PCSK9-IN-13
Based on 1 Customer Validation
PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM.
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- Pureté : 98.00%
- CAS No.: 2244129-23-3
- Formule: C30H33N5O2
- Masse moléculaire:495.62
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf21 | IC50 |
>10 μM
Compound: 3f
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Inhibition of recombinant human N-terminal GST-tagged c-Kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using FAM-labelled P22 peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1
Inhibition of recombinant human N-terminal GST-tagged c-Kit (544 to end residues) expressed in baculovirus infected Sf21 insect cells using FAM-labelled P22 peptide as substrate preincubated for 10 mins followed by substrate addition and measured after 1
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[PMID: 32051094] |
In Vitro
PCSK9-IN-13(compound 3f) (0.1 or 1 μM) restores LDL uptake in HepG2 hepatocytes in a dose-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
The pharmacokinetic parameters of PCSK9-IN-13(compound 3f) in C57BL/6 mice
| Parameter | SC | PO | IV(single) | IV(cassette) |
| Dose(mg/kg) | 20 | 20 | 5 | 0.4 |
| Tmax(h) | 1 | 2 | - | - |
| Cmax(ng/mL) | 2207 | 52.6 | - | - |
| CL(L/h/kg) | - | - | 1.09 | 0.3 |
| Vss(L/kg) | - | - | 3.87 | 9.13 |
| T1/2(h) | 5.47 | - | 9.86 | 25.7 |
| AUC∞(h*ng/mL) | 16811 | - | 4605 | 1472 |
| MRT∞(h) | - | - | 3.56 | 34.9 |
| F(%) | 91.3 | 0.527 | - | - |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2244129-23-3
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Appearance Solid
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Masse moléculaire 495.62
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Formule C30H33N5O2
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Color Light yellow to yellow
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SMILES
O=C(C1=CC(OC2=CC=CC=C2)=C(C=C1)C)NC3=CC(N4C=C(N=C4)C)=CC(CN5C[C@H](CCC5)N)=C3
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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
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (201.77 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)
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 (5.04 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.04 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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.
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 (272 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 |
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| DMSO | 1 mM | 2.0177 mL | 10.0884 mL | 20.1767 mL | 50.4419 mL |
| 5 mM | 0.4035 mL | 2.0177 mL | 4.0353 mL | 10.0884 mL | |
| 10 mM | 0.2018 mL | 1.0088 mL | 2.0177 mL | 5.0442 mL | |
| 15 mM | 0.1345 mL | 0.6726 mL | 1.3451 mL | 3.3628 mL | |
| 20 mM | 0.1009 mL | 0.5044 mL | 1.0088 mL | 2.5221 mL | |
| 25 mM | 0.0807 mL | 0.4035 mL | 0.8071 mL | 2.0177 mL | |
| 30 mM | 0.0673 mL | 0.3363 mL | 0.6726 mL | 1.6814 mL | |
| 40 mM | 0.0504 mL | 0.2522 mL | 0.5044 mL | 1.2610 mL | |
| 50 mM | 0.0404 mL | 0.2018 mL | 0.4035 mL | 1.0088 mL | |
| 60 mM | 0.0336 mL | 0.1681 mL | 0.3363 mL | 0.8407 mL | |
| 80 mM | 0.0252 mL | 0.1261 mL | 0.2522 mL | 0.6305 mL | |
| 100 mM | 0.0202 mL | 0.1009 mL | 0.2018 mL | 0.5044 mL |
PCSK9-IN-13 Related Classifications
HY-148758 Related Classifications
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