Lower Price High purity 99% factory price CAS 144701-48-4 Telmisartan

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Use of Telmisartan

Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.

Telmisartan (telmisartan), chemical name 4'-[(1,4'-dimethyl-2'-propyl[2,6'-bis-1H-benzimidazole]-1'-yl) Methyl]-[1,1'-dibiphenyl]-2-carboxylic acid, molecular formula C33H30N4O2, is white or off-white crystalline powder, odorless and tasteless. It is soluble in chloroform, slightly soluble in dichloromethane or dimethylformamide, slightly soluble in methanol, very slightly soluble in ethanol, almost insoluble in water, and easily soluble in 1mol/L sodium hydroxide solution. Very slightly soluble in 0.1mol/L hydrochloric acid solution.
Molecular structure data
1. Molar refractive index: 154.51
2. Molar volume (cm/mol): 414.9
3. Isotonic specific volume (90.2K): 1096.2
4. Surface tension (dyne/cm): 48.7
5. Polarizability (10-24cm3): 61.25 [2]
Physical and chemical properties
Appearance and properties: white or off-white crystalline powder
Density: 1.16
Melting point: 261-263°C
Boiling point: 771.9ºC at 760mmHg
Flash point: 420.6ºC
Refractive index: 1.624
Water solubility: insoluble
Stability: Stable under normal temperature and pressure.
Storage conditions: Store in a cool, dry place (25ºC). The bottle should be kept tightly closed.
Vapor pressure: 0mmHg at 25°C

For the treatment of essential hypertension.
Non-peptide angiotensin II receptor antagonists can selectively and hardly reverse block ATI receptors without affecting other receptor systems. Used for mild to moderate hypertension. Telmisartan is a new type of blood pressure lowering drug, a specific angiotensin II receptor (AT) antagonist, used to treat essential hypertension. Substitute angiotensin II receptor and AT I receptor subtype (known angiotensin II action site) high-affinity binding. Telmisartan does not have any agonist effect at the AT receptor site, and selectively binds to the AT receptor, and the binding effect is long-lasting. It has no affinity for other receptors (including AT2 and other AT receptors with fewer features). The function of the above-mentioned other receptors is not yet known. As Telmisartan leads to an increase in the level of angiotensin II, the possible receptor overstimulation effect is also unknown. Telmisartan does not inhibit human plasma renin, nor does it block ion channels. It does not inhibit angiotensin-converting enzyme II, which can also degrade the adverse reactions caused by the enhanced bradykinin effect. In humans, 80 mg of telmisartan can almost completely inhibit the increase in blood pressure caused by angiotensin II. The inhibitory effect lasts for 24 hours and can still be measured at 48 hours. The antihypertensive effect is gradually obvious within 3 hours after the first dose. The maximum antihypertensive effect can be obtained 4 weeks after the start of treatment and can be maintained during long-term treatment. If the treatment is suddenly interrupted, the blood pressure gradually returns to the pre-treatment level after a few days without rebound hypertension. In a clinical trial study that directly compared two hypertension drugs, the incidence of dry cough in the treatment group was significantly lower than that in the angiotensin-converting enzyme inhibitor treatment group.

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