UniPR1331
Based on 1 Customer Validation
UniPR1331 is an orally active 3β-hydroxy-Δ5-choline acid derivative that inhibits Eph-ephrin interactions. UniPR1331 blocks the interaction of VEGFR2 with its natural ligand vascular endothelial growth factor and inhibits subsequent autophosphorylation, signaling, and pro-angiogenic activation of endothelial cells. UniPR1331 exhibits anti-angiogenesis, anti-cancer and anti-inflammation effects. UniPR1331 can be used for the researches of cancer and inflammation, such as glioma and colitis.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.57%
- No. CAS: 1809170-59-9
- Fòrmula: C35H48N2O4
- Peso molecular:560.77
-
Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
-
Solvente y solubilidad
- Pureza y Documentación
- Referencias
-
Help & FAQs
-
Bioactive Compound Library Max
HY-L181
-
Bioactive Compound Library
HY-L001
-
Immunology/Inflammation Compound Library
HY-L007
-
Kinase Inhibitor Library
HY-L009
-
Protein Tyrosine Kinase Compound Library
HY-L016
-
Anti-Cancer Compound Library
HY-L025
-
Differentiation Inducing Compound Library
HY-L038
-
Reprogramming Compound Library
HY-L039
-
Orally Active Compound Library
HY-L061
-
Anti-Breast Cancer Compound Library
HY-L074
-
Anti-Lung Cancer Compound Library
HY-L075
-
Anti-Pancreatic Cancer Compound Library
HY-L077
-
Anti-Blood Cancer Compound Library
HY-L079
-
Angiogenesis-Related Compound Library
HY-L088
-
Anti-Liver Cancer Compound Library
HY-L101
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Anti-Pulmonary Fibrosis Compound Library
HY-L125
-
Membrane Protein-targeted Compound Library
HY-L149
-
Membrane Receptor-targeted Compound Library
HY-L150
-
Highly Selective Inhibitors Library
HY-L158
-
Cytokine Inhibitors Library
HY-L161
-
Anti-Hematopathy Compound Library
HY-L171
-
Anti-Ovarian Cancer Compound Library
HY-L173
-
Multi-Target Compound Library
HY-L176
-
MCE Bioactive Compound Library
HY-L001V
-
Anti-Gastric Cancer Compound Library
HY-L184
-
Anti-Brain Cancer Compound Library
HY-L188
-
Protein Kinase Compound Library
HY-L196
-
Cell Proliferation Compound Library
HY-L201
-
High-Throughput Bioactive Compound Library
HY-L205
-
Posttranslational Modification Library
HY-L226
Ver todos los productos específicos de isoformas VEGFR
More
Actividad biológica
|
VEGFR2 62.2 μM (Kd) |
EPHA2 3.3 μM (Kd) |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HUVEC | IC50 |
2.9 μM
Compound: 10
|
Antiangiogenic activity in HUVEC assessed as inhibition of polygons formation after 15 hrs by microscopic analysis
Antiangiogenic activity in HUVEC assessed as inhibition of polygons formation after 15 hrs by microscopic analysis
|
[PMID: 26363867] |
| PC-3 | IC50 |
9.3 μM
Compound: 10
|
Antagonist activity at EphA2 receptor in human PC3 cells assessed as inhibition of ephrin-A1-induced protein phosphorylation after 20 mins by sandwich ELISA
Antagonist activity at EphA2 receptor in human PC3 cells assessed as inhibition of ephrin-A1-induced protein phosphorylation after 20 mins by sandwich ELISA
|
[PMID: 26363867] |
UniPR1331 (4-40 μM) specifically binds to human VEGFR2 (Kd = 62.2 μM) and EphA2 (Kd = 3.3 μM), and competes with VEGF for VEGFR2 binding (IC50 = 16 μM) and ephrin-A1 for EphA2 binding (IC50 = 4 μM)[1].
UniPR1331 (10-30 μM, 10 mins) inhibits VEGF-induced VEGFR2 phosphorylation (IC50 = 22 μM) in HUVECs[1].
UniPR1331 (10-30 μM, 24-48 h) inhibits VEGF-induced proliferation, migration and endothelial sprout formation in HUVECs[2].
UniPR1331 (3-30 μM, 24 h) maintains cells viability above 90% and inhibits TNFα release in mouse splenic lymphocytes treated with PMA (HY-18739) + Ionomycin (HY-13434)[2].
