ML 145
Based on 1 publication(s) in Google Scholar
ML 145 is a selective and competitive human GPR35/CXCR8 antagonist with an IC50/EC50 of 20.1 nM. ML 145 has over 1000-fold more selective for GPR35 compared to GPR55 (IC50/EC50=21.7 μM). ML 145 has no significant activity for GPR35 at either rodent ortholog.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 96.09%
- CAS 番号: 1164500-72-4
- 分子式: C24H22N2O5S2
- 分子量:482.57
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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
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 ML 145
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生物活性
IC50/EC50: 20.1 nM (GPR35), 21.7 μM (GPR55)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
0.522 μM
Compound: 14, ML 145
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Antagonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay
Antagonist activity at C-terminal beta-galactosidase tagged human recombinant GPR35 expressed in CHO cells after 90 mins by beta-arrestin recruitment assay
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[PMID: 23888932] |
| U2OS | IC50 |
0.027 μM
Compound: 14, ML 145
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Antagonist activity at human Gal4-VP16 fused GPR35 expressed in human U2OS cells assessed as beta arrestin translocation by reporter gene assay
Antagonist activity at human Gal4-VP16 fused GPR35 expressed in human U2OS cells assessed as beta arrestin translocation by reporter gene assay
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[PMID: 23888932] |
ML 145 (10 μM) also fully blocks internalization of human FLAG-GPR35-eYFP in response to varying concentrations of Zaprinast, Cromolyn disodium, and Pamoate[2].
ML 145 is either without effect (mouse) or displays only a small and apparently noncompetitive inhibitory effect (rat) at the rodent orthologs[2].
ML 145 acts as a competitive antagonist for a number of agonists at human GPR35 and has an IC50 value against EC80 concentrations of various GPR35 agonists in the region of 20 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 1164500-72-4
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性状 Solid
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分子量 482.57
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分子式 C24H22N2O5S2
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Color Yellow to brown
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SMILES
CC(/C=C(S1)/C(N(CCCC(NC2=CC(O)=C(C(O)=O)C=C2)=O)C1=S)=O)=C\C3=CC=CC=C3
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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 (1)
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Journal Impact Factor
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Most Recent
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Mol Neurobiol
Hippocampal GPR35 Participates in the Pathogenesis of Cognitive Deficits and Emotional Alterations Induced by Aβ1-42 in Mice. [Abstract]2025 Jan;62(1):557-582. PMID: 38878116
溶剤 & 溶解度
DMSO : 50 mg/mL (103.61 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 40% PEG300 5% Tween-80 45% Saline
Solubility: 5 mg/mL (10.36 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 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 (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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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取扱説明書 (2659 KB)
参考文献
[1]. Heynen-Genel S, et al. Selective GPR35 Antagonists - Probes 1 & 2. National Center for Biotechnology Information (US); 2010-2010 Feb 28. [Content Brief]
[2]. Laura Jenkins, et al. Antagonists of GPR35 display high species ortholog selectivity and varying modes of action. J Pharmacol Exp Ther. 2012 Dec;343(3):683-95. [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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0722 mL | 10.3612 mL | 20.7224 mL | 51.8060 mL |
| 5 mM | 0.4144 mL | 2.0722 mL | 4.1445 mL | 10.3612 mL | |
| 10 mM | 0.2072 mL | 1.0361 mL | 2.0722 mL | 5.1806 mL | |
| 15 mM | 0.1381 mL | 0.6907 mL | 1.3815 mL | 3.4537 mL | |
| 20 mM | 0.1036 mL | 0.5181 mL | 1.0361 mL | 2.5903 mL | |
| 25 mM | 0.0829 mL | 0.4144 mL | 0.8289 mL | 2.0722 mL | |
| 30 mM | 0.0691 mL | 0.3454 mL | 0.6907 mL | 1.7269 mL | |
| 40 mM | 0.0518 mL | 0.2590 mL | 0.5181 mL | 1.2951 mL | |
| 50 mM | 0.0414 mL | 0.2072 mL | 0.4144 mL | 1.0361 mL | |
| 60 mM | 0.0345 mL | 0.1727 mL | 0.3454 mL | 0.8634 mL | |
| 80 mM | 0.0259 mL | 0.1295 mL | 0.2590 mL | 0.6476 mL | |
| 100 mM | 0.0207 mL | 0.1036 mL | 0.2072 mL | 0.5181 mL |
ML 145 関連分類
HY-107536 関連分類
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