Thiocolchicoside

Modify Date: 2025-08-21 20:02:39

Thiocolchicoside Structure
Thiocolchicoside structure
 Common Name Thiocolchicoside
CAS Number 602-41-5 Molecular Weight 563.617
Density 1.5±0.1 g/cm3 Boiling Point 929.6±65.0 °C at 760 mmHg
Molecular Formula C27H33NO10S Melting Point 190-198ºC
MSDS Chinese USA Flash Point 516.0±34.3 °C
Symbol GHS07
GHS07		 Signal Word Warning

 Use of Thiocolchicoside


Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties[1].

 Names

Name Thiocolchicoside
Synonym More Synonyms

 Thiocolchicoside Biological Activity

Description Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties[1].
Related Catalog
Target

GABAA) receptor; glycine receptor[1]

In Vitro Thiocolchicoside (0.001, 0.1, 1, 10, 100 μM) reduces the amplitude of eIPSCs in a concentration-dependent manner with this effect being significant at 0.1 μM and maximal at 10 μM[1].
References

[1]. Carta M, et al. The muscle relaxant thiocolchicoside is an antagonist of GABAA receptor function in the central nervous system. Neuropharmacology. 2006 Sep;51(4):805-15.

 Chemical & Physical Properties

Density 1.5±0.1 g/cm3
Boiling Point 929.6±65.0 °C at 760 mmHg
Melting Point 190-198ºC
Molecular Formula C27H33NO10S
Molecular Weight 563.617
Flash Point 516.0±34.3 °C
Exact Mass 563.182495
PSA 189.31000
LogP -1.23
Vapour Pressure 0.0±0.3 mmHg at 25°C
Index of Refraction 1.657
InChIKey LEQAKWQJCITZNK-AXHKHJLKSA-N
SMILES COc1c(OC2OC(CO)C(O)C(O)C2O)cc2c(c1OC)-c1ccc(SC)c(=O)cc1C(NC(C)=O)CC2

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
AC2976015
CHEMICAL NAME :
Acetamide, N-(3-(beta-D-glucopyranosyloxy)-5,6,7,9-tetrahydro-1, 2-dimethoxy-10-(methy lthio)- 9-oxobenzo(a)heptalen-7-yl)-, (S)-
CAS REGISTRY NUMBER :
602-41-5
BEILSTEIN REFERENCE NO. :
0072205
LAST UPDATED :
199801
DATA ITEMS CITED :
5
MOLECULAR FORMULA :
C27-H33-N-O10-S
MOLECULAR WEIGHT :
563.67

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
10 mg/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - excitement
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 109,386,1957
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
27500 ug/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - excitement
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 109,386,1957
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intracerebral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1 ug/kg
TOXIC EFFECTS :
Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - excitement
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 109,386,1957
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Parenteral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 15,533,1960
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRPSAX Farmaco, Edizione Scientifica. (Casella Postale 227, 27100 Pavia, Italy) V.8-43 1953-88 For publisher information, see FRMCE8 Volume(issue)/page/year: 15,533,1960

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302-H315-H319-H335
Precautionary Statements P301 + P312 + P330-P305 + P351 + P338
RIDADR NONH for all modes of transport
RTECS AC2976015

 ThiocolchicosideBioassay

View more

Name: Compound was evaluated for inhibition of rat Gabra1 in an in vitro assay with cellula...
Source: ChEMBL
Target: Gamma-aminobutyric acid receptor subunit alpha-1
External Id: CHEMBL5291801
Name: Binding affinity towards rat Gabra1 in an in vitro assay with cellular components mea...
Source: ChEMBL
Target: Gamma-aminobutyric acid receptor subunit alpha-1
External Id: CHEMBL5291798
Name: Binding affinity towards human ESR1 in an in vitro cell free assay (NIBR assay) measu...
Source: ChEMBL
Target: Estrogen receptor
External Id: CHEMBL5291791
Name: Binding affinity towards human EDNRA in an in vitro assay with cellular components me...
Source: ChEMBL
Target: Endothelin-1 receptor
External Id: CHEMBL5291785
Name: Dicer-mediated maturation of pre-microRNA
Source: Center for Chemical Genomics, University of Michigan
Target: N/A
External Id: TargetID_659_CEMA
Name: Binding affinity towards human DRD2 in an in vitro assay with cellular components mea...
Source: ChEMBL
Target: D(2) dopamine receptor
External Id: CHEMBL5291781
Name: Agonist activity at human DRD1 in an in vitro cell-based assay measured by time-resol...
Source: ChEMBL
Target: D(1A) dopamine receptor
External Id: CHEMBL5291777
Name: Antagonist activity at human CNR1 in an in vitro cell-based assay measured by fluores...
Source: ChEMBL
Target: Cannabinoid receptor 1
External Id: CHEMBL5291772
Name: Agonist activity at human CNR1 in an in vitro cell-based assay measured by fluorescen...
Source: ChEMBL
Target: Cannabinoid receptor 1
External Id: CHEMBL5291771
Name: qHTS assay to test for compound auto fluorescence at 535 nm (green) in HEK293 cell fr...
Source: 824
Target: N/A
External Id: SPEC167MG
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 Synonyms

Thiocolchicoside
UNII:T1X8S697GT
Thiocolchicine Glycoside
N-[(7S)-3-(b-D-glucopyranosyloxy)-1,2-dimethoxy-10-(methylthio)-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide
R. 271
Coltramyl
Musco-ril
N-[(7S)-3-(β-D-Glucopyranosyloxy)-1,2-dimethoxy-10-(methylsulfanyl)-9-oxo-5,6,7,9-tetrahydrobenzo[a]heptalen-7-yl]acetamide
3,10-Di(demethoxy)-3-glucosyloxy-10-methylthiocolchicine
10-Thiocolchicoside
Tiocolchicoside
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