Art. -Nr.: HY-123927

UniPR1331

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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.

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Reinheit: 98.57%
CAS. Nr.: 1809170-59-9
Formel: C₃₅H₄₈N₂O₄
Molecular Weight:560.77

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

UniPR1331 Chemical Structure

CAS. Nr.: 1809170-59-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

VEGFR2

62.2 μM (Kd)

EPHA2

3.3 μM (Kd)

Alle VEGFR Isoform-spezifische Produkte anzeigen :

Alle Ephrin Receptor Isoform-spezifische Produkte anzeigen :

EphB
EphA

Cellular Effect

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]

In Vitro

UniPR1331 (4-40 μM) specifically binds to human VEGFR2 (K_d = 62.2 μM) and EphA2 (K_d = 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.

Western Blot Analysis^[3]

Cell Line:

U87MG glioma cells
Concentration:

10 μM
Incubation Time:

24 h
Result:

Reduced EphA2 phosphorylation levels.
Reduced EphA2 protein expression.

In Vivo

UniPR1331 (50 μM, perivitelline space injection, 48 h post-fertilization) reduces the number and total length of ectopic vessel sprouts in the zebrafish yolk membrane angiogenesis model injected with U251 glioblastoma cells^[1].
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

CAS. Nr. 1809170-59-9
Appearance Solid
Molecular Weight 560.77
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7833 mL

8.9163 mL

17.8326 mL

5 mM

0.3567 mL

1.7833 mL

3.5665 mL

10 mM

0.1783 mL

0.8916 mL

1.7833 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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UniPR1331

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Differentiation Inducing Compound Library

Reprogramming Compound Library

Orally Active Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Pancreatic Cancer Compound Library

Anti-Blood Cancer Compound Library

Angiogenesis-Related Compound Library

Anti-Liver Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Anti-Pulmonary Fibrosis Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Cytokine Inhibitors Library

Anti-Hematopathy Compound Library

Anti-Ovarian Cancer Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Anti-Gastric Cancer Compound Library

Anti-Brain Cancer Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Alle VEGFR Isoform-spezifische Produkte anzeigen

Alle Ephrin Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

UniPR1331 Related Classifications

HY-123927 Related Classifications