| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
VEGF165 isoform. Pegaptanib is a pegylated modified oligonucleotide that adopts a three-dimensional conformation, allowing it to bind specifically to the 165-amino acid isoform of VEGF, while sparing the physiological VEGF121 isoform.
|
|---|---|
| ln Vitro |
Pegaptanib also prevents phospholipase Cγ and VEGFR2 from being phosphorylated by VEGF165, and it also stops VEGF165-induced calcium mobilization in human umbilical vein endothelial cells[1].
Pegaptanib binds to VEGF165 with high affinity and specificity, thereby inhibiting its interaction with VEGF receptors (VEGFR1 and VEGFR2). This inhibition blocks the primary pathological processes responsible for vision loss in wet AMD: angiogenesis (new blood vessel formation) and vascular permeability. |
| ln Vivo |
Pegaptanib has been validated in large Phase 3 clinical trials (VISION studies). In patients with wet AMD, intravitreal injections (0.3 mg) once every six weeks resulted in a significant reduction in the risk of moderate vision loss compared to sham injections. It effectively reduces central retinal thickness and leakage.
|
| Enzyme Assay |
Cell-free binding assays are performed using a nitrocellulose filter binding assay or surface plasmon resonance (SPR). Radiolabeled or biotinylated VEGF165 is incubated with increasing concentrations of pegaptanib. The percentage of bound VEGF165 is quantified, and the equilibrium dissociation constant (Kd) is calculated to determine binding affinity.
|
| Cell Assay |
Human umbilical vein endothelial cells (HUVECs) are used to assess the biological activity of pegaptanib. Cells are plated in a Matrigel matrix to promote tube formation. When stimulated with VEGF165, the cells form capillary-like tube structures. Pegaptanib is added to the culture medium to block this VEGF-induced angiogenesis, and the reduction in tube formation is quantified microscopically.
|
| Animal Protocol |
The standard animal model for choroidal neovascularization (CNV) is the laser-induced CNV model in rats or non-human primates. After laser photocoagulation, animals receive intravitreal injections of pegaptanib. After two weeks, the animals are sacrificed, and the CNV area is measured in choroidal flat mounts stained with a fluorescent dye (e.g., isolectin B4).
|
| ADME/Pharmacokinetics |
Pharmacokinetic data are specific to intravitreal administration. Following injection (0.3 mg/eye), pegaptanib is detected in the vitreous humor, where it has a half-life of approximately 3-4 days. Systemic exposure is minimal. It is primarily eliminated unchanged in the urine via renal filtration. The elimination half-life from the systemic circulation is about 10 days.
|
| Toxicity/Toxicokinetics |
In clinical trials, pegaptanib had a favorable safety profile. The most common adverse events were eye-related, such as vitreous floaters and eye pain. Unlike other anti-VEGF agents, pegaptanib carries a lower risk of systemic adverse events (e.g., hypertension, thromboembolism) due to its selectivity for VEGF165. Its safety has been well-characterized.
|
| References | |
| Additional Infomation |
See also: Pegaptanib Sodium (note moved to).
Other information: Pegaptanib sodium (Macugen) was approved by the FDA in 2004. It is a 28-nucleotide RNA aptamer covalently linked to two branched 20-kDa polyethylene glycol moieties. It was the first aptamer to be approved as a therapeutic agent. It is administered as a 0.3 mg dose once every six weeks via intravitreal injection. |
| Molecular Formula |
C22H44N3O10P
|
|---|---|
| Molecular Weight |
541.57262802124
|
| Exact Mass |
535.227
|
| CAS # |
222716-86-1
|
| PubChem CID |
138398605
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
3
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
22
|
| Heavy Atom Count |
35
|
| Complexity |
642
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
P(C([H])([H])[H])(=O)(O[H])OC([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C([C@]([H])(C([H])([H])C([H])([H])C([H])([H])C([H])([H])N([H])C(=O)OC([H])([H])C([H])([H])OC([H])([H])[H])N([H])C(=O)OC([H])([H])C([H])([H])OC([H])([H])[H])=O
|
| InChi Key |
BXHPKXLPCWQCHL-LMOVPXPDSA-M
|
| InChi Code |
InChI=1S/C20H40N3O10P.Na/c1-29-13-15-31-19(25)22-11-7-5-9-17(23-20(26)32-16-14-30-2)18(24)21-10-6-4-8-12-33-34(3,27)28;/h17H,4-16H2,1-3H3,(H,21,24)(H,22,25)(H,23,26)(H,27,28);/q;+1/p-1/t17-;/m0./s1
|
| Chemical Name |
sodium;(2S)-N-[5-[hydroxy(methyl)phosphoryl]oxypentyl]-2,6-bis(2-methoxyethoxycarbonylamino)hexanimidate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8465 mL | 9.2324 mL | 18.4648 mL | |
| 5 mM | 0.3693 mL | 1.8465 mL | 3.6930 mL | |
| 10 mM | 0.1846 mL | 0.9232 mL | 1.8465 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
