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Israpafant

Israpafant (Y-24180) is a potent, selective and long-acting platelet activation factor (PAF) receptor antagonist with IC50s of 0.84 nM and 3.84 nM against PAF-induced human and rabbit platelet aggregation, respectively. Israpafant stimulates both extracellular Ca2+ influx and intracellular Ca2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice[1][2].

Product Specifications

CAS Number

117279-73-9

Product Name Alternative

Y 24180

UNSPSC

12352005

Target

Platelet-activating Factor Receptor (PAFR)

Type

Reference compound

Related Pathways

GPCR/G Protein

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/israpafant.html

Solubility

10 mM in DMSO

Smiles

CC1=NN=C2N1C3=C(C(C4=C(Cl)C=CC=C4)=NC2C)C=C(S3)CCC5=CC=C(C=C5)CC(C)C

Molecular Formula

C28H29ClN4S

Molecular Weight

489.07

References & Citations

[1]Takehara S, et al. Pharmacological actions of Y-24180, a new specific antagonist of platelet activating factor (PAF) : II. Interactions with PAF and benzodiazepine receptors. Prostaglandins. 1990 Dec;40 (6) :571-83.|[2]Jan C R, Chao Y Y. Novel effect of Y-24180, a presumed specific platelet activation factor receptor antagonist, on Ca2+ levels and growth of human prostate cancer cells. Cellular signalling, 2004, 16 (8) : 959-965.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

Phase 3

Frequently Asked Questions

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