Telmisartan

SKU: T0460

Category: API's & Intermediates

Synonyms: BIBR 277 , Micardis , Pritor , 4'[(1,4'-Dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl][1,1'-biphenyl]-2-carboxylic acid; 144701-48-4
CAS-Number: C₃₃H₃₀N₄O₂
Molecular Formula: 514.62
Molecular Weight

Product Data
Handling
Safety Information
Details

Specifications

Purity: ≥98% (HPLC)
Identity: 1H-NMR
Appearance: White to off-white solid

Properties

Solvents: DMSO, chloroform, DMF, ethanol

Short Term Storage: RT
Use / Stability: Stable for at least 2 years after receipt when stored at RT.
Handling Advice: Protect from light and moisture.
Long Term Storage: RT
Shipping: AMBIENT

Transportation: Not dangerous goods

Description: Telmisartan is a nonpeptide angiotensin II receptor antagonist which selectively inhibits the angiotensin II AT1 receptor subtype (Ki=3.7nM). Telmisartan exhibits antihypertensive activity in a renin-dependent model of hypertension. In addition to blocking the renin–angiotensin system (RAS), telmisartan acts as a selective modulator of peroxisome proliferator-activated receptor gamma (PPAR-?), a central regulator of insulin and glucose metabolism and improving insulin sensitivity. It is believed that telmisartan's dual mode of action may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease (CVD). Through these actions, telmisartan potently reduces blood pressure in various animal models of hypertension, diminishing cardiac hypertrophy, cardiovascular and renal risk and glomerulosclerosis. Furthermore, telmisartan inhibits proliferation in several cancer models by inducing apoptosis and cell cycle arrest.
References: (1) U.J. Ries, et al., J. Med. Chem. 36, 4040 (1993) , (2) W. Wienen, et al., Br. J. Pharmacol. 110, 245 (1993) , (3) K.J. McClellan & A. Markham, Drugs 56, 1039 (1998) , (4) S.C. Benson, et al., Hypertension 43, 993 (2004) , (5) X. Rong, et al., J. Pharmacol. Exp. Ther. 331, 1096 (2009) , (6) R.E. Schmieder, et al., J. Nephrol. 24, 263 (2011) , (7) J.E. Frampton, Drugs 71, 651 (2011) (Review) , (8) T. Kozako, et al., FEBS Open Bio 6, 442 (2016) , (9) E. Samukawa, et al., Int. J. Oncol. 51, 1674 (2017)
InChi Key: RMMXLENWKUUMAY-UHFFFAOYSA-N
Smiles: CN1C2=CC=CC=C2N=C1C3=CC(N(CC4=CC=C(C5=CC=CC=C5C(O)=O)C=C4)C(CCC)=N6)=C6C(C)=C3

Telmisartan is a nonpeptide angiotensin II receptor antagonist which selectively inhibits the angiotensin II AT1 receptor subtype (Ki=3.7nM). Telmisartan exhibits antihypertensive activity in a renin-dependent model of hypertension. In addition to blocking the renin–angiotensin system (RAS), telmisartan acts as a selective modulator of peroxisome proliferator-activated receptor gamma (PPAR-?), a central regulator of insulin and glucose metabolism and improving insulin sensitivity. It is believed that telmisartan’s dual mode of action may provide protective benefits against the vascular and renal damage caused by diabetes and cardiovascular disease (CVD). Through these actions, telmisartan potently reduces blood pressure in various animal models of hypertension, diminishing cardiac hypertrophy, cardiovascular and renal risk and glomerulosclerosis. Furthermore, telmisartan inhibits proliferation in several cancer models by inducing apoptosis and cell cycle arrest.

Artikelnummer: T0460 Kategorie: API's & Intermediates

Zusätzliche Information

Zusätzliche Information

Synonyms	BIBR 277, Micardis, Pritor, 4'[(1,4'-Dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl][1,1'-biphenyl]-2-carboxylic acid
Purity	≥98% (HPLC)
Appearance	White to off-white solid
CAS-Number	144701-48-4
Molecular Formula	C33H30N4O2
Molecular Weight	514.62
Identity	1H-NMR
Solvents	DMSO, chloroform, DMF, ethanol
Smiles	CN1C2=CC=CC=C2N=C1C3=CC(N(CC4=CC=C(C5=CC=CC=C5C(O)=O)C=C4)C(CCC)=N6)=C6C(C)=C3
InChi Key	RMMXLENWKUUMAY-UHFFFAOYSA-N
Shipping	AMBIENT
Short Term Storage	RT
Long Term Storage	RT
Handling Advice	Protect from light and moisture.
Use / Stability	Stable for at least 2 years after receipt when stored at RT.
Transportation	Not dangerous goods
References	(1) U.J. Ries, et al., J. Med. Chem. 36, 4040 (1993), (2) W. Wienen, et al., Br. J. Pharmacol. 110, 245 (1993), (3) K.J. McClellan & A. Markham, Drugs 56, 1039 (1998), (4) S.C. Benson, et al., Hypertension 43, 993 (2004), (5) X. Rong, et al., J. Pharmacol. Exp. Ther. 331, 1096 (2009), (6) R.E. Schmieder, et al., J. Nephrol. 24, 263 (2011), (7) J.E. Frampton, Drugs 71, 651 (2011) (Review), (8) T. Kozako, et al., FEBS Open Bio 6, 442 (2016), (9) E. Samukawa, et al., Int. J. Oncol. 51, 1674 (2017)
Quantity	10 mg, 50 mg, Bulk