Pep2-8 [1541011-97-5]

Référence HY-P2276-1mg

Conditionnement : 1mg

Marque : MedChemExpress

Contactez votre distributeur local :


Téléphone : +1 850 650 7790

Description

Pep2-8 is a PCSK9 inhibitor with a binding KD of 0.7 μM and an IC50 of 1.4 μM[1].

Cellular Effect
Cell Line Type Value Description References
HepG2 EC50
6 μM
Compound: Pep2-8
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
[PMID: 34266235]
LAD2 EC50
>5 μM
Compound: Pep2-8
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
[PMID: 34266235]
In Vitro

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.

Cell Viability Assay[1]

Cell Line: HepG2 cell.
Concentration: 15 μg/mL.
Incubation Time: 4 h.
Result: Inhibited PCSK9 activity.
Masse moléculaire

1715.85

Formule

C83H110N16O24

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Ac-Thr-Val-Phe-Thr-Ser-Trp-Glu-Glu-Tyr-Leu-Asp-Trp-Val-NH2

Sequence Shortening

Ac-TVFTSWEEYLDWV-NH2

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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)

Solvant et solubilité
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.5828 mL 2.9140 mL 5.8280 mL
5 mM 0.1166 mL 0.5828 mL 1.1656 mL
View the 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.

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (1.46 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation
Références

Vous serez peut-être également intéressé par les produits suivants :



Référence
Description
Cond.
Prix HT