Losartan potassium

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Names

[ Name ]:
Losartan potassium

[Synonym ]:
MK 954
potassium salt {2-Butyl-5-chloro-3-[2'-(1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazol-4-yl}-methanol
{2-BUTYL-5-CHLORO-3-[2'-(1H-TETRAZOL-5-YL)-BIPHENYL-4-YLMETHYL]-3H-IMIDAZOL-4-YL}-METHANOL POTASSIUM SALT
5-(4'-{[2-butyl-4-chloro-5-(hydroxyméthyl)-1H-imidazol-1-yl]méthyl}biphényl-2-yl)tétrazol-1-ide de potassium
Lortaan
Losartan potassium
2-BUTYL-4-CHLORO-1-[[2'-(1H-TETRAZOL-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1H-IMIDAZOLE-5-METHANOL MONOPOTASSIUM SALT
Losaprex
COZAAR
Losartan potassium salt
EINECS 200-287-4
Losartanpatassium
mk-0954
Du Pont 753
Losartan (potassium salt)
1H-imidazole-5-methanol, 2-butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, monopotassium salt
Losartan Potassium (DuP 753)
Potassium 5-(4'-{[2-butyl-4-chloro-5-(hydroxymethyl)-1H-imidazol-1-yl]methyl}biphenyl-2-yl)tetrazol-1-ide
LOSARTAN, POTASSIUM SALT
Potassium 5-(4'-{[2-butyl-4-chloro-5-(hydroxymethyl)-1H-imidazol-1-yl]methyl}-2-biphenylyl)tetrazol-1-ide
Aradois
Potassium (2-butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)methanolate
thanolpotassium
Potassium (2-butyl-4-chloro-1-{[2'-(1H-tetrazol-5-yl)-4-biphenylyl]methyl}-1H-imidazol-5-yl)methanolate
LOSARTAN MONOPOTASSIUM SALT
1H-Imidazole-5-methanol, 2-butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-, potassium salt (1:1)
LOSARTANPOTASSIUM
Losartan (potassium)
dupont753
MK-95
potassium (2-butyl-4-chloro-1-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)methanolate
LOSARTAN POTASSIUM, EP STAANDARD
LOSARTAN POTASSIUM(SUBJECT TO PATENT FREE)
DUP 753
MFCD02092704

Chemical & Physical Properties

[ Density]:
0.986 g/mL at 25 °C(lit.)

[ Boiling Point ]:
134 °C(lit.)

[ Melting Point ]:
−69 °C(lit.)

[ Molecular Formula ]:
C₂₂H₂₂ClKN₆O

[ Molecular Weight ]:
461.001

[ Flash Point ]:
76 °F

[ Exact Mass ]:
460.118073

[ PSA ]:
89.61000

[ LogP ]:
3.89590

[ Vapour Pressure ]:
1.55E-19mmHg at 25°C

[ Index of Refraction ]:
n20/D 1.387(lit.)

[ Storage condition ]:
Desiccate at RT

MSDS

Click to get detail MSDS

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: NI6755100

CHEMICAL NAME :: 1H-Imidazole-5-methanol, 2-butyl-4-chloro-1-((2'-(1H-tetrazol-5-yl)(1,1'-bi phenyl)-4-yl) methyl)-, monopotassium salt

CAS REGISTRY NUMBER :: 124750-99-8

LAST UPDATED :: 199701

DATA ITEMS CITED :: 11

MOLECULAR FORMULA :: C22-H23-Cl-N6-O.K

MOLECULAR WEIGHT :: 462.06

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3959,1994

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea Nutritional and Gross Metabolic - dehydration

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3959,1994

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1 gm/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3959,1994

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 400 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - dehydration

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3959,1994

TYPE OF TEST :: LD - Lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >320 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Gastrointestinal - hypermotility, diarrhea Gastrointestinal - nausea or vomiting

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3959,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 16695 mg/kg/53W-I

TOXIC EFFECTS :: Behavioral - food intake (animal) Gastrointestinal - changes in structure or function of salivary glands Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,4001,1994

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2450 mg/kg/14W-I

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands Gastrointestinal - nausea or vomiting

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 28,3969,1994 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 763 mg/kg

SEX/DURATION :: female 15-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 51,367,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2943 mg/kg

