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NE 52-QQ57 

Cat. No.: HY-101784
Handling Instructions

NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM. Anti-inflammatory activities.

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

NE 52-QQ57 Chemical Structure

NE 52-QQ57 Chemical Structure

CAS No. : 1401728-56-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 495 In-stock
Estimated Time of Arrival: December 31
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 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3300 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Description

NE 52-QQ57 is a selective, and orally available GPR4 antagonist with an IC50 of 70 nM[1]. Anti-inflammatory activities[1].

IC50 & Target

IC50: 70 nM (GPR4)[1].

In Vivo

NE 52-QQ57 (compound 13) shows a significant anti-inflammatory effect in the rat antigen induced arthritis model after oral administration at 30 mg/kg bid for 20 days[1]. NE 52-QQ57 (30 mg/kg bid po for 4 days) also prevents angiogenesis in the mouse chamber model as well as pain as demonstrated in the rat complete Freund’s adjuvant model[1].

Animal Model: Female FVB mice (8-10 weeks)[1]
Dosage: 30 mg/kg bid po
Administration: Oral, 4 days, bid
Result: Treatment with GPR4 antagonist 3 at 30 mg/ kg po bid starting on day 0, the day of the chamber implantation, showed a statistically significant reduction (46.8 ± 10.6%) of tissue growth by day 4. The blood levels of 13 on day 4 at 2 and 16 h after compound application in this model were 9.03 ± 2.87 and 0.09 ± 0.06 μM[1].
Animal Model: Male Wistar Han rats[1]
Dosage: 3, 10, and 30 mg/kg
Administration: Oral, 20 days, bid
Result: GPR4 antagonist 3 displays not only higher exposures in the rat AIA but also lower plasma protein binding in rat (95%)[1].
Solvent & Solubility
In Vitro: 

DMSO : 41.67 mg/mL (100.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4008 mL 12.0042 mL 24.0085 mL
5 mM 0.4802 mL 2.4008 mL 4.8017 mL
10 mM 0.2401 mL 1.2004 mL 2.4008 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.08 mg/mL (4.99 mM); Clear solution

References
Molecular Weight

416.52

Formula

C₂₄H₂₈N₆O

CAS No.

1401728-56-0

SMILES

CCC1=NN(C(C)=CC(C)=N2)C2=C1CC3=CC=C(C4=NN=C(C5CCNCC5)O4)C=C3

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

Room temperature in continental US; may vary elsewhere

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Product Name:
NE 52-QQ57
Cat. No.:
HY-101784
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NE 52-QQ57

Cat. No.: HY-101784