ALG1001 TFA

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ALG1001 TFA
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Cat #: V0433 CAS #: 1307293-62-4 Purity ≥ 99%

Description: 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). 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.

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Molecular Weight (MW)751.68
Molecular FormulaC22H39N9O11S TFA
CAS No.1307293-62-4
Storage-20℃ for 3 years in powder form
Solubility In VitroDMSO: >10 mM
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.O=C(O)C(F)(F)F
SynonymsLuminate; H-Gly-Arg-Gly-(L-Ala(SO3))-Thr-Pro-OH; ALG1001; ALG-1001; ALG 1001
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.
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
1mM1.3304 mL6.6518 mL13.3035 mL26.6071 mL
5mM0.2661 mL1.3304 mL2.6607 mL5.3214 mL
10mM0.1330 mL0.6652 mL1.3304 mL2.6607 mL
20mM0.0665 mL0.3326 mL0.6652 mL1.3304 mL
The molarity calculator equation
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The dilution calculator equation
Concentration(start) × Volume(start) = Concentration(final) × Volume(final)

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Step Two: Enter the in vivo formulation
%DMSO + % + %Tween 80 + %ddH2O

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Working concentration: mg/ml;
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.
Method for preparing in vivo formulation: Take µL DMSO master liquid, next add µL PEG300, mix and clarify, next add µL Tween 80,mix and clarify, next add µL ddH2O,mix and clarify.
Note:
  • (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.