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    Telmisartan

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      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.

      SKU: T0460 Category: API's & Intermediates
      • Additional information

      Additional 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

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