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Casanthranol

Cat No.:V29262 Purity: ≥98%
Casanthranol is a concentrated mixture of anthranolic glycosides found in gerbil skin (Rhamnus p.
Casanthranol
Casanthranol Chemical Structure CAS No.: 8024-48-4
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Casanthranol is a concentrated mixture of anthranolic glycosides found in gerbil skin (Rhamnus p.), which can be used as an active ingredient in laxatives. Casanthranol promotes intestinal motility and increases muscle contraction by acting on the intestinal wall.
Casanthranol (CAS 8024-48-4) is a concentrated mixture of anthranol glycosides derived from cascara sagrada, the dried aged bark of the buckthorn plant Rhamnus purshiana (also known as Frangula purshiana). It is a stimulant laxative that encourages bowel movements by acting on the intestinal wall to increase muscle contractions (peristalsis). Casanthranol is commonly used for the treatment of constipation and to facilitate bowel movements. It is not absorbed by the body and acts locally in the intestines, providing relief from constipation without significant systemic effects.
Biological Activity I Assay Protocols (From Reference)
Targets
The primary target of Casanthranol is the intestinal smooth muscle, where it acts as a stimulant laxative. The anthranol glycosides in Casanthranol are metabolized by intestinal bacteria to active anthrone derivatives, which stimulate the myenteric plexus and increase peristaltic contractions. This mechanism promotes bowel movements by acting on the intestinal wall to increase muscle contractions. The compound contains anthraquinone components including emodin and cascarosides.
ln Vitro
In vitro, Casanthranol's components (anthranol glycosides) can be studied for their effects on intestinal smooth muscle contraction. As a stimulant laxative, the active anthrone derivatives increase peristaltic activity in isolated intestinal tissue preparations. However, specific quantitative in vitro activity data (e.g., EC50 values) for Casanthranol is not detailed in publicly available sources.
ln Vivo
In vivo, Casanthranol is used as a stimulant laxative for the treatment of constipation. It acts locally in the intestines without significant systemic absorption, encouraging bowel movements by increasing muscle contractions in the intestinal wall. It is commonly included in various laxative formulations for relief of constipation and other medical conditions requiring bowel stimulation.
Enzyme Assay
Not applicable. Casanthranol is a mixture of natural anthranol glycosides and is not used in cell-free enzyme/receptor binding assays as a test compound for mechanistic studies. Its primary application is as a laxative, and its mechanism of action involves local intestinal stimulation rather than specific enzyme or receptor binding in cell-free systems.
Cell Assay
Not applicable. Casanthranol is not typically used in cell-based pharmacological assays as a test compound. Its primary application is as a laxative, and its mechanism of action involves local intestinal stimulation. Research applications may include studies of intestinal smooth muscle contraction using isolated tissue preparations, but standard cell-based assays are not commonly employed for this compound.
Animal Protocol
In vivo efficacy is evaluated in animal models of constipation or in clinical use for bowel stimulation. Casanthranol is administered orally. Endpoints include time to first bowel movement, stool frequency, stool consistency, and intestinal transit time. Clinical studies focus on its efficacy as a stimulant laxative in patients with constipation.
ADME/Pharmacokinetics
Molecular weight: varies (mixture). CAS No.: 8024-48-4. Appearance: typically a powder or extract. Storage: typical for natural product mixtures (desiccated, protected from light). Solubility: as a glycoside mixture, soluble in water and alcohols.
Toxicity/Toxicokinetics
No detailed toxicity data is publicly available beyond its use as an over-the-counter laxative. As a stimulant laxative, potential side effects include abdominal cramping, electrolyte imbalance, and dehydration with prolonged use. It is generally considered safe for short-term use.
References

[1]. NCIt. Casanthranol.

Additional Infomation
4,5-Dihydroxy-2-(hydroxymethyl)-10-oxo-9,10-dihydro-9-anthraylhexopyranoside is an anthracene compound. Catanthanol is a concentrated mixture of anthraquinone glycosides extracted from the bark of Rhamnus p., used as a laxative for constipation and various other ailments. The stimulant laxative catanthanol promotes defecation by acting on the intestinal wall to increase muscle contractions. (NCI04) Catanthanol is a laxative anthraquinone found in various plants, particularly Rhamnus purshiana. It was once used as a laxative but is now primarily used as a tool in toxicity studies. See also: Catanthanol (note moved to).
Casanthranol is an approved over-the-counter (OTC) laxative ingredient in many countries. It is used for the treatment of constipation and to facilitate bowel movements. Its mechanism involves acting on the intestinal wall to increase muscle contractions. It is not absorbed systemically and acts locally in the intestines. Casanthranol is not used as a prescription drug but is available in various OTC laxative formulations.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C21H22O10
Molecular Weight
434.39338
Exact Mass
434.121
CAS #
8024-48-4
PubChem CID
2098
Appearance
Light yellow to yellow solid powder
LogP
-0.4
Hydrogen Bond Donor Count
7
Hydrogen Bond Acceptor Count
10
Rotatable Bond Count
4
Heavy Atom Count
31
Complexity
646
Defined Atom Stereocenter Count
0
InChi Key
CPUHNROBVJNNPW-UHFFFAOYSA-N
InChi Code
InChI=1S/C21H22O10/c22-6-8-4-10-15(12(25)5-8)17(27)14-9(2-1-3-11(14)24)20(10)31-21-19(29)18(28)16(26)13(7-23)30-21/h1-5,13,16,18-26,28-29H,6-7H2
Chemical Name
1,8-dihydroxy-3-(hydroxymethyl)-10-[3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-10H-anthracen-9-one
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ≥ 50 mg/mL
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.3021 mL 11.5104 mL 23.0208 mL
5 mM 0.4604 mL 2.3021 mL 4.6042 mL
10 mM 0.2302 mL 1.1510 mL 2.3021 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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