UniPR1331 inhibits tube formation of human umbilical vein endothelial cells (HUVEC) (IC50 = 2.9 μM) and human brain microvascular endothelial cells (HBMVEC) (IC50 = 3.9 μM)[3].
UniPR1331 (10 μM, 24 h) inhibits ephrin-A1-induced EphA2 phosphorylation in U87MG glioma cells and decreases EphA2 protein expression[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:U87MG glioma cells
-
Concentration:10 μM
-
Incubation Time:24 h
-
Result:Reduced EphA2 phosphorylation levels.
Reduced EphA2 protein expression.
UniPR1331 (10-25 mg/kg, p.o.) shows anti-inflammation effect in the TNBS-induced colitis model of C57BL/6 mice[2].
UniPR1331 (30 mg/kg, p.o., 5 days a week for 30 days) inhibits tumor growth and prolongs survival in CD1-nu/nu mice with U87MG glioma subcutaneous and intracranial xenografts[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:TNBS-induced colitis model of C57BL/6 mice[1]
-
Dosage:10 and 25 mg/kg
-
Administration:Intraperitoneally injection, twice a day from 8 h after TNBS-induced colitis, continued for 2 days
-
Result:Improved the Disease Activity Index (DAI, including weight loss, stool consistency, rectal bleeding).
Reduced the colonic macroscopic damage score (MS, decreasing strictures, adhesions, ulcers).
Restored colon length (inhibits colon shortening).
Reduced myeloperoxidase (MPO) activity in colon and lung (decreasing neutrophil infiltration).
Restored the splenic CD4+/CD8+ T cell ratio.
-
Animal Model:CD1-nu/nu mice with U87MG glioma subcutaneous and intracranial xenografts[3]
-
Dosage:30 mg/kg
-
Administration:Orally administration, 5 days a week for 30 days
-
Result:Reduced the final weight of tumor.
Prolonged the time to progression.
Decreased the Ki67 proliferation index.
Chemical Information
-
No. CAS 1809170-59-9
-
Appearance Solid
-
Peso molecular 560.77
-
Fòrmula C35H48N2O4
-
Color White to light yellow
-
SMILES
C[C@@]12[C@](CC[C@]2([H])[C@H](C)CCC(N[C@H](C(O)=O)CC3=CNC4=CC=CC=C34)=O)([H])[C@@]5([H])[C@@](CC1)([H])[C@@]6(C(C[C@H](CC6)O)=CC5)C
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
DMSO : 25 mg/mL (44.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
-
Ficha de datos (280 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
[1]. Rusnati M, et al. Cholenic acid derivative UniPR1331 impairs tumor angiogenesis via blockade of VEGF/VEGFR2 in addition to Eph/ephrin. Cancer Gene Ther. 2022 Jul;29(7):908-917. [Content Brief]
[2]. Giorgio C, et al. UniPR1331: Small Eph/Ephrin Antagonist Beneficial in Intestinal Inflammation by Interfering with Type-B Signaling. Pharmaceuticals (Basel). 2021 May 24;14(6):502. [Content Brief]
[3]. Festuccia C, et al. UniPR1331, a small molecule targeting Eph/ephrin interaction, prolongs survival in glioblastoma and potentiates the effect of antiangiogenic therapy in mice. Oncotarget. 2018 May 11;9(36):24347-24363. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7833 mL | 8.9163 mL | 17.8326 mL | 44.5816 mL |
| 5 mM | 0.3567 mL | 1.7833 mL | 3.5665 mL | 8.9163 mL | |
| 10 mM | 0.1783 mL | 0.8916 mL | 1.7833 mL | 4.4582 mL | |
| 15 mM | 0.1189 mL | 0.5944 mL | 1.1888 mL | 2.9721 mL | |
| 20 mM | 0.0892 mL | 0.4458 mL | 0.8916 mL | 2.2291 mL | |
| 25 mM | 0.0713 mL | 0.3567 mL | 0.7133 mL | 1.7833 mL | |
| 30 mM | 0.0594 mL | 0.2972 mL | 0.5944 mL | 1.4861 mL | |
| 40 mM | 0.0446 mL | 0.2229 mL | 0.4458 mL | 1.1145 mL |
UniPR1331 Related Classifications
HY-123927 Related Classifications
Powered by Bioz