Etalocib

Etalocib (LY293111), an orally active leukotriene B4 receptor antagonist, inhibits the binding of [3H]LTB4, with a Ki of 25 nM. Etalocib (LY293111) prevents LTB4-induced calcium mobilization with an lC50 of 20 nM. Etalocib (LY293111) induces apoptosis.

Product information

CAS Number: 161172-51-6

Molecular Weight: 544.61

Formula: C33H33FO6

Chemical Name: 2-{3-[3-({5-ethyl-4'-fluoro-2-hydroxy-[1, 1'-biphenyl]-4-yl}oxy)propoxy]-2-propylphenoxy}benzoic acid

Smiles: CCC1=CC(C2=CC=C(F)C=C2)=C(O)C=C1OCCCOC1=CC=CC(OC2=CC=CC=C2C(O)=O)=C1CCC

InChiKey: YFIZRWPXUYFCSN-UHFFFAOYSA-N

InChi: InChI=1S/C33H33FO6/c1-3-9-25-29(12-7-13-30(25)40-31-11-6-5-10-26(31)33(36)37)38-18-8-19-39-32-21-28(35)27(20-22(32)4-2)23-14-16-24(34)17-15-23/h5-7,10-17,20-21,35H,3-4,8-9,18-19H2,1-2H3,(H,36,37)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 100 mg/mL (183.62 mM; Need ultrasonic)

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: ≥360 days 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

How to use

In Vitro:

Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB4 induced CD11b up-regulation. Etalocib (LY293111) is an extremely potent and selective antagonist of human neutrophil function in vitro. Etalocib (LY293111, 250 and 500 nM, 24-72 h) induces apoptosis and inhibits proliferation in human pancreatic cancer cells.

In Vivo:

Etalocib (LY293111) produces a dose-related inhibition of acute leukotriene B4-induced airway obstruction when administered i.v. (ED50=14 µg/kg) or p.o. (ED50=0.4 mg/kg). Etalocib (LY293111, 10 mg/kg) inhibits A23187-induced lung inflammatory changes at 1 h. Etalocib (LY293111, 250 mg/kg/day, orally) inhibits growth of human pancreatic cancer xenografts in athymic mice.

References:

1. S A Silbaugh, et al. Pharmacologic Actions of the Second Generation Leukotriene B4 Receptor Antagonist LY29311: In Vivo Pulmonary Studies. Naunyn Schmiedebergs Arch Pharmacol. 2000 Apr;361(4):397-404.
2. Wei-Gang Tong, et al. Leukotriene B4 Receptor Antagonist LY293111 Inhibits Proliferation and Induces Apoptosis in Human Pancreatic Cancer Cells. Clin Cancer Res. 2002 Oct;8(10):3232-42.

Products are for research use only. Not for human use.