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

Gemilukast  (Synonyms: ONO-6950)

Cat. No.: HY-16780 Purity: 99.50%
COA 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
Solution
10 mM * 1 mL in DMSO USD 463 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 463 In-stock
Solid
5 mg USD 350 In-stock
10 mg USD 600 In-stock
50 mg USD 1800 In-stock
100 mg USD 3200 In-stock
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500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

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LTB4 LTC4 LTD4/CysLT1 LTE4 CysLT2 CysLT1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

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

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

601.68

Appearance

Solid

Formula

C36H37F2NO5
CAS No.
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 available by MCE.
Purity & Documentation
References
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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.

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This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
C1   V1   C2   V2

Keywords:

Gemilukast1232861-58-3ONO-6950ONO6950ONO 6950Leukotriene ReceptorInhibitorinhibitorinhibit

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