Carbenoxolone disodium

Modify Date: 2024-01-08 11:54:50

Carbenoxolone disodium Structure
Carbenoxolone disodium structure
Common Name Carbenoxolone disodium
CAS Number 7421-40-1 Molecular Weight 614.72000
Density N/A Boiling Point 687.4ºC at 760 mmHg
Molecular Formula C34H48Na2O7 Melting Point N/A
MSDS N/A Flash Point 211.6ºC

 Use of Carbenoxolone disodium


Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD[1]. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication[2]. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation.

 Names

Name Carbenoxolone disodium,(3β,20β)-3-(3-Carboxy-1-oxopropoxy)-11-oxoolean-12-en-29-oicaciddisodium
Synonym More Synonyms

 Carbenoxolone disodium Biological Activity

Description Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD[1]. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication[2]. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation.
Related Catalog
Target

IC50: human 11β-HSD; bacterial 3α, 20β-HSD[1]; gap junction; Vaccinia virus[2]

In Vitro Carbenoxolone disodium (6-150 μM; pre-treatment 1 hour) inhibits Vaccinia virus (VACV) replication in a gap junction-independent in HaCaT cells, and it has toxicity effects on VACV-A5L-EGFP infected cells at 48 h[2]. Carbenoxolone (30 μM; pre-treatment 1 hour) does not upregulate PP2A expression, but induces the late protein A27 expression in hacat cells[2]. Cell Viability Assay[2] Cell Line: HaCaT cells Concentration: 6 μM, 12 μM, 30 μM, 60 μM, 150 μM Incubation Time: Pre-treatment 1 hour Result: Had no toxicity until 48 hours at high dose in virus-infected cells. Western Blot Analysis[2] Cell Line: HaCaT cells Concentration: 30 μM Incubation Time: Pre-treatment 1 hour Result: Presented an obvious upregulation of A27.
In Vivo Carbenoxolone (intraperitoneal injection; 100, 200 and 300 mg/kg; 30, 60 and 60 min before Diazepam) does not induce a muscle relaxant activity and shows muscle relaxant activity compared to normal saline, and this effect was more than diazepam in the traction test[3]. Carbenoxolone (intraperitoneal injection; 100, 200 and 300 mg/kg; 30, 60 and 60 min before Pentylenetetrazole) significantly increases sleeping time and decreases latency in mice as a dose-dependent manner in Pentylenetetrazole (PTZ) Seizure model. The ED50 value is 83.3 mg/kg (%95 CL:556.29)[3]. Animal Model: Male BALB/c mice[3] Dosage: 100, 200 and 300 mg/kg Administration: Intraperitoneal injection; 30, 60 and 60 min before Pentylenetetrazole Result: Significantly increased the sleeping time in mice.
References

[1]. W L Duax, et al. Steroid Dehydrogenase Structures, Mechanism of Action, and Disease. Vitam Horm. 2000;58:121-48.

[2]. Hossein Hosseinzadeh, et al. Anticonvulsant, Sedative and Muscle Relaxant Effects of Carbenoxolone in Mice. BMC Pharmacol. 2003 Apr 29;3:3.

[3]. Ismar R Haga, et al. Carbenoxolone-mediated Cytotoxicity Inhibits Vaccinia Virus Replication in a Human Keratinocyte Cell Line. Sci Rep. 2018 Nov 16;8(1):16956.

 Chemical & Physical Properties

Boiling Point 687.4ºC at 760 mmHg
Molecular Formula C34H48Na2O7
Molecular Weight 614.72000
Flash Point 211.6ºC
Exact Mass 614.32000
PSA 123.63000
LogP 4.15890

 MSDS


Section1. IDENTIFICATION OF THE SUBSTANCE/MIXTURE
Product identifiers
Product name: Carbenoxolone disodium salt
CAS-No.: 7421-40-1
Relevant identified uses of the substance or mixture and uses advised against
Identified uses: Laboratory chemicals, Manufacture of substances



