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Telmisartan

Chemical Properties Mechanisms of Action Side Effects Patent
Telmisartan
Telmisartan structure
CAS No.
144701-48-4
Chemical Name:
Telmisartan
Synonyms
TU-199;PRITOR;BIBR 277;MICARDIS;Telmisaran;TIMISHATAN;BIBR 277SE;TELMISARTAN;Telmisattan;TIMETAZIDINE
CBNumber:
CB4266172
Molecular Formula:
C33H30N4O2
Formula Weight:
514.63
MOL File:
144701-48-4.mol

Telmisartan Properties

Melting point:
261-263°C
Density 
1.16
RTECS 
DV2037500
storage temp. 
Hygroscopic, -20°C Freezer, Under Inert Atmosphere
solubility 
DMSO: >5 mg/mL at 60 °C
form 
solid
color 
white
Water Solubility 
insoluble
Merck 
14,9129
InChIKey
RMMXLENWKUUMAY-UHFFFAOYSA-N
CAS DataBase Reference
144701-48-4(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
Hazard Codes  Xi
Risk Statements  36/37/38
Safety Statements  22-24/25-36-26
WGK Germany  2
HS Code  2933995300

Telmisartan price More Price(15)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich PHR1855 Telmisartan Pharmaceutical Secondary Standard; Certified Reference Material 144701-48-4 500mg $137 2018-11-20 Buy
Sigma-Aldrich 1643419 Telmisartan United States Pharmacopeia (USP) Reference Standard 144701-48-4 200mg $348 2018-11-13 Buy
TCI Chemical T2861 Telmisartan >98.0%(HPLC)(T) 144701-48-4 1g $101 2018-11-22 Buy
TCI Chemical T2861 Telmisartan >98.0%(HPLC)(T) 144701-48-4 5g $352 2018-11-22 Buy
Alfa Aesar J61441 Telmisartan, 99% 144701-48-4 250mg $56.2 2018-11-13 Buy

Telmisartan Chemical Properties,Uses,Production

Chemical Properties

White or off-white crystalline powder, odorless and tasteless. Soluble in chloroform, slightly soluble in methanol, very slightly soluble in acetone, practically insoluble in water. Slightly soluble in 0.1mol/L hydrochloric acid, soluble in 0.1mol/L sodium hydroxide.
Absorption coefficient(E1%1cm):509~541

Mechanisms of Action

80mg of telmisartan for the human body will practically completely counter the high blood pressure caused by angiotension II. Effects will last for 24 and can still be detected within 48 hours. Blood pressure-lowering effects should gradually become apparent within 3 hours after the initial dose. If treatment is suddenly interrupted, blood pressure will return to the same level as before treatment in a matter of days, and there will be no rebound high blood pressure. In a clinical trial that compared two kinds of antihypertensive drugs, patients in the treatment group experienced lower rates of coughing than those in the group treated by angiotensin converting enzyme inhibitors.
Telmisartan has a half-life of 18~24 hours, and will take effect 1~4 hours after taken. Medicinal effects can last for as long as 35 hours, with a high (T/P) ratio and outstanding effects in controlling morning blood pressure. Thus, this medicine can effectively control blood pressure for 24 hours, and it meets the once-daily medicinal standard (40~80mg, qd).
Clinical effects and characteristics: Overall, Telmisartan has the following characteristics in comparison with other antihypertensive medicine: specific receptor effects, noticeable hypertensive effects, good diuretic effects, improvement of myocardial stenosis, safe usage, good tolerance, and convenient daily dosage.

Side Effects

In the placebo control experiment, the incidence rate of negative events for the Telmisartan group (41.4%) was similar to that of the placebo group (43.9%). Negative events were unrelated to dosage, sex, age, or race.
The following lists negative reactions were accumulated via the 5788 hypertensive patients that were treated with Telmisartan in the clinical trial.
Negative effects are categorized by incident rate as:
Very common (>1/10); common (>1/100, <1/10=); uncommon (>1/1000, <1/100=); rare (>1/10000, <1/1000=); very rare (<1/100000=)
Bodily reaction: Common: Back pain (e.g. sciatica), chest pain, flu-like symptoms, infection symptoms (e.g. urinary tract infection including cystitis). Uncommon: sight abnormality, sweating.
Central and peripheral nervous system: Common: vertigo.
Digestive system: Common: stomach pain, diarrhea, indigestion, gastrointestinal disorders. Rare: dry mouth, bloating.
Muscle skeletal system: Common: joint pain, leg cramps or leg pain, muscle pain. Rare: Tenosensitis symptoms.
Nervous system: Rare: anxiety.
Respiratory system: Common: upper respiratory tract infection, including pharyngitis and rhinitis.
Skin and accessory system: Common: Skin abnormalities such as eczema.
Additionally, since Telmisartan entered the market, there have been individual cases of erythema, itching, syncope, insomnia, depression, stomach discomfort, vomiting, hypotension, bradycardia, tachycardia, dyspnea, eosinophilia, thrombocytopenia, weakness, and reduced work efficiency. Similar to other angiotensin II receptor blockers, very few cases have reported vascular edema, nettles, and other negative reactions.
The laboratory found: compared to the placebo, the Telmisartan group occasionally exhibited lowered hemoglobin or raised uric acid. Any increase in serum creatinine or liver enzymes in the Telmisartan group was similar or lower than that of the placebo group.

