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Tipelukast

SKU: orb1707142

Description

Tipelukast (KCA 757) is an orally active leukotriene receptor antagonist studied for asthma. Its anti-inflammatory properties reduce fibrosis by downregulating TIMP-1 and type I collagen, as demonstrated in relevant in vivo and in vitro models of airway inflammation and remodeling.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number125961-82-2
MW530.67
Purity>99.99% (May vary between batches)
FormulaC29H38O7S
SMILESCCCc1c(O)c(ccc1SCCCOc1ccc(C(C)=O)c(OCCCC(O)=O)c1CCC)C(C)=O
TargetLeukotriene Receptor
SolubilityEthanol:< 1 mg/mL

Bioactivity

Target IC50
LTD4:6.41 (pA2,guinea-pigs)|LTE4:6.45 (pA2,guinea-pigs)|LTD4 receptor:2.3 μmol (pulmonary cell membrane)
In Vivo
Fifteen minutes after an aerosolized antigen challenge, and inhaled 5 minutes later into the guinea pigs, Tipelukast significantly modifies the bronchoconstriction induced by UNDW. Intravenous administration of Tipelukast (1 and 5 mg/kg) 15 minutes after antigen challenge dose-dependently reduces propranolol-induced bronchoconstriction (PIB) in guinea-pigs.
In Vitro
Tipelukast inhibits the binding of [3H] LTD4 to the LTD4 receptors on the pulmonary cell membrane of guinea-pigs (IC50 = 2.3 μmol).

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

MN 001, MN001, MN-001, LTE4, LTD4, KCA 757, KCA757, KCA-757, LeukotrieneReceptor, leukotriene receptor, Leukotriene Receptor, Tipelukast

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Key Properties

No computed properties available.

Protocol Information

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1 mg
$ 210.00
5 mg
$ 440.00
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