CAS 396-01-0|Triamterene

Introduction:Basic information about CAS 396-01-0|Triamterene, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameTriamterene
CAS Number396-01-0Molecular Weight253.26300
Density1.502 g/cm3Boiling Point573.4ºC at 760 mmHg
Molecular FormulaC12H11N7Melting Point316°C
MSDSChineseUSAFlash Point11 °C
Symbol
GHS07
Signal WordWarning

Names

Name2,4,7-Triamino-6-Phenylpteridine
SynonymMore Synonyms

Triamterene BiologicalActivity

DescriptionTriamterene blocks epithelial Na+ channel (ENaC) in a voltage-dependent manner, which used as a mild diuretic.Target: Sodium ChannelTriamterene blocked rENaC in a voltage-dependent manner, and was 100-fold less potent than amiloride at pH 7.5. At -90 mV and -40 mV, the IC50 values were 5 microM and 10 microM, respectively. The blockage by triamterene, which is a weak base with a pKa of 6.2, was dependent on the extracellular pH. The IC50 was 1 microM at pH 6.5 and only 17 microM at pH 8.5 [1]. Triamterene (TA) is partly eliminated by a first-pass-effect. The main metabolite of TA is OH-TA-ester, which is pharmacologically active [2].
Related CatalogSignaling Pathways >>Membrane Transporter/Ion Channel >>Sodium ChannelResearch Areas >>Metabolic Disease
References

[1]. Busch, A.E., et al., Blockade of epithelial Na+ channels by triamterenes - underlying mechanisms and molecular basis. Pflugers Arch, 1996. 432(5): p. 760-6.

[2]. Gilfrich, H.J., et al., Pharmacokinetics of triamterene after i.v. administration to man: determination of bioavailability. Eur J Clin Pharmacol, 1983. 25(2): p. 237-41.

Chemical & Physical Properties

Density1.502 g/cm3
Boiling Point573.4ºC at 760 mmHg
Melting Point316°C
Molecular FormulaC12H11N7
Molecular Weight253.26300
Flash Point11 °C
Exact Mass253.10800
PSA129.62000
LogP2.57700
InChIKeyFNYLWPVRPXGIIP-UHFFFAOYSA-N
SMILESNc1nc(N)c2nc(-c3ccccc3)c(N)nc2n1
Storage condition2-8°C
Water Solubility<0.1 G/100 ML AT 20 ºC

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UO3470000
CHEMICAL NAME :
Pteridine, 2,4,7-triamino-6-phenyl-
CAS REGISTRY NUMBER :
396-01-0
BEILSTEIN REFERENCE NO. :
0266723
LAST UPDATED :
199612
DATA ITEMS CITED :
21
MOLECULAR FORMULA :
C12-H11-N7
MOLECULAR WEIGHT :
253.30
WISWESSER LINE NOTATION :
T66 BN DN GN JNJ CZ EZ HR& IZ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
42 mg/kg/3W-I
TOXIC EFFECTS :
Liver - hepatitis (hepatocellular necrosis), zonal Nutritional and Gross Metabolic - body temperature increase
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
400 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 - rat
DOSE/DURATION :
200 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 :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
285 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 :
249 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 :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
620 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 :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
25077 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Unreported
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
25 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 :
157 mg/kg/3W-I
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2700 mg/m3/15D-C
TOXIC EFFECTS :
Endocrine - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
6370 mg/m3/13W-C
TOXIC EFFECTS :
Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
8190 mg/kg/13W-C
TOXIC EFFECTS :
Endocrine - other changes Blood - changes in leukocyte (WBC) count Nutritional and Gross Metabolic - weight loss or decreased weight gain
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
21840 mg/kg/2Y-C
TOXIC EFFECTS :
Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
34944 mg/kg/2Y-C
TOXIC EFFECTS :
Tumorigenic - neoplastic by RTECS criteria Liver - tumors

MUTATION DATA

TYPE OF TEST :
Sister chromatid exchange
TEST SYSTEM :
Rodent - hamster Lung
DOSE/DURATION :
12600 ug/L
REFERENCE :
SNSHBT Senshokutai. Chromosome. (Sensyokutai Gakkai, Kaokusai Kirisutokyo Daigaku, Mitaka, Tokyo-to, Japan) No.1- 1946- Adopted new numbering in 1976. Volume(issue)/page/year: (20),574,1980 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5679 No. of Facilities: 60 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 587 (estimated) No. of Female Employees: 310 (estimated)

Safety Information

Symbol
GHS07
Signal WordWarning
Hazard StatementsH302-H315-H319-H335
Precautionary StatementsP301 + P312 + P330-P305 + P351 + P338
Personal Protective Equipmentdust mask type N95 (US);Eyeshields;Faceshields;Gloves
Hazard CodesXn:Harmful;
Risk PhrasesR22;R36/37/38
Safety PhrasesS26-S36/37/39-S45-S33-S24-S16-S7
RIDADR2811
WGK Germany3
RTECSUO3470000
Packaging GroupIII
Hazard Class6.1(b)
HS Code2933990090

Customs

HS Code2933990090
Summary2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

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Synonyms

Triamterene
MFCD00006708
6-Phenylpteridine-2,4,7-triamine
2,4,7-Triamino-6-phenylpteridine,6-Phenyl-2,4,7-pteridinetriamine
EINECS 206-904-3
2,4,7-Triamino-6-phenylpteridine 6-Phenyl-2,4,7-pteridinetriamine
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