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> Pep2-8 [1541011-97-5]

Pep2-8 [1541011-97-5]

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Cat# HY-P2276-1mg

Size : 1mg

Brand : MedChemExpress

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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.

Custom Peptide Synthesis

Pep2-8 Chemical Structure

Pep2-8 Chemical Structure

CAS No. : 1541011-97-5

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Other Forms of Pep2-8:

  • Pep2-8 TFA Get quote
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.

Pep2-8 Related Antibodies

Cell Viability Assay[1]

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

1715.85

Formula

C83H110N16O24
CAS No.

1541011-97-5
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
Shipping

Room temperature in continental US; may vary elsewhere.
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
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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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.

  • 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.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.74%

SDS (393 KB)

COA (252 KB) LCMS (258 KB) Elemental Analysis Report (109 KB)

Handling Instructions (2659 KB)
References

  • [1]. Yingnan Zhang, et al. Identification of a small peptide that inhibits PCSK9 protein binding to the low density lipoprotein receptor. J Biol Chem. 2014 Jan 10;289(2):942-55.  [Content Brief]

  • [1]. Yingnan Zhang, et al. Identification of a small peptide that inhibits PCSK9 protein binding to the low density lipoprotein receptor. J Biol Chem. 2014 Jan 10;289(2):942-55.

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
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Pep2-8 Related Classifications

  • Cancer
  • Cancer Targeted Therapy Cancer Metabolism and Metastasis
  • Metabolic Enzyme/Protease
  • PCSK9
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pep2-81541011-97-5PCSK9Proprotein convertase subtilisin/kexin type 9LDLHepG2Inhibitorinhibitorinhibit

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