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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;timishatyan
        CBNumber:
        CB4266172
        Molecular Formula:
        C33H30N4O2
        Formula Weight:
        514.63
        MOL File:
        144701-48-4.mol

        Telmisartan Properties

        Melting point:
        261-263°C
        Boiling point:
        771.9±70.0 °C(Predicted)
        Density 
        1.16
        RTECS 
        DV2037500
        storage temp. 
        Hygroscopic, -20°C Freezer, Under Inert Atmosphere
        solubility 
        DMSO: >5 mg/mL at 60 °C
        form 
        solid
        pka
        3.86±0.36(Predicted)
        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 $140 2019-12-02 Buy
        Sigma-Aldrich 1643419 Telmisartan United States Pharmacopeia (USP) Reference Standard 144701-48-4 200mg $352.8 2019-12-02 Buy
        TCI Chemical T2861 Telmisartan >98.0%(HPLC)(T) 144701-48-4 1g $112 2019-12-02 Buy
        TCI Chemical T2861 Telmisartan >98.0%(HPLC)(T) 144701-48-4 5g $388 2019-12-02 Buy
        Alfa Aesar J61441 Telmisartan, 99% 144701-48-4 250mg $57.8 2019-12-02 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( 495)Suppliers
        Supplier Tel Fax Email Country ProdList Advantage
        Zhuhai Beri Medical Technology Co., Ltd 0756-8699456-
        +8607568699 456 sales@zhberi.com; China 140 58
        Guangzhou Kafen Biotech Co.,Ltd 18029243487 QQ:2355327168
        020-31121510 gy@yccreate.com China 4783 55
        Jiangsu United-value International Trading Co., Ltd. 0519-89885611 89885616 15312500313
        +86(519)89885615 luke.li@uvcs.cn.com China 476 58
        Foshan DaoQi Biological Co., Ltd. 15372409258
        0571-87068629 wcq@chembj.com China 2898 58
        Jiangsu Zhongbang Pharmaceutical Co., Ltd 025-87151129
        0086-25- 87151120 sales@chinaredsun.com China 142 58
        Suzhou Langen Biotechnology Co., Ltd. 13921996628
        +86-512-58875450 sales1@bio-langen.com China 110 58
        Beijing xinyanhui pharmaceutical research and development co., LTD
        1461866103@qq.com China 6077 58
        Absin Bioscience Inc. 021-38015121-
        zhouzz@absin.cn China 11550 58
        J & K SCIENTIFIC LTD. 010-82848833- ;010-82848833-
        86-10-82849933 jkinfo@jkchemical.com;market6@jkchemical.com China 96505 76
        Meryer (Shanghai) Chemical Technology Co., Ltd. 21-61259100-
        86-21-61259102 sh@meryer.com China 40268 62

        Related articles


        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

        144701-48-4(Telmisartan)Related Search:


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