Etalocib
Based on 2 publication(s) in Google Scholar
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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- 純度: 99.03%
- CAS 番号: 161172-51-6
- 分子式: C33H33FO6
- 分子量:544.61
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Etalocib
MoreLeukotriene Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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LTB4 |
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.
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Cell Line:MiaPaCa-2 and AsPC-1 human pancreatic cancer cells.[3]
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Concentration:500 nM.
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Incubation Time:24, 48, and 72 h.
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Result:Caused both a concentration-dependent and time-dependent inhibition of thymidine incorporation in both MiaPaCa-2 and AsPC-1 human pancreatic cancer cells.
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Cell Line:MiaPaCa-2 and AsPC-1 human pancreatic cancer cells.
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Concentration:250 and 500 nM.
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Incubation Time:24 h.
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Result:Induced apoptosis in human pancreatic cancer cells.
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.
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Animal Model:Guinea pigs[2].
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Dosage:1-10 mg/kg.
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Administration:Orally once.
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 161172-51-6
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性状 Solid
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分子量 544.61
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分子式 C33H33FO6
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Color White to off-white
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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
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別名
LY293111; VML 295
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Cancer Sci
CML With Mutant ASXL1 Showed Decreased Sensitivity to TKI Treatment via Upregulation of the ALOX5-BLTR Signaling Pathway. [Abstract]2025 Apr;116(4):1115-1125. PMID: 39905783 -
Antiviral Res
Large-scale deep learning identifies the antiviral potential of PKI-179 and MTI-31 against coronaviruses. [Abstract]2024 Nov:231:106012. PMID: 39332537
溶剤 & 溶解度
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)
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.
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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.
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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
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参考文献
[1]. P Marder, et al. Blockade of Human Neutrophil Activation by 2-[2-propyl-3-[3-[2-ethyl-4-(4-fluorophenyl)-5- Hydroxyphenoxy]propoxy]phenoxy]benzoic Acid (LY293111), a Novel Leukotriene B4 Receptor Antagonist. Biochem Pharmacol. 1995 May 26;49(11):1683-90. [Content Brief]
[2]. 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. [Content Brief]
[3]. 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. [Content Brief]
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 |
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| 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 |
Etalocib 関連分類
HY-13628 関連分類
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