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5mg |
ALG1001 has been discontinued due to commercial reasons.ALG1001 TFA, the trifluoroacetic acid salt of 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). ALG1001s potency relies onanti-angiogenesisandvitreolysisto 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.
ln 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). ALG1001s potency relies onanti-angiogenesisandvitreolysisto 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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ln 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.
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References |
US 20130129621 A1 20130523;WO 2012154894 A2 20121115.
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Molecular Formula |
C22H39N9O11STFA
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Molecular Weight |
751.68
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CAS # |
1307293-62-4
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SMILES |
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
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Synonyms |
Luminate; H-Gly-Arg-Gly-(L-Ala(SO3))-Thr-Pro-OH; ALG1001; ALG-1001; ALG 1001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO: >10 mM
Water:>10 mM
Ethanol:
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3304 mL | 6.6518 mL | 13.3035 mL | |
5 mM | 0.2661 mL | 1.3304 mL | 2.6607 mL | |
10 mM | 0.1330 mL | 0.6652 mL | 1.3304 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(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.