2 20121115. |