WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 328102
CAS#: 117279-73-9 (racemic)
Description: Israpafant (also known as Y-24180) is a drug which acts as a selective antagonist for the platelet-activating factor receptor, and was originally developed for the treatment of asthma. Its chemical structure is a thienotriazolodiazepines, closely related to the sedative benzodiazepine derivative etizolam. However, israpafant binds far more tightly to the platelet-activating factor receptor, with an IC50 of 0.84nM for inhibiting PAF-induced human platelet aggregation, while it binds only weakly to benzodiazepine receptors, with a Ki of 3680nM. Israpafant has been found to inhibit the activation of eosinophil cells and consequently delays the development of immune responses. It has also been shown to have anti-nephrotoxic properties and to mobilize calcium transport.
MedKoo Cat#: 328102
CAS#: 117279-73-9 (racemic)
Chemical Formula: C28H29ClN4S
Exact Mass: 488.1801
Molecular Weight: 489.078
Elemental Analysis: C, 68.76; H, 5.98; Cl, 7.25; N, 11.46; S, 6.56
This product is not in stock, which may be available by custom synthesis.
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Related CAS #: 136624-39-0 (S-isomer) 136624-40-3 (R-isomer) 117279-73-9 (racemic) 142415-76-7 (HCl)
Synonym: Israpafant; Y-24180; Y 24180; Y24180
IUPAC/Chemical Name: 4-(2-chlorophenyl)-2-(4-isobutylphenethyl)-6,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
InChi Key: RMSWMRJVUJSDGN-UHFFFAOYSA-N
InChi Code: InChI=1S/C28H29ClN4S/c1-17(2)15-21-11-9-20(10-12-21)13-14-22-16-24-26(23-7-5-6-8-25(23)29)30-18(3)27-32-31-19(4)33(27)28(24)34-22/h5-12,16-18H,13-15H2,1-4H3
SMILES Code: CC1=NN=C2N1C3=C(C=C(CCC4=CC=C(CC(C)C)C=C4)S3)C(C5=CC=CC=C5Cl)=NC2C
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 489.078 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|