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40180-04-9

40180-04-9 structure
40180-04-9 structure
  • Name: Tienilic acid
  • Chemical Name: tienilic acid
  • CAS Number: 40180-04-9
  • Molecular Formula: C13H8Cl2O4S
  • Molecular Weight: 331.17
  • Catalog: Research Areas Metabolic Disease
  • Create Date: 2018-06-11 15:19:40
  • Modify Date: 2024-01-06 13:22:56
  • Tienilic acid is a uricosuric diuretic. Tienilic acid possesses certain hepatotoxicity[1][3].
Name tienilic acid
Synonyms Tienilic acid
(2,3-Dichloro-4-(2-thienylcarbonyl)phenoxy)acetic acid
Tienilico acido
(2,3-Dichloro-4-(2-thiophenecarbonyl)phenoxy)acetic acid
Acidum tienilicum
TienilicAcid
Selacryn
acetic acid, [2,3-dichloro-4-(2-thienylcarbonyl)phenoxy]-
Diflurex
Ticrynafen Tienylic acid [2,3-Dichloro-4-(2-thienylcarbonyl)phenoxy]-acetic acid
[2,3-dichloro-4-(2-thenoyl)phenoxy]acetic acid
Acido tienilico
Acide tienilique
2,3-dichloro-4-(thien-2-ylcarbonyl)-phenoxyacetic acid
[2,3-dichloro-4-(thiophene-2-carbonyl)-phenoxy]-acetic acid
[2,3-Dichloro-4-(2-thienylcarbonyl)phenoxy]acetic acid
Acetic acid, 2-[2,3-dichloro-4-(2-thienylcarbonyl)phenoxy]-
Ticrex
{[2,3-dichloro-4-(2-thienylcarbonyl)phenyl]oxy}acetic acid
Ticrynafen
2-[2,3-dichloro-4-(thiophene-2-carbonyl)phenoxy]acetic acid
Thienylic acid
[2,3-dichloro-4-(thiophen-2-ylcarbonyl)phenoxy]acetic acid
Description Tienilic acid is a uricosuric diuretic. Tienilic acid possesses certain hepatotoxicity[1][3].
Related Catalog
In Vivo Tienilic acid (100 mg/lg in rats and mice, 5 mg/kg in pigs and dog; PO and IV; single dosage) is only found in plasma, eliminates by the biliary and the urinary fast, and exhibits small differences in the different species[2]. Tienilic acid (0-480 mg/kg; PO; for 28 days) decreases blood pressure, serum, uric acid hemoglobin, and increased S-GPT; induces unicellular necrosis of small groups of liver cells[3]. Animal Model: Rats, mice, pigs and dogs[2] Dosage: 100 mg/lg in rats and mice, 5 mg/kg in pigs and dogs Administration: PO and IV; single dosage Result: Only found in plasma with important bindings to the plasma proteins at the blood level; pharmacological action for several hours; eliminated by the biliary and particularly the urinary fast, practically total in the first 48 hours after administration; only small differences were observed for the parameters measured in the different species. Animal Model: Female and male Sprague-Dawley rats[3] Dosage: 0, 30, 120 and 480 mg/kg Administration: PO; for 28 days Result: Decreased blood pressure and serum uric acid at 30 mg/kg; decreased slightly hemoglobin and increased S-GPT at 120 and 480 mg/kg; significantly increase the liver weight and serum magnesium concentration in male rats, while the liver weight of female rats increased only slightly; besides, induced unicellular necrosis of small groups of liver cells.
References

[1]. Lemieux G, et al, Baverel G. Metabolic effects in man of tienilic acid, a new diuretic with uricosuric properties. Nephron. 1978;20(1):54-64.

[2]. Levron, J.C., et al. Pharmacokinetic study of 2,3-dichloro 4- (2-thienyl keto14C) phenoxyacetic acid (tienilic acid) in animals. European Journal of Drug Metabolism and Pharmacokinetics 2, 107–120 (1977).

[3]. Oker-Blom C, et al. Toxicological studies on tienilic acid in rats. Toxicol Lett. 1980;6(2):93-99.
Density 1.5±0.1 g/cm3
Boiling Point 534.6±50.0 °C at 760 mmHg
Melting Point 148-149ºC
Molecular Formula C13H8Cl2O4S
Molecular Weight 331.17
Flash Point 277.1±30.1 °C
Exact Mass 329.952026
PSA 91.84000
LogP 3.07
Vapour Pressure 0.0±1.5 mmHg at 25°C
Index of Refraction 1.632
Storage condition -20°C

CHEMICAL IDENTIFICATION

RTECS NUMBER :
AG9300000
CHEMICAL NAME :
Acetic acid, (2,3-dichloro-4-(2-thienylcarbonyl)phenoxy)-
CAS REGISTRY NUMBER :
40180-04-9
BEILSTEIN REFERENCE NO. :
1260086
LAST UPDATED :
199612
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C13-H8-Cl2-O4-S
MOLECULAR WEIGHT :
331.17
WISWESSER LINE NOTATION :
T5SJ BVR BG CG DO1VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
3571 ug/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - urine volume decreased
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
6666 ug/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
5 mg/kg
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - urine volume decreased
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
1275 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
318 mg/kg
TOXIC EFFECTS :
Kidney, Ureter, Bladder - urine volume increased
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
225 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
3360 mg/kg/28D-I
TOXIC EFFECTS :
Vascular - BP lowering not characterized in autonomic section Liver - changes in liver weight Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
6300 mg/kg/14D-I
TOXIC EFFECTS :
Liver - other changes Kidney, Ureter, Bladder - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - hepatic microsomal mixed oxidase (dealkylation, hydroxylation, etc.)

MUTATION DATA

TYPE OF TEST :
Mutation in mammalian somatic cells
TEST SYSTEM :
Rodent - hamster Lung
DOSE/DURATION :
100 umol/L
REFERENCE :
MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 157,1,1985
Hazard Codes Xi
RIDADR NONH for all modes of transport
RTECS AG9300000
HS Code 2934999090
Precursor  0

DownStream  1

HS Code 2934999090
Summary 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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