2. Metabolic Enzyme/Protease Apoptosis
  3. Phospholipase Apoptosis
  4. Darapladib

Darapladib  (Synonyms: SB-480848)

製品番号: HY-10521 純度: 99.94%
COA 取扱説明書

Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer.

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Darapladib 構造式

Darapladib 構造式

CAS 番号 : 356057-34-6

容量 価格（税別） 在庫状況 数量
無料サンプル (0.1 - 0.5 mg)   今すぐ申し込む  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 191 在庫あり
Solution
10 mM * 1 mL in DMSO USD 191 在庫あり
Solid
5 mg USD 130 在庫あり
10 mg USD 210 在庫あり
25 mg USD 420 在庫あり
50 mg USD 680 在庫あり
100 mg   お問い合わせ  
200 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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

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Based on 4 publication(s) in Google Scholar

Darapladib 関連抗体

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製品説明

Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer[1][2][3][4].

IC50 & Target

IC50: 0.25 nM (Lp-PLA2)[1]
体外実験

Darapladib (5 μM; 6, 12 h) induces cell cycle arrest in glioma cells (C6 glioma cells and U251MG cells)[2].
Darapladib (5 μM; 3, 6 h) triggers cell apoptosis in glioma cells[2].
Darapladib (5 μM; 5, 15, 30, 60 and 90 min) induces an increase in phosphorylation of ERK1/2 proteins in glioma cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Darapladib 関連抗体

Apoptosis Analysis[2]

Cell Line: C6 glioma cells and U251MG cells.
Concentration: 5 μM
Incubation Time: 3, 6 h
Result: Triggered cell apoptosis in glioma cells.

Cell Cycle Analysis[2]

Cell Line: C6 glioma cells and U251MG cells.
Concentration: 5 μM
Incubation Time: 6, 12 h
Result: Induced cell cycle arrest in glioma cells.

Western Blot Analysis[2]

Cell Line: C6 glioma cells and U251MG cells.
Concentration: 5 μM
Incubation Time: 5, 15, 30, 60 and 90 min
Result: Induced an increase in phosphorylation of ERK1/2 proteins, but reduced AKT phosphorylation in glioma cells.
体内実験

Darapladib (50 mg/kg; p.o.; once daily for 6 weeks) significantly inhibits serum Lp-PLA2 activity in LDLR-deficient mice[3].
Darapladib (50 mg/kg; p.o.; once daily for 6 weeks) decreases serum hs-CRP and IL-6 levels[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male homozygous LDLR-deficient mice (C57/Bl6 genetic background)[3].
Dosage: 50 mg/kg
Administration: Oral administration; once daily for 6 weeks.
Result: Significantly inhibited activity of serum Lp-PLA2.
臨床実験
分子量

666.77

Appearance

Solid

分子式

C36H38F4N4O2S
CAS 番号
SMILES

FC1=CC=C(CSC(N(CC(N(CCN(CC)CC)CC2=CC=C(C3=CC=C(C(F)(F)F)C=C3)C=C2)=O)C4=C5CCC4)=NC5=O)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 100 mg/mL (149.98 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4998 mL 7.4988 mL 14.9977 mL
5 mM 0.3000 mL 1.4998 mL 2.9995 mL
10 mM 0.1500 mL 0.7499 mL 1.4998 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (3.75 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (3.75 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.5 mg/mL (3.75 mM); Clear solution

*All of the co-solvents are available by MedChemExpress (MCE).
純度とドキュメンテーション

純度: 99.94%

COA (248 KB) HNMR (283 KB) LCMS (265 KB)

取扱説明書 (2659 KB)
参考文献
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Darapladib Related Classifications

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.

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  • 希釈カルキュレーター

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

Darapladib356057-34-6SB-480848SB480848SB 480848PhospholipaseApoptosisatherosclerosiscancerglioma cellapoptosisU251MG cellssubG1 cellcycle arrestInhibitorinhibitorinhibit

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製品番号:
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