Description
Iralukast is a cysteinyl-leukotriene antagonist (CysLT) with a pKi of 7.8 for CysLT1. Both Iralukast and CGP 57698 are able to compete for the two sites labelled by [3H]-LTD4. As in all the G-protein coupled receptors, Iralukast and CGP 57698 do not discriminate between the high and the low affinitystates of the CysLT receptor labelled by LTD4 (Ki1=Ki2=16.6 nM±36% CV and Ki1=Ki2=5.7 nM±19% CV, respectively). Iralukast, displays a slow bindingkinetic, because preincubation (15 min) increases its antagonist potency. Iralukast and CGP 57698 antagonize LTD4-induced contraction of humanbronchi, with pA2 values of 7.77±4.3% CV and 8.51±1.6% CV, respectively, and slopes not significantly different from unity. . Magnus B?ck, et al. Update on leukotriene, lipoxin and oxoeicosanoid receptors: IUPHAR Review 7. Br J Pharmacol. 2014 Aug; 171(15): 3551-3574. . Valérie Capra, et al. Pharmacological characterization of the cysteinyl-leukotrieneantagonists CGP 45715A (iralukast) and CGP 57698 in human airways in vitro.Br J Pharmacol. 1998 Feb; 123(3): 590-598.
Product information
CAS Number: 151581-24-7
Molecular Weight: 710.76
Formula: C38H37F3O8S
Chemical Name: 7-{[(1R,2S,3E,5Z)-10-(4-acetyl-3-hydroxy-2-propylphenoxy)-1-hydroxy-1-[3-(trifluoromethyl)phenyl]deca-3,5-dien-2-yl]sulfanyl}-4-oxo-4H-chromene-2-carboxylic acid
Smiles: CC(=O)C1=CC=C(OCCCC/C=C\C=C\[C@H](SC2C=C3OC(=CC(=O)C3=CC=2)C(O)=O)[C@H](O)C2C=C(C=CC=2)C(F)(F)F)C(CCC)=C1O
InChiKey: IXJCHVMUTFCRBH-SDUHDBOFSA-N
InChi: InChI=1S/C38H37F3O8S/c1-3-11-29-31(18-17-27(23(2)42)36(29)45)48-19-9-7-5-4-6-8-14-34(35(44)24-12-10-13-25(20-24)38(39,40)41)50-26-15-16-28-30(43)22-33(37(46)47)49-32(28)21-26/h4,6,8,10,12-18,20-22,34-35,44-45H,3,5,7,9,11,19H2,1-2H3,(H,46,47)/b6-4-,14-8+/t34-,35+/m0/s1
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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