Section2. HAZARDS IDENTIFICATION
Classification of the substance or mixture
Classification according to Regulation (EC) No 1272/2008 [EU-GHS/CLP]
Eye irritation (Category 2)
Classification according to EU Directives 67/548/EEC or 1999/45/EC
Irritating to eyes.
Label elements
Labelling according Regulation (EC) No 1272/2008 [CLP]
Pictogram
Signal wordWarning
Hazard statement(s)
H319Causes serious eye irritation.
Precautionary statement(s)
P305 + P351 + P338IF IN EYES: Rinse cautiously with water for several minutes. Remove
contact lenses, if present and easy to do. Continue rinsing.
Supplemental Hazardnone
Statements
According to European Directive 67/548/EEC as amended.
Hazard symbol(s)
R-phrase(s)
R36Irritating to eyes.
S-phrase(s)
S26In case of contact with eyes, rinse immediately with plenty of water and
seek medical advice.
S36Wear suitable protective clothing.
Other hazards - none

Section3. COMPOSITION/INFORMATION ON INGREDIENTS
Substances
: 3β-Hydroxy-11-oxoolean-12-en-30-oic acid 3-hemisuccinate
Synonyms
Formula: C34H48Na2O7
Molecular Weight: 614,72 g/mol
ComponentConcentration
Carbenoxolone disodium
CAS-No.7421-40-1-
EC-No.231-044-0

Section4. FIRST AID MEASURES
Description of first aid measures
General advice
Consult a physician. Show this safety data sheet to the doctor in attendance.
If inhaled
If breathed in, move person into fresh air. If not breathing, give artificial respiration. Consult a physician.
In case of skin contact
Wash off with soap and plenty of water. Consult a physician.
In case of eye contact
Rinse thoroughly with plenty of water for at least 15 minutes and consult a physician.
If swallowed
Never give anything by mouth to an unconscious person. Rinse mouth with water. Consult a physician.
Most important symptoms and effects, both acute and delayed
To the best of our knowledge, the chemical, physical, and toxicological properties have not been
thoroughly investigated.
Indication of any immediate medical attention and special treatment needed
no data available

Section5. FIREFIGHTING MEASURES
Extinguishing media
Suitable extinguishing media
Use water spray, alcohol-resistant foam, dry chemical or carbon dioxide.
Special hazards arising from the substance or mixture
Carbon oxides, Sodium oxides
Advice for firefighters
Wear self contained breathing apparatus for fire fighting if necessary.
Further information
no data available

Section6. ACCIDENTAL RELEASE MEASURES
Personal precautions, protective equipment and emergency procedures
Use personal protective equipment. Avoid dust formation. Avoid breathing vapors, mist or gas. Ensure
adequate ventilation. Avoid breathing dust.
Environmental precautions
Do not let product enter drains.
Methods and materials for containment and cleaning up
Pick up and arrange disposal without creating dust. Sweep up and shovel. Keep in suitable, closed
containers for disposal.
Reference to other sections
For disposal see section 13.

Section7. HANDLING AND STORAGE
Precautions for safe handling
Avoid contact with skin and eyes. Avoid formation of dust and aerosols.
Provide appropriate exhaust ventilation at places where dust is formed.
Conditions for safe storage, including any incompatibilities
Store in cool place. Keep container tightly closed in a dry and well-ventilated place.
Recommended storage temperature: 2 - 8 °C
Specific end uses
no data available

