Darapladib

製品コードS7520 バッチS752001

印刷

化学情報

Synonyms

SB-480848

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₃₆H₃₈F₄N₄O₂S

分子量

666.77

CAS No.

356057-34-6

Solubility (25°C)*

体外

DMSO (warmed with 50ºC water bath)

100 mg/mL (149.97 mM)

Ethanol

100 mg/mL (149.97 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (7.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	5.000mg/ml (7.50mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.
in vitro	During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM. ^[1]
in vivo	In the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. ^[1] This compound, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. ^[2] In DMHC pigs, this compound reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons. ^[3]

製品説明

Darapladib is a reversible lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor with IC50 of 0.25 nM. Phase 3.

in vitro

During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM. ^[1]

in vivo

In the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. ^[1]

This compound, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. ^[2]

In DMHC pigs, this compound reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons. ^[3]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Cell-free assays
	濃度	0.25 nM
	反応時間
	実験の流れ
動物実験	動物モデル	WHHL rabbits
	投薬量	~30 mg/kg
	投与方法	p.o.

参考

https://pubmed.ncbi.nlm.nih.gov/12643913/
https://pubmed.ncbi.nlm.nih.gov/18806801/
https://pubmed.ncbi.nlm.nih.gov/23388174/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Synergistic activity of RSL3 and Pyrimethamine to inhibit the proliferation of Plasmodium falciparum [ Antimicrob Agents Chemother, 2025, e0047125.]	PubMed: 40823867
A combined AI and cell biology approach surfaces targets and mechanistically distinct Inflammasome inhibitors [ iScience, 2024, 27(12):111404]	PubMed: 39687021
Phospholipase PLA2G7 is complementary to GPX4 in mitigating punicic-acid-induced ferroptosis in prostate cancer cells [ iScience, 2024, 27(5):109774]	PubMed: 38711443
Secreted Apoe rewires melanoma cell state vulnerability to ferroptosis [ Sci Adv, 2024, 10(42):eadp6164]	PubMed: 39413195
The lipoprotein-associated phospholipase A2 inhibitor Darapladib sensitises cancer cells to ferroptosis by remodelling lipid metabolism [ Nat Commun, 2023, 14(1):5728]	PubMed: 37714840
The lipoprotein-associated phospholipase A2 inhibitor Darapladib sensitises cancer cells to ferroptosis by remodelling lipid metabolism [ Nat Commun, 2023, 14(1):5728]	PubMed: 37714840
Darapladib, an inhibitor of Lp-PLA2, sensitizes cancer cells to ferroptosis by remodeling lipid metabolism [ bioRxiv, 2023, 10.1101/2023.04.08.536136]	PubMed: None
Thrombin induces ACSL4-dependent ferroptosis during cerebral ischemia/reperfusion [ Signal Transduct Target Ther, 2022, 7(1):59]	PubMed: 35197442
Human peroxiredoxin 6 is essential for malaria parasites and provides a host-based drug target [ Cell Rep, 2022, 39(11):110923]	PubMed: 35705035
Elevated dietary ω-6 polyunsaturated fatty acids induce reversible peripheral nerve dysfunction that exacerbates comorbid pain conditions [ Nat Metab, 2021, 3(6):762-773]	PubMed: 34140694

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。