Home Neuronal Signaling Hydrotropic Agents inhibitor - Beta Amyloid inhibitor (2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD)

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(2-Hydroxypropyl)-β-cyclodextrin (HP-β-CD) Hydrotropic Agents inhibitor

Cat.No.S4760

(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) Hydrotropic Agents inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 1541.54

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 1541.54 Formula

C63H112O42

 Storage (From the date of receipt)
CAS No. 128446-35-5 Download SDF Storage of Stock Solutions

Synonyms HP-β-cyclodextrin, Hydroxypropyl betadex, Hydroxypropyl-β-cyclodextrin 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

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (64.87 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Mechanism of Action

Targets/IC50/Ki
amyloid-β aggregation [1]
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].
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].
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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