Patent

Telmisartan was originally formulated by the German pharmaceutical company Boehringer Ingelheim; it earned the German patent EP502,314 in 1991, was first approved to enter the American market in November 1998, and then entered German, Philippines, Australian, Belgium, British, and other markets.

Description

Telmisartan was launched in the US for the treatment of hypertension. It can be prepared in eight steps starting with methyl 4-amino-3-methyl benzoate; the first and second cyclization into a benzimidazole ring occur at steps 4 and 6 respectively. Telmisartan blocks the action of angiotensin II (Ang II), the primary effector molecule of the renin-angiotensin-aldosterone system (RAAS). It is the sixth of this class of 《sartans》 to be marketed after the lead compound Losartan. Its long lasting effect (24h half-life) could be the main difference with other angiotensin II antagonists. Unlike several other agents in this category, its activity does not depend upon transformation into an active metabolite, the 1-O-acylglucuronide being the principal metabolite found in humans. Telmisartan is a potent competitive antagonist of AT1 receptors that mediate most of the important effects of angiotensin II while lacking affinity for the AT2 subtypes or other receptors involved in cardiovascular regulation. In several clinical studies, Telmisartan, at a once daily dosage, produced effective and sustained blood-pressure lowering effects with a low incidence of side effects (particularly treatment-related cough associated with ACE inhibitors in elderly patients).

Chemical Properties

White or off white crystalline powder

Originator

Boehringer Ingelheim (Germany)

Uses

cardiotonic

Uses

Telmisartan is an angiotensin II receptor antagonist.

Uses

anti-cancer agent

Uses

Used alone or in combination with other classes of antihypertensives for the treatment of hypertension. Also used in the treatment of diabetic nephropathy in hypertensive patients with type 2 diabetes mellitus, as well as the treatment of congestive heart

Definition

ChEBI: A member of the class of benzimidazoles used widely in the treatment of hypertension.

brand name

Micardis (Boehringer Ingelheim).

General Description

Telmisartan, 4'-[(1,4'-dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl]-[1,1'-biphenyl]-2-carboxylic acid (Micardis), does not appear to bear any structuralrelationship to this class, but there is actually a great dealof overlap in the chemical architecture with other agents. Thefirst, and most significant, difference is the replacement of theacidic tetrazole system with a simple carboxylic acid. Thisacid, like the tetrazole, plays a role in receptor binding. Thesecond difference is the lack of a carboxylic acid near the imidazolenitrogen that also contributes to receptor binding.As with irbesartan, however, there is not a need for this groupto be acidic but, rather, to be one that participates in receptorbinding. The second imidazole ring, much like a purine basein deoxyribonucleic acid (DNA), can hydrogen bond with theangiotensin II receptor.

Telmisartan Preparation Products And Raw materials

Raw materials

Preparation Products


Telmisartan Suppliers

Global( 479)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Jiangsu Zhongbang Pharmaceutical Co., Ltd.
025-87151996
025-87151996 [email protected] CHINA 32 55
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 [email protected] China 19918 60
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 [email protected] CHINA 3194 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
[email protected] CHINA 21752 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 [email protected] CHINA 20672 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 [email protected] CHINA 32447 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 [email protected] CHINA 892 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 [email protected] CHINA 24191 60
Hebei Chisure Biotechnology Co., Ltd.
+8613292890173
0311 66567340 [email protected] CHINA 1017 58
career henan chemical co
+86-371-86658258
[email protected] CHINA 30002 58

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View Lastest Price from Telmisartan manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-12-17 Telmisartan
144701-48-4
US $7.00 / kg 1kg 99% 100kg career henan chemical co

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