Thiocolchicoside

Catalog No.S5049 Batch:S504901

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Technical Data

Formula

C27H33NO10S

Molecular Weight 563.62 CAS No. 602-41-5
Solubility (25°C)* In vitro DMSO 100 mg/mL (177.42 mM)
Water 100 mg/mL (177.42 mM)
Ethanol 2 mg/mL (3.54 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Thiocolchicoside (Thiocolchicine 2-glucoside analog, Coltramyl) is a natural occuring glycoside originated from the flower seeds of superba gloriosa with anti-inflammatory and analgesic properties as well as pronounced convulsant activity. It is also an antagonist of GABAA receptor.
Targets
GABAA receptor [2]
In vitro Thiocolchicoside exhibits a selective affinity for the inhibitory gamma-aminobutyric acid and glycinergic receptors. It has an agonistic action at the spinal-strychnine-sensitive receptors that could mediate its myorelaxant effect. It might preferentially interact with a cortical subtype of the gamma-aminobutyric acid type A (GABAA) receptor that expresses low-affinity binding sites for GABA. GABAB receptors are largely unaffected by thiocolchicoside and hence do not contribute to its muscle relaxation action. Thiocolchicoside suppresses osteoclastogenesis induced by receptor activator of nuclear factor kappa-B ligand, breast cancer and multiple myeloma cells through inhibition of inflammatory pathways[3].
In vivo Thiocolchicoside is used as muscle relaxant agent without any side effects. It is rapidly absorbed from the gastrointestinal tract, undergoes first pass metabolism with an oral bioavailability of about 25 % and a biological half-life of 5-6 h. Thiocolchicoside is broken down in the body to a metabolite called 3-demethylthiocolchicine that could damage cells therefore inducing toxicity in the embryo, neoplastic changes and fertility reduction in male. Local skin preparations are less toxic[1].

Protocol (from reference)

Animal Study:

[2]

  • Animal Models

    Male Sprague-Dawley CD rats

  • Dosages

    10-30 mg/kg

  • Administration

    i.p.

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.