Section8. EXPOSURE CONTROLS/PERSONAL PROTECTION
Control parameters
Components with workplace control parameters
Exposure controls
Appropriate engineering controls
Handle in accordance with good industrial hygiene and safety practice. Wash hands before breaks and
at the end of workday.
Personal protective equipment
Eye/face protection
Safety glasses with side-shields conforming to EN166 Use equipment for eye protection tested
and approved under appropriate government standards such as NIOSH (US) or EN 166(EU).
Skin protection
Handle with gloves. Gloves must be inspected prior to use. Use proper glove removal technique
(without touching glove's outer surface) to avoid skin contact with this product. Dispose of
contaminated gloves after use in accordance with applicable laws and good laboratory practices.
Wash and dry hands.
The selected protective gloves have to satisfy the specifications of EU Directive 89/686/EEC and
the standard EN 374 derived from it.
Body Protection
impervious clothing, The type of protective equipment must be selected according to the
concentration and amount of the dangerous substance at the specific workplace.
Respiratory protection
For nuisance exposures use type P95 (US) or type P1 (EU EN 143) particle respirator.For higher
level protection use type OV/AG/P99 (US) or type ABEK-P2 (EU EN 143) respirator cartridges.
Use respirators and components tested and approved under appropriate government standards
such as NIOSH (US) or CEN (EU).

Section9. PHYSICAL AND CHEMICAL PROPERTIES
Information on basic physical and chemical properties
a) AppearanceForm: solid
b) Odourno data available
c) Odour Thresholdno data available
d) pHno data available
e) Melting point/freezingno data available
point
f) Initial boiling point and no data available
boiling range
g) Flash pointno data available
h) Evaporation rateno data available
i) Flammability (solid, gas) no data available
j) Upper/lowerno data available
flammability or
explosive limits
k) Vapour pressureno data available
l) Vapour densityno data available
m) Relative densityno data available
n) Water solubilityno data available
o) Partition coefficient: n- no data available
octanol/water
p) Autoignitionno data available
temperature
q) Decompositionno data available
temperature
r) Viscosityno data available
s) Explosive propertiesno data available
t) Oxidizing propertiesno data available
Other safety information
no data available

Section10. STABILITY AND REACTIVITY
Reactivity
no data available
Chemical stability
no data available
Possibility of hazardous reactions
no data available
Conditions to avoid
no data available
Incompatible materials
no data available
Hazardous decomposition products
Other decomposition products - no data available

Section11. TOXICOLOGICAL INFORMATION
Information on toxicological effects
Acute toxicity
LD50 Oral - rat - 2.450 mg/kg
Remarks: Cardiac:Pulse rate. Respiratory disorder Skin and Appendages: Other: Hair.
Skin corrosion/irritation
no data available
Serious eye damage/eye irritation
no data available
Respiratory or skin sensitization
no data available
Germ cell mutagenicity
no data available
Carcinogenicity
IARC:No component of this product present at levels greater than or equal to 0.1% is identified as
probable, possible or confirmed human carcinogen by IARC.
Reproductive toxicity
no data available
Specific target organ toxicity - single exposure
no data available
Specific target organ toxicity - repeated exposure
no data available
Aspiration hazard
no data available
Potential health effects
InhalationMay be harmful if inhaled. May cause respiratory tract irritation.
IngestionMay be harmful if swallowed.
SkinMay be harmful if absorbed through skin. May cause skin irritation.
EyesCauses serious eye irritation.
Signs and Symptoms of Exposure
To the best of our knowledge, the chemical, physical, and toxicological properties have not been
thoroughly investigated.
Additional Information
RTECS: RK0250000

Section12. ECOLOGICAL INFORMATION
Toxicity
no data available
Persistence and degradability
no data available
Bioaccumulative potential
no data available
Mobility in soil
no data available
Results of PBT and vPvB assessment
no data available
Other adverse effects
no data available

Section13. DISPOSAL CONSIDERATIONS
Waste treatment methods
Product
Offer surplus and non-recyclable solutions to a licensed disposal company. Dissolve or mix the material
with a combustible solvent and burn in a chemical incinerator equipped with an afterburner and scrubber.
Contaminated packaging
Dispose of as unused product.

