Captisol is a unique reproducible mixture of polyanionic β-cyclodextrin derivatives in which a sodium sulfonate salt is tethered to the lipophilic cyclodextrin cavity by a butyl ether group, or sulfobutylether (SBE). The sulfobutyl ether (SBE) substituent is introduced at the 2, 3, and 6 positions in one or more of the glucopyranose units in the cyclodextrin structure.
Int J Cancer. 2013 Nov;133(9):2065-76.
Combined targeting of AKT and mTOR using MK-2206 and RAD001 is synergistic in the treatment of cholangiocarcinoma.
Captisol(SBE-β-CD) purchased from AbMole
|Source||J Biomed Mater Res B Appl Biomater (2016). Figure 3. Captisol|
|Method||Transmission electron microscopy|
|Cell Lines||MRC-5 cells|
|Incubation Time||24 h|
|Results||Deionized water-dispersed ICG, SCyD, and MCyD showed a size distribution ranging from 2 to 200 nm.|
|Source||J Biomed Mater Res B Appl Biomater (2016). Figure 1. Captisol|
|Incubation Time||24 h|
|Results||Over 24 h, ICG retained just 0.383 of its initial fluorescence in water, while MCyD-I and SCyD-I in water retained 1.943 and 2.063 higher fluorescence than ICG at t0. In PBS, ICG retained 0.753 of its initial fluorescence while MCyD-I actually increased to 29.863 and SCyD-I retained 20.833 of initial ICG fluorescence in PBS.|
|Cell lines||Caco-2 cells|
|Preparation method||The cells were then preincubated for 30 min without Nos solution+permeation enhancer CH or CP and then incubated for 120 min at 37 ℃ with the Nos solution (50 mg/ml)+permeation enhancer CH or CP.|
|Incubation time||2 h|
|Formulation||10-mL solution composed of 25% water and 75% PEG400|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||Water > 100 mg/ml|
GK921 is a transglutaminase 2 (TGase 2) inhibitor.
Miridesap is a ligand for serum amyloid P component (SAP) and intends to inhibit and dissociate SAP binding to amyloid fibrils and tangles.
Aramchol is a cholesterol solubilizer that prevents gallstone formation in inbred mice.
Cytochalasin B is a cell-permeable mycotoxin binding to the barbed end of actin filaments, disrupting the formation of actin polymers, with Kd value of 1.4-2.2 nM for F-actin.
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