Telmisartan Powder CAS 144701-48-4

Basic information of Telmisartan：

Telmisartan powder is a white or white-like crystalline powder, which is odorless. It is almost insoluble at pH = 3 ~ 9. Insoluble in strong acid (but soluble in hydrochloric acid). Soluble in strong alkali solution.

Telmisartan is an effective angiotensin II type 1 receptor antagonist, which can inhibit its activity, and its IC50 value is 9.2 nM.
As an angiotensin II receptor blocker, telmisartan has a particularly high affinity for angiotensin II receptor type I (AT1), which is 3000 times that of angiotensin II receptor type II (AT2). The half-life of telmisartan is as long as 24 hours, which is the longest and the most widely distributed in volume among similar drugs.

Pruduct name	Telmisartan powder
CAS	144701-48-4
Molecular formula	C33H30N4O2
Molecular weight	514.62
Melting point	261-263°C
Density	1.16
Boiling point	771.9±70.0 °C(Predicted)
Storage condition	2-8°C
Solubility	DMSO:>5 mg/mLat 60 °C
Appearance	white powder
Water solubility	insoluble

 

What is Telmisartan?

Telmisartan powder is a new antihypertensive drug and a specific angiotensin ⅱ receptor (AT ⅰ) antagonist, which is used to treat essential hypertension. Substituted angiotensin Ⅱ receptor binds to ATⅠ receptor subtype (known angiotensin Ⅱ action site) with high affinity. Telmisartan has no agonist effect on at ⅰ receptor site and selectively binds to at ⅰ receptor, and the binding effect is lasting. There is no affinity for other receptors (including AT2 and other AT receptors with less characteristics). The functions of these other receptors are unknown, and the possible receptor overstimulation effect due to the increase of angiotensin ⅱ level caused by telmisartan is also unknown. Telmisartan does not inhibit human plasma renin or block ion channels. It does not inhibit angiotensin-converting enzyme ⅱ, but it can also degrade the adverse reactions caused by the enhanced action of bradykinin. The administration of 80mg telmisartan in the human body can almost completely inhibit the increase of blood pressure caused by angiotensin ⅱ. The inhibitory effect lasted for 24 hours and was still detectable at 48 hours. The hypotensive effect gradually became 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 in the long-term treatment. If the treatment is suddenly interrupted, the blood pressure will gradually return to the pre-treatment level after a few days, without rebounding hypertension. The incidence of dry cough in the treatment group was significantly lower than that in the angiotensin-converting enzyme inhibitor treatment group.

Product Specification

What is the pharmacological mechanism of Telmisartan?

1. Hypotensive effect: Telmisartan powder is a reversible and competitive angiotensin Ⅱ receptor antagonist. Angiotensin Ⅱ synthesized by renin-angiotensin converting enzyme pathway and non-renin-angiotensin converting enzyme pathway binds to AT1 receptors on cell membranes of vascular smooth muscle, adrenal gland, kidney and heart, causing vasoconstriction, aldosterone release and water loss.
2. Reduce the heart load: when heart failure occurs, the product dilates arteries and veins, reducing the resistance or afterload of peripheral blood vessels; Reduce pulmonary capillary entrapment or preload, and also reduce pulmonary vascular resistance; So as to improve cardiac output, increase exercise tolerance and prolong exercise time.
3. Others: This product can also reverse left ventricular hypertrophy, protect kidney, promote urinary sodium and uric acid excretion, significantly reduce proteinuria, and obviously delay the progress of end-stage renal disease.

What is the synthetic method of Telmisartan?

2- N- propyl -4- methyl benzimidazole -6- carboxylic acid and N-methyl o-phenylenediamine reacted in paraformaldehyde at 150℃ and cyclized to form 2- n-propyl -4- methyl -6-(1- methyl benzimidazole -2- yl) benzimidazole. Then it was alkylated with tert-butyl 2-(4- bromomethylphenyl) benzoate in dimethyl sulfoxide in the presence of potassium tert-butoxide. The obtained product was hydrolyzed in dimethylformamide under the action of trifluoroacetic acid to obtain Telmisartan. Details are as follows:

What are the advantages and disadvantages of Telmisartan?

