1. GPCR/G Protein
  2. Leukotriene Receptor
  3. Gemilukast

Gemilukast (Synonyms: ONO-6950)

Cat. No.: HY-16780 Purity: 99.58%
Handling Instructions

Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.

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

Gemilukast Chemical Structure

Gemilukast Chemical Structure

CAS No. : 1232861-58-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 463 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3200 In-stock
Estimated Time of Arrival: December 31
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Description

Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively.

IC50 & Target[1]

CysLT1

1.7 nM (IC50, in human)

CysLT2

25 nM (IC50, in human)

In Vitro

Gemilukast is an orally active and potent dual cysteinyl leukotriene 1 and 2 receptors (CysLT1 and CysLT2) antagonist, with IC50s of 1.7, 25 nM for human CysLT1 and CysLT2, respectively[1]. Both Gemilukast (ONO-6950) and montelukast inhibit human CysLT1 receptor-mediated calcium response with IC50 values of 1.7 and 0.46 nM, respectively[2].

In Vivo

Gemilukast at 0.03 to 10 mg/kg, p.o. dose-dependently attenuates LTC4-induced bronchoconstriction with almost complete inhibition at 3 mg/kg. The inhibitory effect of Gemilukast on LTC4-induced bronchoconstriction is significantly stronger than that of montelukast at the dose of 1 mg/kg or more. Gemilukast (0.03 to 1 mg/kg, p.o.) dose-dependently attenuates LTD4-induced airway vascular hyperpermeability with complete inhibition at 0.3 mg/kg. Gemilukast at 0.1 to 3 mg/kg, p.o. dose-dependently inhibits OVA-induced bronchoconstriction. The inhibitory effect of Gemilukast at 3 mg/kg is significantly greater than that of montelukast alone and comparable to that of combination therapy with montelukast and BayCysLT2RA[2].

Molecular Weight

601.68

Formula

C₃₆H₃₇F₂NO₅

CAS No.

1232861-58-3

SMILES

O=C(O)CCCN1C(C)=C(CCCC(O)=O)C2=C1C(C#CC3=CC=C(OCCCCC4=CC=CC(F)=C4C)C=C3)=CC=C2F

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 : 250 mg/mL (415.50 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.6620 mL 8.3101 mL 16.6201 mL
5 mM 0.3324 mL 1.6620 mL 3.3240 mL
10 mM 0.1662 mL 0.8310 mL 1.6620 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: ≥ 2.08 mg/mL (3.46 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (3.46 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Gemilukast
Cat. No.:
HY-16780
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