| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg | |||
| Other Sizes |
| Targets |
NRP1 antagonist 2 selectively targets Neuropilin-1 (NRP1), a cell surface receptor involved in angiogenesis, tumor progression, and neuronal guidance. By blocking NRP1, it disrupts VEGF-A165 signaling and related downstream pathways.
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|---|---|
| ln Vitro |
Detailed in vitro potency and activity characterization is primarily qualitative. As an antagonist, it blocks the interaction between NRP1 and its ligands, such as VEGF-A165. This inhibition has potential applications in cancer research focused on angiogenesis.
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| ln Vivo |
Dedicated in vivo efficacy studies for this specific antagonist are not extensively documented in standard profiles. As a research tool for NRP1, it has shown potential in reducing angiogenesis and tumor progression in preclinical models, but detailed study data is not widely available.
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| Enzyme Assay |
Binding affinity to NRP1 is typically measured by Surface Plasmon Resonance (SPR) or ELISA-based competition assays using the b1 domain of NRP1. Functional antagonism is assessed by evaluating the inhibition of VEGF-A165-induced signaling in cellular assays, such as measuring VEGFR2 phosphorylation.
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| Cell Assay |
Endothelial cells (e.g., HUVECs) are treated with NRP1 antagonist 2 in the presence or absence of VEGF-A165. Cell migration and tube formation assays are performed to assess functional angiogenesis. NRP1 downstream signaling is assessed by Western blot for phosphorylated VEGFR2 and ERK.
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| Animal Protocol |
Dedicated in vivo protocols for NRP1 antagonist 2 would typically involve murine xenograft tumor models. The compound would be administered via intraperitoneal injection. Tumor angiogenesis would be assessed by CD31 immunostaining of tumor sections. Tumor growth and metastasis would be monitored.
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| ADME/Pharmacokinetics |
Detailed PK parameters for NRP1 antagonist 2 are not extensively documented. As a research compound with a molecular weight of 456.97 g/mol, its solubility and permeability properties require further investigation for in vivo applications.
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| Toxicity/Toxicokinetics |
Toxicological data for NRP1 antagonist 2 is not available in standard profiles. As a research chemical not intended for clinical development, comprehensive toxicology studies have not been performed. Standard laboratory safety precautions apply.
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| References | |
| Additional Infomation |
The compound is fully non-peptidic, which is an advantage over peptide-based NRP1 antagonists for potential oral bioavailability and stability. It is strictly a research tool for studying the role of Neuropilin-1 in cancer and angiogenesis. It is not a clinical drug.
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| Molecular Formula |
C20H17CLN6OS2
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|---|---|
| Molecular Weight |
456.971579313278
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| Exact Mass |
456.059
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| CAS # |
483289-96-9
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| PubChem CID |
996896
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| Appearance |
White to off-white solid powder
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| LogP |
4.7
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
30
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| Complexity |
569
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCC1=NN=C(S1)NC(=O)CSC2=NN=C(N2C3=CC(=CC=C3)Cl)C4=CC=CC=C4
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| InChi Key |
CTRUPGGFDZUABL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H17ClN6OS2/c1-2-17-23-25-19(30-17)22-16(28)12-29-20-26-24-18(13-7-4-3-5-8-13)27(20)15-10-6-9-14(21)11-15/h3-11H,2,12H2,1H3,(H,22,25,28)
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| Chemical Name |
2-[[4-(3-chlorophenyl)-5-phenyl-1,2,4-triazol-3-yl]sulfanyl]-N-(5-ethyl-1,3,4-thiadiazol-2-yl)acetamide
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| HS Tariff Code |
2934.99.9001
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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: ~100 mg/mL (~218.8 mM; with ultrasonication and warming by heating to 80°C)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (5.47 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1883 mL | 10.9416 mL | 21.8833 mL | |
| 5 mM | 0.4377 mL | 2.1883 mL | 4.3767 mL | |
| 10 mM | 0.2188 mL | 1.0942 mL | 2.1883 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.
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