1. Immunology/Inflammation
  2. Complement System
  3. EG01377 dihydrochloride

EG01377 dihydrochloride 

Cat. No.: HY-112151A Purity: 98.21%
Handling Instructions

EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects.

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

EG01377 dihydrochloride Chemical Structure

EG01377 dihydrochloride Chemical Structure

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5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2100 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3350 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

EG01377 dihydrochloride is a potent, bioavailable and selective inhibitor of neuropilin-1 (NRP1), with a Kd of 1.32 μM, and IC50s of 609 nM for both NRP1-a1 and NRP1-b1. EG01377 dihydrochloride has antiangiogenic, antimigratory, and antitumor effects[1].

IC50 & Target

IC50: 609 nM (NRP1-a1 and NRP1-b)[1]

In Vitro

EG01377 (3-30 μM; 30 minutes) inhibits vascular endothelial growth factor A (VEGF-A) stimulated tyrosine phosphorylation of VEGF-R2/KDR[1].
EG01377 (30 μM) is able to significantly reduce HUVEC cell migration in response to VEGFA[1].
EG01377 (30 μM; 5 days) can delay the VEGF-induced wound closure[1].
EG01377 (30 μM) reduces network area, length, and branching points[1].
EG01377 (30 μM; 7 days) reduces VEGF-induced angiogenesis[1].
EG01377 (30 μM; 7 days) in combination with VEGFA reduces A375P (malignant melanoma) spheroid outgrowth[1].
EG01377 (500 nM; 2 hours) blocks the production of transforming growth factor beta (TGFβ) by Nrp1+ regulatory T-cell SMAD3/AKT (Tregs) in the presence of tumor cell-derived factors[1].

Western Blot Analysis[1]

Cell Line: Human umbilical vein endothelial cells (HUVECs)
Concentration: 3, 10, 30 μM
Incubation Time: 30 minutes
Result: Inhibited VEGF-A stimulated tyrosine phosphorylation of VEGF-R2/KDR with an IC50 of 30 μM.
In Vivo

EG01377 (2 mg/kg; i.v.) exhibits an encouraging half-life of 4.29 h, sufficient to sustain once per day dosing in mice[1].

Animal Model: 6-8 week-old BABL/c female mice[1]
Dosage: 2 mg/kg (Pharmacokinetic Analysis)
Administration: I.v. administration
Result: The half time (T1/2) of 4.29 h.
Molecular Weight

659.60

Formula

C₂₆H₃₂Cl₂N₆O₆S₂

SMILES

O=S(C1=CC(C2=CC=C(CN)C=C2)=CC3=C1OCC3)(NC4=C(C(N[[email protected]@H](CCC/N=C(N)/N)C(O)=O)=O)SC=C4)=O.Cl.Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Solvent & Solubility
In Vitro: 

DMSO : 200 mg/mL (303.21 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.5161 mL 7.5804 mL 15.1607 mL
5 mM 0.3032 mL 1.5161 mL 3.0321 mL
10 mM 0.1516 mL 0.7580 mL 1.5161 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 5 mg/mL (7.58 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

EG01377EG 01377EG-01377Complement Systemneuropilin-1NRP1NRP1-a1NRP1-b1antiangiogenicantimigratoryantitumorInhibitorinhibitorinhibit

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EG01377 dihydrochloride
Cat. No.:
HY-112151A
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