Montelukast (Synonyms: MK-476) |
رقم الكتالوجGC52105
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يعد مونتيلوكاست (القاعدة الحرة MK0476) مضادًا قويًا وانتقائيًا ونشطًا عن طريق الفم لمستقبلات السيستينيل ليكوترين 1 (CysLT1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 158966-92-8
Sample solution is provided at 25 µL, 10mM.
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Montelukast is a cysteinyl leukotriene 1 (CysLT1) receptor antagonist (IC50 = 4.9 nM in HEK293 cell membranes expressing the human receptor).1 It is selective for CysLT1 over CysLT2 receptors (IC50 = >10,000 nM in COS-7 cell membranes expressing the human receptor).2 Montelukast inhibits bronchoconstriction induced by leukotriene D4 in anesthetized guinea pigs (ED50 = 69 nmol/kg, p.o.).3 It inhibits ovalbumin-induced airway hyperresponsiveness and increases in the number of total cells and eosinophils in bronchoalveolar lavage fluid (BALF) in a mouse model of allergic asthma when administered at doses of 3 and 10 mg/kg.4 Formulations containing montelukast have been used in the treatment of asthma, allergic rhinitis, and exercise-induced bronchoconstriction.
1.Sarau, H.M., Ames, R.S., Chambers, J., et al.Identification, molecular cloning, expression, and characterization of a cysteinyl leukotriene receptorMol. Pharmacol.56(3)657-663(1999) 2.Heise, C.E., O’Dowd, B.F., Figueroa, D.J., et al.Characterization of the human cysteinyl leukotriene 2 receptorJ. Biol. Chem.275(39)30531-30536(2000) 3.CabrÉ, F., Carabaza, A., GarcÍa, A.M., et al.Pharmacological profile of MEN91507, a new CysLT1 receptor antagonistEur. J. Pharmacol.451(3)317-326(2002) 4.Eum, S.Y., Maghni, K., Hamid, Q., et al.Involvement of the cysteinyl-leukotrienes in allergen-induced airway eosinophilia and hyperresponsiveness in the mouseAm. J. Respir. Cell Mol. Biol.28(1)25-32(2003)
| Cas No. | 158966-92-8 | SDF | |
| المرادفات | MK-476 | ||
| Canonical SMILES | CC(C)(O)C(C=CC=C1)=C1CC[C@H](C2=CC(/C=C/C3=NC4=C(C=CC(Cl)=C4)C=C3)=CC=C2)SCC5(CC5)CC(O)=O | ||
| Formula | C35H36ClNO3S | M.Wt | 586.2 |
| الذوبان | DMF: 2 mg/ml,DMSO: 2 mg/ml,Ethanol: insol,PBS (pH 7.2): insol | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.7059 mL | 8.5295 mL | 17.059 mL |
| 5 mM | 341.2 μL | 1.7059 mL | 3.4118 mL |
| 10 mM | 170.6 μL | 853 μL | 1.7059 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)