Biological Activity

SBE-β-CD (Sulfobutylether beta-cyclodextrin) 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. 

Product Citations

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  Cell Rep. 2023 Jun 27;42(7):112690.

  Identification of XAF1 as an endogenous AKT inhibitor
  SBE-β-CD (Sulfobutylether beta-cyclodextrin) purchased from AbMole

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  Int J Mol Sci. 2023 Feb 6;24(4):3229.

  The Role of the Dopamine System in Post-Stroke Mood Disorders in Newborn Rats
  SBE-β-CD (Sulfobutylether beta-cyclodextrin) purchased from AbMole

• 

  The American Journal of Pathology. 2022 Dec.

  EZH2 Promotes Cholangiocarcinoma Development and Progression through Histone Methylation and microRNA-Mediated Down-Regulation of Tumor Suppressor Genes
  SBE-β-CD (Sulfobutylether beta-cyclodextrin) purchased from AbMole

• 

  Anal Cell Pathol (Amst). 2022 Oct 5;2022:3770715.

  Chemoprevention of 4NQO-Induced Mouse Tongue Carcinogenesis by AKT Inhibitor through the MMP-9/RhoC Signaling Pathway and Autophagy
  SBE-β-CD (Sulfobutylether beta-cyclodextrin) purchased from AbMole

• 

  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.
  SBE-β-CD (Sulfobutylether beta-cyclodextrin) purchased from AbMole

Customer Product Validations & Biological Datas

	Source	J Biomed Mater Res B Appl Biomater (2016). Figure 3. Captisol
	Method	Transmission electron microscopy
	Cell Lines	MRC-5 cells
	Concentrations	1 μM
	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
	Method	Fluorescence
	Cell Lines
	Concentrations	10 mM
	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.

Protocol (for reference only)

Cell Experiment
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.
Concentrations	50 mg/ml
Incubation time	2 h

Animal Experiment
Animal models	pig
Formulation	10-mL solution composed of 25% water and 75% PEG400
Dosages	5 mg/kg
Administration	bolus infusions

Chemical Information

Molecular Weight	1451.29
Formula	C50H84Na2O41S2
CAS Number	182410-00-0
Solubility (25°C)	Water > 120 mg/mL
Storage	Powder          -20°C   3 years ;  4°C   2 years In solvent       -80°C   6 months ;  -20°C   1 month

Conversion of different model animals based on BSA (PMID: 27057123)

Species	Mouse	Rat	Rabbit	Guinea pig	Hamster	Dog
Weight (kg)	0.02	0.15	1.8	0.4	0.08	10
Body Surface Area (m2)	0.007	0.025	0.15	0.05	0.02	0.5
Km factor	3	6	12	8	5	20

Animal A (mg/kg) = Animal B (mg/kg) multiplied by	Animal B Km
	Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the K_m factor for a mouse and then divide by the K_m factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Mamoru Fukuda, et al. Int J Pharm. Influence of sulfobutyl ether beta-cyclodextrin (Captisol) on the dissolution properties of a poorly soluble drug from extrudates prepared by hot-melt extrusion

[2] Valentino J Stella, et al. Sulfobutylether-β-cyclodextrin

[3] Farouk Semcheddine, et al. Effects of the Preparation Method on the Formation of True Nimodipine SBE-β-CD/HP-β-CD Inclusion Complexes and Their Dissolution Rates Enhancement

[4] David R Luke, et al. Review of the basic and clinical pharmacology of sulfobutylether-beta-cyclodextrin (SBECD)

[5] Valentino J Stella, et al. Cyclodextrins

[6] V Zia, et al. Effect of cyclodextrin charge on complexation of neutral and charged substrates: comparison of (SBE)7M-beta-CD to HP-beta-CD