mersalyl

Mersalyl (Salirgan) is a potent vascular endothelial growth factor (VEGF) and hypoxia-inducible factor 1 (HIF-1) inducer. Mersalyl induces VEGF and ENO1 mRNA expression. Mersalyl shows diuresis effects[1][2][3].

Signaling Pathways >> Metabolic Enzyme/Protease >> HIF/HIF Prolyl-Hydroxylase

Research Areas >> Metabolic Disease

Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR

Mersalyl (100 µM) induces VEGF and ENO1 mRNA expression but inhibits EPO mRNA expression induced by hypoxia, DFO, or CoCl2[2]. Mersalyl (20 µM; 5 min) is a cell-impermeant organomercurial compound that reacts with free thiol groups in mitochondrial membrane protein[1]. RT-PCR[2] Cell Line: Hep3B cells Concentration: 100 µM Incubation Time: 6 h Result: Induced VEGF and ENO1 mRNA expression but inhibited EPO mRNA expression induced by hypoxia, DFO, or CoCl2.

Mersalyl (2.5-40 mg/kg; intramuscularly injection) shows diuresis effects in Rats[3]. Animal Model: Rats[3] Dosage: 2.5-40 mg/kg Administration: Intramuscularly injection Result: Significantly depressed in sulfhydryl concentration at 5 mg/kg.

[1]. Kowaltowski AJ, et al. Mitochondrial membrane protein thiol reactivity with N-ethylmaleimide or mersalyl is modified by Ca2+: correlation with mitochondrial permeability transition. Biochim Biophys Acta. 1997 Feb 15;1318(3):395-402.

[2]. Agani F, et al. Mersalyl is a novel inducer of vascular endothelial growth factor gene expression and hypoxia-inducible factor 1 activity. Mol Pharmacol. 1998 Nov;54(5):749-54.

[3]. FARAH A, et al. Histochemical studies on the site of action of mercurial diuretics. J Histochem Cytochem. 1955 Jul;3(4):271-3.

MOLECULAR FORMULA :

C13-H16-Hg-N-O6.Na

MOLECULAR WEIGHT :

505.88

WISWESSER LINE NOTATION :

QV1OR BVM1YO1&1-HG-Q &-NA-

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 :

17700 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 40,249,1951

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intramuscular

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

24 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 40,249,1951

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

118 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

JOCEAH Journal of Organic Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB 57136, West End Stn., Washington, DC 20037) V.1- 1936- Volume(issue)/page/year: 16,1879,1951

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

72600 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 40,249,1951

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - rabbit

DOSE/DURATION :

7 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 152,341,1930

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intramuscular

SPECIES OBSERVED :

Rodent - rabbit

DOSE/DURATION :

24500 ug/kg

REFERENCE :

JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 40,249,1951 *** REVIEWS *** ACGIH TLV-TWA 0.1 mg(Hg)/m3 (skin) DTLVS* The Threshold Limit Values (TLVs) and Biological Exposure Indices (BEIs) booklet issues by American Conference of Governmental Industrial Hygienists (ACGIH), Cincinnati, OH, 1996 Volume(issue)/page/year: TLV/BEI,1997 *** U.S. STANDARDS AND REGULATIONS *** MSHA STANDARD-air:TWA 0.05 mg(Hg)/m3 DTLWS* "Documentation of the Threshold Limit Values for Substances in Workroom Air," Supplements. For publisher information, see 85INA8. Volume(issue)/page/year: 3,22,1973 *** OCCUPATIONAL EXPOSURE LIMITS *** OEL-AUSTRALIA:TWA 0.05 mg(Hg)/m3;Skin JAN 1993 OEL-BELGIUM:TWA 0.05 mg(Hg)/m3;Skin JAN 1993 OEL-DENMARK:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-FINLAND:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-FRANCE:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-GERMANY:TWA 0.01 ppm (0.1 mg(Hg)/m3) JAN 1993 OEL-HUNGARY:TWA 0.02 mg(Hg)/m3;STEL 0.04 mg(Hg)/m3 JAN 1993 OEL-JAPAN:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-THE NETHERLANDS:TWA 0.05 mg(Hg)/m3;STEL 0.15 mg(Hg)/m3 JAN 1993 OEL-THE PHILIPPINES:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-POLAND:TWA 0.01 mg(Hg)/m3 JAN 1993 OEL-RUSSIA:TWA 0.05 mg(Hg)/m3;STEL 0.01 mg(Hg)/m3 JAN 1993 OEL-SWEDEN:TWA 0.05 mg(Hg)/m3 JAN 1993 OEL-THAILAND:STEL 0.05 mg(Hg)/m3 JAN 1993 OEL-UNITED KINGDOM:TWA 0.05 mg(Hg)/m3;STEL 0.15 mg(Hg)/m3 JAN 1993 OEL IN BULGARIA, COLOMBIA, JORDAN, KOREA check ACGIH TLV OEL IN NEW ZEALAND, SINGAPORE, VIETNAM check ACGIH TLV *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH RECOMMENDED EXPOSURE LEVEL (REL) : NIOSH REL TO MERCURY, ARYL AND INORGANIC-air:CL 0.1 mg/m3 (Sk) REFERENCE : NIOSH* National Institute for Occupational Safety and Health, U.S. Dept. of Health, Education, and Welfare, Reports and Memoranda. Volume(issue)/page/year: DHHS #92-100,1992