CLP-3094
Based on 2 publication(s) in Google Scholar
CLP-3094 is a potent BF3 (binding function 3)-directed inhibitor of the androgen receptor (AR). CLP-3094 inhibits AR transcriptional activity (IC50=4 μM). CLP-3094 is a selective, potent GPR142 antagonist.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.92%
- No. CAS: 312749-73-8
- Fòrmula: C15H13ClN2OS
- Peso molecular:304.79
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) CLP-3094
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| LNCaP | IC50 |
4 μM
Compound: 51
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Inhibition of BF3 site of androgen receptor in human LNCAP cells expressing ARR2PB after 3 days by eGFP transcriptional assay
Inhibition of BF3 site of androgen receptor in human LNCAP cells expressing ARR2PB after 3 days by eGFP transcriptional assay
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[PMID: 23301637] |
CLP-3094 inhibits both an increase of intracellular Ca2+ concentration ([Ca2+]i) induced by L-tryptophan using CHO-K1 cells expressing GPR142 in the aequorin assay, and an accumulation of inositol phosphates using HEK293 cells expressing GPR142 in the SPA assay. The IC50 of CLP-3094 is 0.2 μM against 200 μM L-tryptophanfor the mouse receptor and 2.3 μM against 1 mM L-tryptophan for the human receptor in the aequorin assay. CLP-3094 also inhibits the insulin secretion from islets induced by both L-tryptophan and GPR142 agonists[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CAIA mouse model (Female DBA1/J mice were i.v. administered with2 mg of anti-collagen antibody, followed by i.p. administration of 50 μg of LPS)[2]
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Dosage:30, 100 mg/kg
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Administration:I.p. daily from Day 0 to Day 11
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Result:Dose-dependently reduced, by not much, the arth-ritis scores.
Chemical Information
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No. CAS 312749-73-8
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Appearance Solid
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Peso molecular 304.79
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Fòrmula C15H13ClN2OS
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Color Off-white to light yellow
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SMILES
ClC1=CC=C(OCCSC2=NC3=CC=CC=C3N2)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (2)
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Journal Impact Factor
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Most Recent
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Diabetes
Gut microbiota-tryptophan metabolism-GLP-1 axis participates in β-cell regeneration induced by dapagliflozin. [Abstract]2024 Jun 1;73(6):926-940. PMID: 38471012 -
Obesity
Intestinal ACE2 regulates glucose metabolism in diet-induced obese mice through a novel gut-islet axis mediated by tryptophan. [Abstract]2023 May;31(5):1311-1325. PMID: 36998145
CLP-3094 purchased from MedChemExpress. Usage Cited in: Obesity. 2023 May;31(5):1311-1325. [Abstract]
CLP-3094 (CLP; 0.7 μM; 48 h) inhibits the PA (palmitic acid) increased expression of PDX-1, NKX6.1, and MAFA in MIN6 cells. whereas L-Trp (0.7 mM; 48 h) causes an opposing effect.
Solvente y solubilidad
DMSO : 100 mg/mL (328.09 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (8.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Pureza y Documentación
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Ficha de datos (272 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Munuganti RS, et al. Targeting the binding function 3 (BF3) site of the androgen receptor through virtual screening. 2. development of 2-((2-phenoxyethyl) thio)-1H-benzimidazole derivatives. J Med Chem. 2013;56(3):1136-1148. [Content Brief]
[2]. Murakoshi M, et al. Discovery and pharmacological effects of a novel GPR142 antagonist. J Recept Signal Transduct Res. 2017;37(3):290-296. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.2809 mL | 16.4047 mL | 32.8095 mL | 82.0237 mL |
| 5 mM | 0.6562 mL | 3.2809 mL | 6.5619 mL | 16.4047 mL | |
| 10 mM | 0.3281 mL | 1.6405 mL | 3.2809 mL | 8.2024 mL | |
| 15 mM | 0.2187 mL | 1.0936 mL | 2.1873 mL | 5.4682 mL | |
| 20 mM | 0.1640 mL | 0.8202 mL | 1.6405 mL | 4.1012 mL | |
| 25 mM | 0.1312 mL | 0.6562 mL | 1.3124 mL | 3.2809 mL | |
| 30 mM | 0.1094 mL | 0.5468 mL | 1.0936 mL | 2.7341 mL | |
| 40 mM | 0.0820 mL | 0.4101 mL | 0.8202 mL | 2.0506 mL | |
| 50 mM | 0.0656 mL | 0.3281 mL | 0.6562 mL | 1.6405 mL | |
| 60 mM | 0.0547 mL | 0.2734 mL | 0.5468 mL | 1.3671 mL | |
| 80 mM | 0.0410 mL | 0.2051 mL | 0.4101 mL | 1.0253 mL | |
| 100 mM | 0.0328 mL | 0.1640 mL | 0.3281 mL | 0.8202 mL |
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