Section14. TRANSPORT INFORMATION
UN number
ADR/RID: -IMDG: -IATA: -
UN proper shipping name
ADR/RID: Not dangerous goods
IMDG: Not dangerous goods
IATA:Not dangerous goods
Transport hazard class(es)
ADR/RID: -IMDG: -IATA: -
Packaging group
ADR/RID: -IMDG: -IATA: -
Environmental hazards
ADR/RID: noIMDG Marine pollutant: noIATA: no
Special precautions for user
no data available

Section15. REGULATORY INFORMATION
This safety datasheet complies with the requirements of Regulation (EC) No. 1907/2006.
Safety, health and environmental regulations/legislation specific for the substance or mixture
no data available
Chemical Safety Assessment
no data available

Section16. OTHER INFORMATION
Further information
Copyright 2012 Co. LLC. License granted to make unlimited paper copies for internal use
only.
The above information is believed to be correct but does not purport to be all inclusive and shall be
used only as a guide. The information in this document is based on the present state of our knowledge
and is applicable to the product with regard to appropriate safety precautions. It does not represent any
guarantee of the properties of the product. Corporation and its Affiliates shall not be held
liable for any damage resulting from handling or from contact with the above product. See
and/or the reverse side of invoice or packing slip for additional terms and conditions of sale.

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
RK0250000
CHEMICAL NAME :
Olean-12-en-30-oic acid, 3-beta-hydroxy-11-oxo-, hydrogen succinate, disodium salt
CAS REGISTRY NUMBER :
7421-40-1
LAST UPDATED :
199610
DATA ITEMS CITED :
13
MOLECULAR FORMULA :
C34-H48-O7.2Na
MOLECULAR WEIGHT :
614.80
WISWESSER LINE NOTATION :
T F6 E6 B666 DO BUTJ F1 IOV2VQ J1 J1 N1 O1 R1 U1VQ U1 &-NA- 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
120 mg/kg/6W
TOXIC EFFECTS :
Vascular - BP elevation not characterized in autonomic section Nutritional and Gross Metabolic - changes in potassium
REFERENCE :
CMAJAX Canadian Medical Association Journal. (Canadian Medical Assoc., POB 8650, Ottawa, ON K1G 0G8, Canada) V.1- 1911- Volume(issue)/page/year: 117,1155,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2450 mg/kg
TOXIC EFFECTS :
Cardiac - pulse rate Lungs, Thorax, or Respiration - respiratory depression Skin and Appendages - hair
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,263,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
92 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
FRMCE8 Farmaco. (Societa Chimica Italiana, Corso Strada Nova, 86, Casella Postale 227, 27100 Pavia, Italy) V.44- 1989- Volume(issue)/page/year: 49,281,1994
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
1515 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
120 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
21NDAB "Symposium on Carbenoxolone Sodium," Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968 Volume(issue)/page/year: -,6,1968
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
198 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
21NDAB "Symposium on Carbenoxolone Sodium," Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968 Volume(issue)/page/year: -,6,1968
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
3900 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
371 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 10,710,1979
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
1060 mg/kg
TOXIC EFFECTS :
Behavioral - altered sleep time (including change in righting reflex) Behavioral - tremor
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,263,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
371 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Cardiac - pulse rate
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,263,1976
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
2 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
21NDAB "Symposium on Carbenoxolone Sodium," Robson, J.M., and F.M. Sullivan, eds., London, Butterworth, 1968 Volume(issue)/page/year: -,6,1968 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
36400 mg/kg/26W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume decreased Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Nutritional and Gross Metabolic - weight loss or decreased weight gain
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,859,1976
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
12 gm/kg/30D-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - other changes in urine composition Endocrine - changes in thymus weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 11,831,1976

 Safety Information

Hazard Codes Xn
Risk Phrases 22-36
Safety Phrases 26-36
WGK Germany 3
RTECS RK0250000

 Synonyms

sodium carbenoxolone
pyrogastrone
CARBENOXOLONE SODIUM
EINECS 231-044-0
ulcus-tablinen
neogel
sanodin
Carbenoxolon-Dinatriumsalz
duogastrone
Carbenoxalone Sodium
carbenoxolone disodium
Biogastrone
MFCD00079043
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