Advantages of Telmisartan:

1. Telmisartan powder has strong fat solubility, strong tissue penetration, high affinity with AT1 receptor of angiotensin II, and strong antagonistic effect on angiotensin II, so it is the strongest antihypertensive product of this kind.
2. The plasma half-life of telmisartan can reach 24 hours, which is the longest in this kind of products. Telmisartan has long-term characteristics and can effectively control 24-hour blood pressure. Telmisartan can reduce both high and low blood pressure at the same time, and the antihypertensive effect is stable and mild, with little blood pressure fluctuation. In vivo, 99% of telmisartan is metabolized by the liver, and only 1% is excreted by the kidney, which reduces blood pressure and does not increase the burden on the kidney.
3. In terms of safety, there are very few adverse drug reactions directly related to telmisartan, which is also a major advantage of telmisartan.

Disadvantages of Telmisartan:
1. The antihypertensive effect is slow, and it usually takes 2 ~ 4 weeks to achieve the antihypertensive effect. If the initial blood pressure is not up to standard, don't rush to increase or replace it, and insist on using blood pressure will gradually stabilize.
2. Telmisartan can reduce glomerular filtration function, leading to an increase in serum potassium and creatinine. Patients with renal insufficiency should be closely monitored during initial treatment.
3. Telmisartan has reproductive toxicity, which can lead to oligohydramnios and spontaneous abortion in pregnant women, resulting in fetal growth retardation, skeletal malformation, patent ductus arteriosus, lung and kidney hypoplasia and even death. Telmisartan should be banned in pregnant women.

In a word, telmisartan has outstanding advantages, clear antihypertensive effect, long action time, target organ protection, no increase in kidney burden, and good safety and tolerance. Telmisartan also has some disadvantages, such as slow onset, easy to cause the increase of serum potassium and creatinine, and reproductive toxicity, so we should pay attention to it in the use process.

Valsartan, Losartan carboxylic acid, Telmisartan and Irbesartan, which is the best? Let me give you a detailed answer:

1. Valsartan

Valsartan has moderate antihypertensive intensity and is suitable for mild to moderate essential hypertension. The advantages of this product are obvious. It has cardiovascular protection, can reduce the mortality and cardiovascular event risk of patients with myocardial infarction, significantly improve the prognosis of patients with heart failure, and can reduce fasting and postprandial blood sugar, prevent diabetes, and reduce urinary protein. It has the effect of protecting renal function and is the only antihypertensive product that has been proved to improve the quality of sexual life of patients with hypertension.

2. Losartan carboxylic acid

Losartan carboxylic acid is the first sartan drug in the world, which has long-term use, stable effects, and kidney protection. It can be used to treat hypertension and diabetic nephropathy and also has a certain uric acid lowering effect, so it is suitable for people with hypertension complicated with high uric acid. However, because it is the first generation of Sartan, its blood pressure is not high, its absorption is not high, only about 30% and its half-life is only 6~9 hours, which can not guarantee stable blood pressure reduction for 24 hours, and its price is more expensive than other sartans, so it is currently used less.

3. Telmisartan

Telmisartan has the advantages of a large antihypertensive range, long half-life, lasting curative effect, and cardiovascular protection, and is suitable for patients with hypertension and cardiovascular diseases or high-risk cardiovascular events, for example, for the follow-up treatment of patients with stroke and myocardial infarction. The disadvantage is that the antihypertensive effect is too obvious, and many people will have hypotension after using it, so pay attention to monitoring blood pressure after using it.

4. Irbesartan

Irbesartan has a good antihypertensive effect and lasting drug effect and is effective for diabetic nephropathy, atrial fibrillation, etc. It can reverse left ventricular hypertrophy and reduce urinary protein. It is an antihypertensive product approved by the state for the treatment of hypertension complicated with type 2 diabetes. However, it should be noted that irbesartan is mainly metabolized by the liver CYP2C9 enzyme, so it is not suitable for patients with liver dysfunction. At the same time, when using irbesartan, attention should be paid to its interaction with other products.

Generally speaking, these four products have their own advantages, and patients with hypertension can choose according to their own situation. It should be noted that no matter which one is used, it is necessary to do a good job in blood pressure monitoring and regular review to prevent side effects or hypertension complications.

Hot Tags: telmisartan powder cas 144701-48-4, China, suppliers, manufacturers, factory, customized, wholesale, buy, price, bulk, pure, producer, discount, for sale, in stock, free sample, raw powder, raw material, made in China