L687
Based on 1 publication(s) in Google Scholar
L687 is an activator of TRPC3, TRPC6, and TRPC7 cation channels and induces calcium influx. L687 induces macropinocytosis and endocytosis. L687 enhances cellular uptake and knockdown activity of antisense oligonucleotides. L687 alone does not alter SRRM4 expression. L687 can be used for research on small cell lung cancer.
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- Pureté : 99.49%
- CAS No.: 2776151-36-9
- Formule: C26H33ClN4O3
- Masse moléculaire:485.02
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) L687
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Activité biologique
Description
IC50 & Target
[1]|
TRPC3 |
TRPC6 |
TRPC7 |
In Vitro
L687 (30 μM; 48 h) potentiates ERBB2_ASO-mediated reduction of SK-OV-3 cell viability[1].
L687 (30 μM; 48 h) directs ASO to endosomes/lysosomes in A549 and N417 cells, and UNC7938 enhances endosomal escape and nuclear/cytosolic ASO distribution[1].
L687 (10-30 μM; 24 h) increases endocytosis of Alexa647-labelled dextran in A549 cells[1].
L687 (3-30 μM) is a TRPC3/C6/C7-selective activator that induces dose-dependent Ca2+ influx in HEK293-overexpressing TRPC3/C6/C7 and A549 cells[1].
L687 (10-30 μM; 24-72 h) promotes cellular uptake of Alexa647-labelled ASO in A549, 22Rv1, N417, and H209 cells, with no substantial increase in H146 cells[1].
L687 (30 μM; 48-72 h) enhances knockdown activity of MALAT1-, SRRM4-, REST-, and ERBB2-targeted ASOs in A549, N417, and SK-OV-3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, N417, and SK-OV-3 cells
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Concentration:30 μM (L687); 100 nM (SRRM4_ASO, REST_ASO, ERBB2_ASO)
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Incubation Time:48 h; 72 h (REST_ASO)
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Result:Compared with MALAT1_ASO without L687, the addition of MALAT1_ASO with 30 μM L687 significantly decreased MALAT1 expression in A549 cells.
After 48 h of culture, SRRM4_ASO with L687 significantly decreased the relative expression of SRRM4 when compared with SRRM4_ASO alone.
The addition of ASO with L687 or CBD significantly decreased the relative expression of REST when compared with control A549 cells or cells exposed to ASO alone.
L687 and CBD without REST_ASO did not affect REST expression.
The relative expression of REST mRNA after 72 h was significantly repressed when compared with that observed after 48 h.
The addition of ERBB2_ASO with 30 μM L687 significantly reduced the relative expression of ERBB2 when compared with ERBB2_ASO without L687.
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Cell Line:SK-OV-3 cells
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Concentration:30 μM (L687); 100 nM (ERBB2_ASO)
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Incubation Time:48 h
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Result:The addition of ERBB2_ASO with 30 μM L687 significantly reduced cell viability when compared with ERBB2_ASO without L687.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c Slc-nu/nu (male, 7-week-old)[1]
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Dosage:1.5 μg in DMSO (0.3 μl) in 10 μl PBS (Day 1); 1.5 μg in DMSO (0.3 μl) (24 h later with SRRM4_ASO 10 μg)
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Administration:intratumoral; Day 1 and 24 h later; tumours collected 24 h after second administration
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Result:Tumours treated with L687 plus SRRM4_ASO had higher SRRM4_ASO levels than tumours treated with DMSO plus SRRM4_ASO.
Relative SRRM4 expression was reduced in tumours administered SRRM4_ASO plus L687 compared with tumours administered SRRM4_ASO with DMSO.
Chemical Information
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CAS No. 2776151-36-9
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Appearance Solid
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Masse moléculaire 485.02
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Formule C26H33ClN4O3
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Color White to off-white
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SMILES
O=C(N1CCCCC1)C2=CC(Cl)=C(N3CCN(CC(NC4=C(OCC)C=CC=C4)=O)CC3)C=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (206.18 mM; ultrasonic and warming and heat to 60°C; 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)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.15 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.
In Vivo Dissolution Calculator
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.
Pureté et documentation
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Fiche technique (276 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instruction de manipulation (2659 KB)
Références
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 | 2.0618 mL | 10.3089 mL | 20.6177 mL | 51.5443 mL |
| 5 mM | 0.4124 mL | 2.0618 mL | 4.1235 mL | 10.3089 mL | |
| 10 mM | 0.2062 mL | 1.0309 mL | 2.0618 mL | 5.1544 mL | |
| 15 mM | 0.1375 mL | 0.6873 mL | 1.3745 mL | 3.4363 mL | |
| 20 mM | 0.1031 mL | 0.5154 mL | 1.0309 mL | 2.5772 mL | |
| 25 mM | 0.0825 mL | 0.4124 mL | 0.8247 mL | 2.0618 mL | |
| 30 mM | 0.0687 mL | 0.3436 mL | 0.6873 mL | 1.7181 mL | |
| 40 mM | 0.0515 mL | 0.2577 mL | 0.5154 mL | 1.2886 mL | |
| 50 mM | 0.0412 mL | 0.2062 mL | 0.4124 mL | 1.0309 mL | |
| 60 mM | 0.0344 mL | 0.1718 mL | 0.3436 mL | 0.8591 mL | |
| 80 mM | 0.0258 mL | 0.1289 mL | 0.2577 mL | 0.6443 mL | |
| 100 mM | 0.0206 mL | 0.1031 mL | 0.2062 mL | 0.5154 mL |
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