(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)

別名:HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin

(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin) is a well-known sugar used in drug delivery, genetic vectors, environmental protection, and the treatment of Niemann-Pick disease type C1 (NPC1). It is an inhibitor of amyloid-β aggregation and widely used drug delivery vehicle to improve stability and bioavailability.

(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)化学構造

CAS No. 128446-35-5

サイズ 価格(税別) 在庫状況
JPY 22000 国内在庫あり
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Hydrotropic Agents阻害剤の選択性比較

生物活性

製品説明 (2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD, HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin) is a well-known sugar used in drug delivery, genetic vectors, environmental protection, and the treatment of Niemann-Pick disease type C1 (NPC1). It is an inhibitor of amyloid-β aggregation and widely used drug delivery vehicle to improve stability and bioavailability.
Targets
amyloid-β aggregation [1]
In Vitro
In vitro

HP-β-CD molecules were not only nontoxic to cells, but also greatly inhibited Aβ fibrillization and reduced Aβ-induced toxicity in a concentration-dependent manner. Too low concentrations of HP-β-CD caused insufficient interactions with Aβ, while too high concentrations of HP-β-CD caused HP-β-CD to self-aggregate into inactive species. HP-β-CD interacted preferentially with some of the hydrophobic residues of Aβ, which prevented Aβ oligomers from further growing into mature fibrils via peptide elongation and lateral association[1].

細胞実験 細胞株 SH-SY5Y cell line
濃度 25, 50, 125, and 250 μM
反応時間 24 and 48 h
実験の流れ

Cells that was cultured at 37 ℃ in the mixture of sterile-filtered Eagle's minimum essential medium and Ham's F-12 medium mixed at a 1 : 1 ratio with 10% fetal bovine serum, 1% penicillin/streptomycin and humidified air with 5% CO2 was employed as a model neuron. Cells were cultured to confluence and harvested using 0.25 mg/mL trypsin/EDTA solution. Before adding Aβ1-42 and HP-β-CD, cells were resuspended in Opti-MEM reduced serum medium and counted using a hemocytometer. Cells were then plated in a 96-well tissue culture plate with approximately 100 000 cells per well in 200 μL medium. To determine the cell viability, colorimetric MTT metabolic activity assay was performed. SH-SY5Y cells were cultured in a 96-well plate at 37 1C. Then, Aβ1-42, HP-β-CD and Aβ1-42-HP-β-CD solutions were individually added to the cultured cells, which were then continually cultured for additional 24 h and 48 h. After removing the supernatant of each well, 20 μL of MTT solution (5 mg/mL in PBS) and 100 mL of medium were then added into the systems. After incubation for another 4 h, the formazan crystals were dissolved in dimethyl sulfoxide (150 μL) and the absorbance intensity was measured using a microplate reader at 570 nm.

In Vivo
In Vivo

HP-β-CD, due to its excellent biocompatibility, has been widely used in drug delivery systems, environmental remediation, food additives, and pharmacotherapy. HP-β-CD can readily cross the BBB and target nerve cells[1]. HP-β-CD is well tolerated in the animal species tested (rats, mice and dogs), particularly when dosed orally, and shows only limited toxicity. After a single 200 mg/kg intravenous dose in rats and dogs, 14C-HP-β-CD was eliminated rapidly (more than 90% in 4 h), almost completely as the intact compound and mostly by renal excretion. The excretion in faeces and expired air was minimal. The plasma elimination half-life was 0.4 h in rats and 0.8 h in dogs. After oral administration of HP-β-CD in both rats and dogs, 86% was excreted via the faeces in both species, where as less than 5% was excreted in the urine. The absolute bioavailability was estimated at 3.3% in the dog and less in the rat. In both rats and dogs following intravenous administration, tissue distribution was limited: in rats the highest concentration was found in the kidney and lung and in dogs, the highest concentrations were in the kidney and the liver. Plasma levels of unchanged HP-β-CD declined rapidly and showed a bi-phasic decline after single intravenous and oral dosing in healthy volunteers. The utility of a 45%w/v HP-β-CD aqueous dosing vehicle in preclinical studies is very common. This vehicle is useful with poorly aqueous drugs[2].

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02912793 Completed
Niemann-Pick Disease Type C1
Cyclo Therapeutics Inc.
March 20 2017 Phase 1|Phase 2

化学情報

分子量 1541.54 化学式

C63H112O42

CAS No. 128446-35-5 SDF Download (2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD) SDFをダウンロードする
Smiles CC(COCC1C2C(C(C(O1)OC3C(OC(C(C3O)O)OC4C(OC(C(C4O)O)OC5C(OC(C(C5O)O)OC6C(OC(C(C6O)O)OC7C(OC(C(C7O)O)OC8C(OC(O2)C(C8O)O)COCC(C)O)COCC(C)O)COCC(C)O)COCC(C)O)COCC(C)O)COCC(C)O)O)O)O
保管

In vitro
Batch:

DMSO : 100 mg/mL ( (64.87 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 100 mg/mL

Ethanol : 100 mg/mL

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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