2. GPCR/G Protein
    Apoptosis
  3. Leukotriene Receptor
    Apoptosis
  4. Etalocib

Etalocib  (Synonyms: LY293111; VML 295)

Cat. No.: HY-13628 Purity: 98.27%
COA Handling Instructions

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.

For research use only. We do not sell to patients.

Etalocib Chemical Structure

Etalocib Chemical Structure

CAS No. : 161172-51-6

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5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 680 In-stock
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25 mg USD 1350 In-stock
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50 mg USD 2150 In-stock
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100 mg USD 3450 In-stock
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Based on 1 publication(s) in Google Scholar

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LTB4 LTC4 LTD4/CysLT1 LTE4 CysLT2 CysLT1

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Description

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[1][2][3].

In Vitro

Etalocib (LY293111) elicits a concentration-dependent inhibition of LTB4 induced CD11b up-regulation[1].
Etalocib (LY293111) is an extremely potent and selective antagonist of human neutrophil function in vitro[2].
Etalocib (LY293111, 250 and 500 nM, 24-72 h) induces apoptosis and inhibits proliferation in human pancreatic cancer cells[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[3]

Cell Line: MiaPaCa-2 and AsPC-1 human pancreatic cancer cells.[3]
Concentration: 500 nM.
Incubation Time: 24, 48, and 72 h.
Result: Caused both a concentration-dependent and time-dependent inhibition of thymidine incorporation in both MiaPaCa-2 and AsPC-1 human pancreatic cancer cells.

Apoptosis Analysis[3]

Cell Line: MiaPaCa-2 and AsPC-1 human pancreatic cancer cells.
Concentration: 250 and 500 nM.
Incubation Time: 24 h.
Result: Induced apoptosis 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)[2].
Etalocib (LY293111, 10 mg/kg) inhibits A23187-induced lung inflammatory changes at 1 h[2].
Etalocib (LY293111, 250 mg/kg/day, orally) inhibits growth of human pancreatic cancer xenografts in athymic mice[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Guinea pigs[2].
Dosage: 1-10 mg/kg.
Administration: Orally once.
Result: A single 1 mg/kg oral dose inhibited excised lung gas volume increases by 76.7±7.1% (n=4, P<0.002) when given 8 h prior to leukotriene B4 challenge, and 28.6±20.3% (n=4, NS) when given 24 h before challenge.
Had no effect (10 mg/kg) on pulmonary gas trapping at 1 h or 2 h after A23187 challenge. However, at 4 h, the pulmonary gas trapping response was significantly less than that of vehicle-treated controls and not different from sham values. The 10 mg/kg dose inhibited A23187-induced lung inflammatory changes at 1 h, but was without effect at 2 h or 4 h after challenge.
Clinical Trial
Molecular Weight

544.61

Appearance

Solid

Formula

C33H33FO6
CAS No.
SMILES

O=C(O)C1=CC=CC=C1OC2=CC=CC(OCCCOC3=C(CC)C=C(C4=CC=C(F)C=C4)C(O)=C3)=C2CCC
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8362 mL 9.1809 mL 18.3618 mL
5 mM 0.3672 mL 1.8362 mL 3.6724 mL
10 mM 0.1836 mL 0.9181 mL 1.8362 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (4.59 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (4.59 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

Etalocib161172-51-6LY293111 VML 295LY 293111LY-293111VML295VML 295VML-295Leukotriene ReceptorApoptosisPulmonaryantiinflammatoryasthmabronchiectasisInhibitorinhibitorinhibit

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