| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
The peptide specifically targets VEGFR2 (also known as KDR/flk-1). By binding to VEGFR2, it acts as a competitive antagonist, blocking the interaction of VEGF with its receptor and thereby inhibiting downstream signaling cascades involved in angiogenesis.
|
|---|---|
| ln Vitro |
ATWLPPR Peptide selectively inhibits human endothelial cell proliferation in vitro. It completely inhibits VEGF binding to KDR, preventing VEGF-induced endothelial cell activation and subsequent proliferation, migration, and tube formation in a concentration-dependent manner without affecting non-endothelial cell types.
|
| ln Vivo |
The peptide completely abrogates VEGF-induced angiogenesis in vivo. By blocking VEGFR2 signaling, it effectively prevents new blood vessel formation in various animal models. This activity is confirmed in the chick chorioallantoic membrane (CAM) assay and Matrigel plug assays, where it reduces vascular infiltration.
|
| Enzyme Assay |
In a non-cellular assay, the peptide is tested using a competition ELISA or SPR. Recombinant VEGFR2/KDR protein is immobilized on a sensor chip or plate. Varying concentrations of the ATWLPPR peptide are co-incubated with labeled VEGF, and the ability of the peptide to disrupt VEGF-receptor binding is measured, quantifying the IC50 for inhibition of binding.
|
| Cell Assay |
The primary in vitro cellular assay involves culturing human umbilical vein endothelial cells (HUVECs). Cells are treated with VEGF to stimulate proliferation, and ATWLPPR peptide is added at various concentrations (typically 0-100 microM). Endothelial cell proliferation is quantified by [3H]-thymidine incorporation or MTT assay after 48-72 hours. Tube formation assays on Matrigel can also be used to assess inhibition of capillary network development.
|
| Animal Protocol |
In vivo angiogenesis is assessed using a mouse Matrigel plug assay. Matrigel mixed with VEGF and the ATWLPPR peptide (or vehicle) is injected subcutaneously into mice. After 7-14 days, the plugs are excised and hemoglobin content is measured as a marker of neovascularization. Alternatively, a chick CAM assay can be used, where the peptide is applied to the CAM, and the reduction of VEGF-induced vessel branching is scored.
|
| ADME/Pharmacokinetics |
PK data for this specific peptide is limited. As a peptide, systemic bioavailability after oral delivery is very low due to gastrointestinal degradation. When administered intravenously or subcutaneously, it is rapidly cleared from circulation via proteolysis and renal filtration, typically exhibiting a short half-life (in the order of minutes to a few hours).
|
| Toxicity/Toxicokinetics |
As a short peptide, ATWLPPR is generally considered to have low acute toxicity, though no detailed toxicology reports are available for this specific sequence. The primary risk is associated with its pharmacological activity, namely the potential for off-target inhibition of physiological angiogenesis in healthy tissues if used systemically.
|
| Additional Infomation |
The peptide consists of 7 amino acids (Ala-Thr-Trp-Leu-Pro-Pro-Arg) with a molecular weight of 839.98. It is a specific VEGFR2/KDR heptapeptide antagonist discovered through phage display screening. It is intended for research use only to study angiogenesis mechanisms and is not approved for clinical therapy.
|
| Molecular Formula |
C40H61N11O9
|
|---|---|
| Molecular Weight |
839.98064
|
| Exact Mass |
839.465
|
| CAS # |
272121-15-0
|
| Related CAS # |
ATWLPPR Peptide TFA
|
| PubChem CID |
9854089
|
| Appearance |
White to off-white solid powder
|
| LogP |
-2.7
|
| Hydrogen Bond Donor Count |
10
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
20
|
| Heavy Atom Count |
60
|
| Complexity |
1580
|
| Defined Atom Stereocenter Count |
8
|
| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CC1=CNC2=CC=CC=C21)C(=O)N[C@@H](CC(C)C)C(=O)N3CCC[C@H]3C(=O)N4CCC[C@H]4C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)[C@H](C)N)O
|
| InChi Key |
MKSPBYRGLCNGRC-OEMOKZHXSA-N
|
| InChi Code |
InChI=1S/C40H61N11O9/c1-21(2)18-29(48-34(54)28(19-24-20-45-26-11-6-5-10-25(24)26)47-36(56)32(23(4)52)49-33(53)22(3)41)37(57)51-17-9-14-31(51)38(58)50-16-8-13-30(50)35(55)46-27(39(59)60)12-7-15-44-40(42)43/h5-6,10-11,20-23,27-32,45,52H,7-9,12-19,41H2,1-4H3,(H,46,55)(H,47,56)(H,48,54)(H,49,53)(H,59,60)(H4,42,43,44)/t22-,23+,27-,28-,29-,30-,31-,32-/m0/s1
|
| Chemical Name |
(2S)-2-[[(2S)-1-[(2S)-1-[(2S)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-aminopropanoyl]amino]-3-hydroxybutanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-4-methylpentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-5-(diaminomethylideneamino)pentanoic acid
|
| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 Vitro) |
DMSO: 100 mg/mL (119.05 mM)
|
|---|---|
| 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 | 1.1905 mL | 5.9525 mL | 11.9050 mL | |
| 5 mM | 0.2381 mL | 1.1905 mL | 2.3810 mL | |
| 10 mM | 0.1191 mL | 0.5953 mL | 1.1905 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
