Pep2-8
Based on 1 Customer Validation
Pep2-8 is a PCSK9 inhibitor with a binding KD of 0.7 μM and an IC50 of 1.4 μM.
For research use only. We do not sell to patients.
- Purity: 99.13%
- CAS No.: 1541011-97-5
- Formula: C83H110N16O24
- Molecular Weight:1715.85
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Storage:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
6 μM
Compound: Pep2-8
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Reversal of LDL uptake in human HepG2 cells for 2 hrs preincubation with PCSK9 followed by LDL addition and measured after 4 hrs by fluorimetry method relative to control
Reversal of LDL uptake in human HepG2 cells for 2 hrs preincubation with PCSK9 followed by LDL addition and measured after 4 hrs by fluorimetry method relative to control
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[PMID: 34266235] |
| LAD2 | EC50 |
>5 μM
Compound: Pep2-8
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Effect on mast cell degranulation in human LAD2 cells assessed as CCL3 release measured after 2 hrs by Luminex bead based assay
Effect on mast cell degranulation in human LAD2 cells assessed as CCL3 release measured after 2 hrs by Luminex bead based assay
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[PMID: 34266235] |
Pep2-8 binds to C-terminally truncated PCSK9[1].
Pep2-8 restored LDL uptake of PCSK9-treated HepG2 cells to about 90% of control activity at a concentration of 50 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 cell.
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Concentration:15 μg/mL.
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Incubation Time:4 h.
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Result:Inhibited PCSK9 activity.
Chemical Information
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CAS No. 1541011-97-5
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Appearance Solid
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Molecular Weight 1715.85
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Formula C83H110N16O24
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Color White to off-white
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Sequence
Ac-Thr-Val-Phe-Thr-Ser-Trp-Glu-Glu-Tyr-Leu-Asp-Trp-Val-NH2
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Sequence Shortening
Ac-TVFTSWEEYLDWV-NH2
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvent & Solubility
DMSO : 100 mg/mL (58.28 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 (sealed storage, away from moisture and light). 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 (sealed storage, away from moisture and light). 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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.
Purity & Documentation
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Data Sheet (274 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)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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 (sealed storage, away from moisture and light). 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 | 0.5828 mL | 2.9140 mL | 5.8280 mL | 14.5700 mL |
| 5 mM | 0.1166 mL | 0.5828 mL | 1.1656 mL | 2.9140 mL | |
| 10 mM | 0.0583 mL | 0.2914 mL | 0.5828 mL | 1.4570 mL | |
| 15 mM | 0.0389 mL | 0.1943 mL | 0.3885 mL | 0.9713 mL | |
| 20 mM | 0.0291 mL | 0.1457 mL | 0.2914 mL | 0.7285 mL | |
| 25 mM | 0.0233 mL | 0.1166 mL | 0.2331 mL | 0.5828 mL | |
| 30 mM | 0.0194 mL | 0.0971 mL | 0.1943 mL | 0.4857 mL | |
| 40 mM | 0.0146 mL | 0.0729 mL | 0.1457 mL | 0.3643 mL | |
| 50 mM | 0.0117 mL | 0.0583 mL | 0.1166 mL | 0.2914 mL |