2. Protein Tyrosine Kinase/RTK
  3. VEGFR Ephrin Receptor
  4. UniPR1331

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.

For research use only. We do not sell to patients.

UniPR1331

UniPR1331 Chemical Structure

CAS No. : 1809170-59-9

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Based on 1 publication(s) in Google Scholar

UniPR1331 Related Antibodies

Top Publications Citing Use of Products

View All VEGFR Isoform Specific Products:

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VEGFR1/Flt-1 VEGFR2/KDR/Flk-1 VEGFR3/Flt-4

View All Ephrin Receptor Isoform Specific Products:

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EphA

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2][3].

IC50 & Target[1]

VEGFR2

62.2 μM (Kd)

EPHA2

3.3 μM (Kd)

In Vitro

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.

UniPR1331 Related Antibodies

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.
Molecular Weight

560.77

Formula

C35H48N2O4
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7833 mL 8.9163 mL 17.8326 mL
5 mM 0.3567 mL 1.7833 mL 3.5665 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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
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UniPR1331 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

UniPR13311809170-59-9UniPR 1331UniPR-1331VEGFREphrin ReceptorVascular endothelial growth factor receptorEph-ephrinAnti-angiogenesisAnti-cancerAnti-inflammationGliomaColitisEphAU87U251Inhibitorinhibitorinhibit

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