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

Etalocib  (Synonyms: LY293111; VML 295)

Cat. No.: HY-13628 Purity: 98.74%
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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.

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Etalocib Chemical Structure

Etalocib Chemical Structure

CAS No. : 161172-51-6

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1 mg USD 132 In-stock
5 mg USD 330 In-stock
10 mg USD 495 In-stock
25 mg USD 890 In-stock
50 mg USD 1335 In-stock
100 mg USD 1870 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Etalocib:

Etalocib Related Antibodies

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LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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].

IC50 & Target

LTB4

 

In Vitro

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

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

Etalocib Related Antibodies

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 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 (10 mg/kg) inhibits A23187-induced lung inflammatory changes at 1 h[2].
Etalocib (250 mg/kg/day, orally) inhibits growth of human pancreatic cancer xenografts in athymic mice[3].

MedChemExpress (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

Formula

C33H33FO6
CAS No.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (183.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8362 mL 9.1809 mL 18.3618 mL 45.9044 mL
5 mM 0.3672 mL 1.8362 mL 3.6724 mL 9.1809 mL
10 mM 0.1836 mL 0.9181 mL 1.8362 mL 4.5904 mL
15 mM 0.1224 mL 0.6121 mL 1.2241 mL 3.0603 mL
20 mM 0.0918 mL 0.4590 mL 0.9181 mL 2.2952 mL
25 mM 0.0734 mL 0.3672 mL 0.7345 mL 1.8362 mL
30 mM 0.0612 mL 0.3060 mL 0.6121 mL 1.5301 mL
40 mM 0.0459 mL 0.2295 mL 0.4590 mL 1.1476 mL
50 mM 0.0367 mL 0.1836 mL 0.3672 mL 0.9181 mL
60 mM 0.0306 mL 0.1530 mL 0.3060 mL 0.7651 mL
80 mM 0.0230 mL 0.1148 mL 0.2295 mL 0.5738 mL
100 mM 0.0184 mL 0.0918 mL 0.1836 mL 0.4590 mL
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Etalocib Related Classifications

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.

Keywords:

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

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