CAS 396-01-0|Triamterene
| Common Name | Triamterene | ||
|---|---|---|---|
| CAS Number | 396-01-0 | Molecular Weight | 253.26300 |
| Density | 1.502 g/cm3 | Boiling Point | 573.4ºC at 760 mmHg |
| Molecular Formula | C12H11N7 | Melting Point | 316°C |
| MSDS | ChineseUSA | Flash Point | 11 °C |
| Symbol | GHS07 | Signal Word | Warning |
Names
| Name | 2,4,7-Triamino-6-Phenylpteridine |
|---|---|
| Synonym | More Synonyms |
Triamterene BiologicalActivity
| Description | Triamterene 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 Catalog | Signaling 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
| Density | 1.502 g/cm3 |
|---|---|
| Boiling Point | 573.4ºC at 760 mmHg |
| Melting Point | 316°C |
| Molecular Formula | C12H11N7 |
| Molecular Weight | 253.26300 |
| Flash Point | 11 °C |
| Exact Mass | 253.10800 |
| PSA | 129.62000 |
| LogP | 2.57700 |
| InChIKey | FNYLWPVRPXGIIP-UHFFFAOYSA-N |
| SMILES | Nc1nc(N)c2nc(-c3ccccc3)c(N)nc2n1 |
| Storage condition | 2-8°C |
| Water Solubility | <0.1 G/100 ML AT 20 ºC |
Toxicological Information
CHEMICAL IDENTIFICATION |
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)
- 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 Word | Warning |
| Hazard Statements | H302-H315-H319-H335 |
| Precautionary Statements | P301 + P312 + P330-P305 + P351 + P338 |
| Personal Protective Equipment | dust mask type N95 (US);Eyeshields;Faceshields;Gloves |
| Hazard Codes | Xn:Harmful; |
| Risk Phrases | R22;R36/37/38 |
| Safety Phrases | S26-S36/37/39-S45-S33-S24-S16-S7 |
| RIDADR | 2811 |
| WGK Germany | 3 |
| RTECS | UO3470000 |
| Packaging Group | III |
| Hazard Class | 6.1(b) |
| HS Code | 2933990090 |
Customs
| HS Code | 2933990090 |
|---|---|
| Summary | 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
Articles33
More Articles| [Clinical strategies for prevention of drug-induced urinary calculi]. Clin. Calcium 21(10) , 1457-63, (2011) Drug-induced urinary calculi, although they account for only 1-2% of urinary calculi, deserve consideration because most of them are preventable. In the drug-containing calculi resulting from the crys... | |
| Bioavailability study of triamterene and xipamide using urinary pharmacokinetic data following single oral dose of each drug or their combination. J. Pharm. Biomed. Anal. 61 , 78-85, (2012) An efficient chromatographic method for the simultaneous determination of triamterene (TRI) and xipamide (XIP) in urine samples, based on high performance liquid chromatography with photodiode array d... | |
| Spectrophotometric and spectrodensitometric determination of triamterene and xipamide in pure form and in pharmaceutical formulation. Drug Test. Anal. 2(3) , 113-21, (2010) Sensitive and validated UV-spectrophotometric, chemometric and TLC-densitometric methods were developed for determination of triamterene (TRM) and xipamide (XIP) in their binary mixture, formulated fo... |
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 |