SEX/DURATION :: female 15-21 day(s) after conception lactating female 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 51,367,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2943 mg/kg

SEX/DURATION :: female 15-21 day(s) after conception lactating female 20 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Specific Developmental Abnormalities - urogenital system

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 51,367,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 9265 mg/kg

SEX/DURATION :: female 15 day(s) pre-mating female 0-19 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

REFERENCE :: TJADAB Teratology, The International Journal of Abnormal Development. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1968- Volume(issue)/page/year: 51,383,1995

Safety Information

[ Personal Protective Equipment ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
R36/37/38

[ Safety Phrases ]:
26-36/37/39

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
NI6755100

[ HS Code ]:
2933290090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

[2-(1H-Tetrazol-5-yl)phenyl]boronic acid
3-(4-Bromobenzyl)-2-butyl-4-chloro-1H-imidazol-5-ylmethanol
Losartan
Trityl losartan
2-BUTYL-4-CHLORO-5-(HYDROXYMETHYL)-1-{[2'-[(TRIPHENYLMETHYL)TETRAZOLE-5YL]BIPHENYL-4-YL]METHYL}IMIDAZOLE
Potassium hydroxide
Methanol
4'-[(2-Butyl-4-chloro-5-hydroxymethyl-1H-imidazol-1-yl)methyl]-1,1'-biphenyl-2-carbonitrile
4'-Methyl-2-cyanobiphenyl
4-Bromomethyl-2-cyanobiphenyl

DownStream

2-BUTYL-4-CHLORO-5-(HYDROXYMETHYL)-1-{[2'-[(TRIPHENYLMETHYL)TETRAZOLE-5YL]BIPHENYL-4-YL]METHYL}IMIDAZOLE
EXP 3174
Losartan Carboxaldehyde
Losartan

Customs

[ HS Code ]: 2933290090

[ Summary ]:
2933290090. other compounds containing an unfused imidazole ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Articles

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Bioorg. Med. Chem. 22(15) , 3931-7, (2014)

The 2-[(18)F]fluoro-3-pent-4-yn-1-yloxypyridine ([(18)F]FPyKYNE) analog of the potent non-peptide angiotensin II type 1 receptor (AT1R) blocker losartan was produced via click chemistry linking [(18)F...

Role of 5-HT7 receptors in the inhibition of the vasodepressor sensory CGRPergic outflow in pithed rats

Vascul. Pharmacol. 63(1) , 4-12, (2014)

The role of calcitonin gene-related peptide (CGRP) in the modulation of vascular tone has been widely documented. Indeed, electrical stimulation of the perivascular sensory outflow in pithed rats indu...

Simultaneous determination of polar pharmaceuticals and personal care products in biological organs and tissues.

J. Chromatogr. A. 1355 , 193-205, (2014)

In the present study, a sensitive and accurate isotope dilution method was developed for the simultaneous determination of 17 polar pharmaceutical and personal care product (PPCP) residues (logKow=1.4...

losartan potassium and hydrochlorothiazide
potassium,[2-butyl-5-chloro-1-[[2,3,5,6-tetradeuterio-4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanolate
Losartan Carboxaldehyde-d3
(2S,3S,4S,5R,6R)-6-[5-[2-[4-[[2-butyl-4-chloro-5-(hydroxymethyl)imidazol-1-yl]methyl]phenyl]phenyl]tetrazol-2-yl]-3,4,5-trihydroxyoxane-2-carboxylic acid
Losartan-d3 Carboxylic Acid
[5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-2-(4,4,4-trideuteriobutyl)imidazol-4-yl]methanol
2-Thiophenecarboxaldehyde, 5-ethenyl-
Hydrazinylmethanol
1H-3-benzazepin-2-amine
1-Bromodiamantane
N,N'-bis(4-methoxyphenyl)quinazoline-2,4-diamine
(3R,4R)-1-tert-Butyl-2-oxo-4-phenylazetidine-3-carbonitrile
tert-butyl N-(6-oxo-3,6-dihydro-2H-pyran-3-yl)carbamate
3,3-Dimethyl-2-oxobutanoyl chloride
Ceramide 7
2-((1-(3-chlorophenyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl)thio)-N-(6-methylbenzo[d]thiazol-2-yl)acetamide

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