1. MAPK/ERK Pathway
  2. MAP4K
  3. GNE-495

GNE-495 

Cat. No.: HY-100343 Purity: 98.79%
Handling Instructions

GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.

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

GNE-495 Chemical Structure

GNE-495 Chemical Structure

CAS No. : 1449277-10-4

Size Price Stock Quantity
1 mg USD 80 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 450 In-stock
Estimated Time of Arrival: December 31
100 mg USD 750 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

GNE-495 is a potent and selective MAP4K4 inhibitor with an IC50 of 3.7 nM.

IC50 & Target

IC50: 3.7 nM (MAP4K4)[1]

In Vitro

GNE-495 is a potent and selective MAP4K4 inhibitor with efficacy in retinal angiogenesis. GNE-495 shows the best balance of MAP4K4 inhibition, permeability, microsomal stability, and cellular potency[1].

In Vivo

GNE-495 is administered intraperitoneally to neonatal mouse pups at high doses: 25 and 50 mg/kg. GNE-495 shows good in vivo profile in all species tested, with low clearances, moderate terminal half-lives, and reasonable oral exposure levels (F=37-47%)[1].

Molecular Weight

405.42

Formula

C₂₂H₂₀FN₅O₂

CAS No.

1449277-10-4

SMILES

O=C(C1=C2C=CC(C3=CC=CC(F)=C3)=NC2=C(N)N=C1)NC4CN(C(C5CC5)=O)C4

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 : 2.17 mg/mL (5.35 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4666 mL 12.3329 mL 24.6658 mL
5 mM 0.4933 mL 2.4666 mL 4.9332 mL
10 mM --- --- ---
*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: ≥ 0.22 mg/mL (0.54 mM); Clear solution

  • 2.

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

    Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution

  • 3.

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

    Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

Rats, Mice and Pups [1]
For the brain cassette study, three male Sprague-Dawley (SD) rats are dosed with intravenous (IV) bolus of six test compounds (e.g., GNE-495; 0.5 mg/kg). For the mouse PK study, female CD-1 mice are administered IV bolus doses of GNE-495 (1 mg/kg). In addition, female CD-1 mice are administered GNE-495 (5 mg/kg) via oral (PO) gavage. A dosing volume of 2 mL/kg is used for the rat brain cassette PK and 5 mL/kg is used for all other dosing. Animals are not fasted prior to dose administration, and water and food are available ad libitum. Following administration of the compound of interest, three blood samples (~60 μL) are collected at each time point from individual mice up to either 9 or 24 hours post-dose using a serial sampling approach. Immediately upon collection, the blood is mixed with K2EDTA and stored on ice or in a chilled Kryorack prior to centrifugation to obtain plasma. Within 1 hr of collection, blood samples are centrifuged at approximately 1000-2000× g for 10-15 min at 4°C, and plasma is harvested. The plasma samples are stored at -70 to -80°C until analysis. For neonate PK, 3-day old CD1 pups are injected with 25 mg/kg and 50 mg/kg GNE-495 intraperitoneally, blood samples are collected at the time points indicated, retinas are collected one hour post-dose and snap frozen in liquid nitrogen and stored at -80°C until analysis. Plasma and retinal lysate concentrations are determined by LC/MS/MS.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 98.79%

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GNE-495
Cat. No.:
HY-100343
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