TelmisartanA nonpeptide angiotensin II receptor type 1 antagonist

Telmisartan (CAS 144701-48-4)

Telmisartan | CAS 144701-48-4 is rated 5.0 out of 5 by 1.
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Synonym: Micardis; Pritor; BIBR 277
Application: A nonpeptide angiotensin II receptor type 1 antagonist
CAS Number: 144701-48-4
Purity: ≥98%
Molecular Weight: 514.62
Molecular Formula: C33H30N4O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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Telmisartan is an angiotensin II receptor blocker (ARB) that has high affinity for the angiotensin II receptor type 1 (AT1). Telmisartan interferes with the binding of angiotensin II to AT1 receptors in vascular smooth muscle and thus inhibits the vasoconstricting action of angiotensin II. Additionally, telmisartan is a selective modulator of peroxisome proliferator-activated receptor gamma (PPARγ), an essential regulator of insulin and glucose metabolism. Therefore, telmisartan is useful for studying hypertension.


References

1. Wienen, W., et al. 1993. Br. J. Pharmacol. 110: 245-252. PMID: 8220885
2. McClellan, K.J., et al. 1998. Drugs. 56: 1039-46. PMID: 9878991

Appearance :
Crystalline
Physical State :
Solid
Solubility :
Soluble in DMSO (13 mg/ml at 25° C), chloroform, DMF (~1.6 mg/ml), and ethanol (<1 mg/ml at 25° C). Insoluble in water.
Storage :
Store at room temperature
Melting Point :
261-263° C
Boiling Point :
~771.9° C at 760 mmHg (Predicted)
Density :
~1.2 g/cm3 (Predicted)
Refractive Index :
n20D 1.67 (Predicted)
IC50 :
AT2: IC50 = 0.33 nM (human); AT1: IC50 = 0.49 nM (human); Type-1B angiotensin II receptor: IC50 = 3 nM (rat); Plasmodium berghei: IC50 = 25 nM; PPARγ: EC5050 = 1.52 µM
Ki Data :
Type-1A angiotensin II receptor: Ki= 0.23 nM (rat)
pK Values :
pKa: 3.86 (Predicted), pKb: 5.01 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
RTECS :
DV2037500
PubChem CID :
65999
Merck Index :
14: 9129
MDL Number :
MFCD00918125
Beilstein Registry :
6624054
SMILES :
CCCC1=NC2=C(C=C(C=C2N1CC3=CC=C(C=C3)C4=CC=CC=C4C(=O)O)C5=NC6=CC=CC=C6N5C)C

Download SDS (MSDS)

Certificate of Analysis

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Telmisartan  Product Citations

See how others have used Telmisartan. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 27693991  Görgens, C. et al. 2016. Journal of pharmaceutical and biomedical analysis. 131: 482-496.

PMID: # 26420482  Zhang, H. et al. 2015. J. Biol. Chem. 290: 29127-39.

PMID: # 24301614  Kumai, Y. et al. 2014. The Journal of endocrinology. 220: 195-205.

PMID: # 20362079  Ma, L. et al. 2010. Bone. 47: 5-11.

Citations 1 to 4 of 4 total
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Rated 5 out of 5 by from McClellan et al McClellan et al. (PubMed ID 9878991) found that the angiotensin II receptor antagonist selectively inactivated AT1 receptor without affecting other circulatory system receptors involved. -SCBT Publication Review
Date published: 2015-04-03
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