Clofilium tosylate

Modify Date: 2024-01-02 19:28:43

Clofilium tosylate Structure
Clofilium tosylate structure
Common Name Clofilium tosylate
CAS Number 92953-10-1 Molecular Weight 510.172
Density N/A Boiling Point N/A
Molecular Formula C28H44ClNO3S Melting Point N/A
MSDS Chinese USA Flash Point N/A
Symbol GHS07
GHS07
Signal Word Warning

 Use of Clofilium tosylate


Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent[1].

 Names

Name 4-(4-chlorophenyl)butyl-diethyl-heptylazanium,4-methylbenzenesulfonate
Synonym More Synonyms

 Clofilium tosylate Biological Activity

Description Clofilium tosylate, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Antiarrhythmic agent[1].
Related Catalog
Target

Potassium channel[1]

In Vitro HL-60 cells treated with Clofilium (0-20 μM; 24, 48, and 72 hours) lead to suppression of viability and proliferation in both time and concentration-dependent manners. Cell viability decreases significantly in HL-60 cells treated with 2.5 μM to 10 μM of Clofilium[1]. Clofilium (10 μM, 12 hours) induces the proteolytic cleavage of inactive procaspase-3, p34 into its active form, p17 and subsequent cleavage of its substrate PARP at 2 h after exposure to 10 mM Clofilium. However, there is no significant change in expression of Bcl-2 and Bax proteins[1]. Cell Viability Assay[1] Cell Line: HL-60 cells Concentration: 0-20 μM Incubation Time: 24, 48, and 72 hours Result: Inhibited HL-60 cells with IC50s of 6.3 μM for 24 hours, 3.4 μM for 48 hours, 2.4 μM for 72 hours, respectively. Western Blot Analysis[1] Cell Line: HL-60 cells Concentration: 10 μM Incubation Time: 12 hours Result: Induced proteolytic cleavage of caspase-3 and subsequent cleavage of its substrate, PARP, while Bcl-2 and Bax proteins were unaltered.
References

[1]. Choi BY, et al. Clofilium, a potassium channel blocker, induces apoptosis of human promyelocytic leukemia (HL-60) cells via Bcl-2-insensitive activation of caspase-3. Cancer Lett. 1999 Dec 1;147(1-2):85-93.

 Chemical & Physical Properties

Molecular Formula C28H44ClNO3S
Molecular Weight 510.172
Exact Mass 509.273041
PSA 65.58000
LogP 8.46960
Storage condition 2-8℃

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
CY9040870
CAS REGISTRY NUMBER :
92953-10-1
LAST UPDATED :
198910
DATA ITEMS CITED :
2
MOLECULAR FORMULA :
C21-H37-Cl-N.C7-H7-O3-S
MOLECULAR WEIGHT :
510.24

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
456 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 2,103,1984
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
416 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 2,103,1984

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H302
Personal Protective Equipment dust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard Codes Xn: Harmful;
Risk Phrases 22
Safety Phrases 36
RIDADR NONH for all modes of transport
RTECS CY9040870

 Articles3

More Articles
Block of heart potassium channels by clofilium and its tertiary analogs: relationship between drug structure and type of channel blocked.

Mol. Pharmacol. 34 , 60-66, (1988)

The whole-cell arrangement of the patch clamp was used to study delayed rectifier and inward rectifier K channels in isolated guinea pig ventricular cells. Block of these channels by an externally app...

The differential response of normal and ischaemic Purkinje fibres to clofilium, d-sotalol and bretylium.

Cardiovasc. Res. 23 , 554-559, (1989)

To determine whether ischaemic tissue is more sensitive than normal tissue to class III anti-arrhythmic agents, we studied the effects of the class III agents clofilium, d-sotalol and bretylium on nor...

Clofilium and other class III agents. Steinberg, et al., Williams, et al.

Handbook of Experimental Pharmacology Berlin Heidelberg 89 , 389, (1989)

 Synonyms

N-[4-(4-Chlorophenyl)butyl]-N,N-diethyl-1-heptanaminium 4-methylbenzenesulfonate
Benzenebutanaminium,4-chloro-N,N-diethyl-N-heptyl-,salt with 4-methylbenzenesulfonicacid (1:1)
4-Chloro-N,N-diethyl-N-heptylbenzenebutanaminium tosylate
Clofilium tosylate
Prestwick_682
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