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MedKoo Cat#: 318797 | Name: Telmisartan
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Telmisartan is an angiotensin II receptor antagonist (angiotensin receptor blocker, ARB) used in the management of hypertension.

Chemical Structure

Telmisartan
Telmisartan
CAS#144701-48-4

Theoretical Analysis

MedKoo Cat#: 318797

Name: Telmisartan

CAS#: 144701-48-4

Chemical Formula: C33H30N4O2

Exact Mass: 514.2369

Molecular Weight: 514.63

Elemental Analysis: C, 77.02; H, 5.88; N, 10.89; O, 6.22

Price and Availability

Size Price Availability Quantity
500mg USD 150.00 Ready to ship
1g USD 200.00 Ready to ship
2g USD 300.00 Ready to ship
5g USD 450.00 2 Weeks
10g USD 750.00 2 Weeks
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Related CAS #
144701-48-4 528560-93-2 (methyl ester)
Synonym
BIBR-277; BIBR277; BIBR 277; Telmisartan; Kinzalmono; Micardis
IUPAC/Chemical Name
4'-((1,7'-dimethyl-2'-propyl-1H,3'H-[2,5'-bibenzo[d]imidazol]-3'-yl)methyl)-[1,1'-biphenyl]-2-carboxylic acid
InChi Key
RMMXLENWKUUMAY-UHFFFAOYSA-N
InChi Code
InChI=1S/C33H30N4O2/c1-4-9-30-35-31-21(2)18-24(32-34-27-12-7-8-13-28(27)36(32)3)19-29(31)37(30)20-22-14-16-23(17-15-22)25-10-5-6-11-26(25)33(38)39/h5-8,10-19H,4,9,20H2,1-3H3,(H,38,39)
SMILES Code
O=C(C1=CC=CC=C1C2=CC=C(CN3C4=CC(C5=NC6=CC=CC=C6N5C)=CC(C)=C4N=C3CCC)C=C2)O
Appearance
White to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot#T8C03I21
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
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.
In vitro activity:
Unlike the recently reported data, in the current study, telmisartan increased AMPK activity first (at 6 hours of treatment) (Fig. 2B) with the mTOR/p70S6K inhibition following at 12 hours of treatment (Fig. 1C). Furthermore, the AMPK inhibition of the mTOR/p70S6K signaling axis was almost completely reversed in the dn-AMPKα1-transfected VSMCs (Fig. 2E). Therefore, it is reasonable to accept that AMPK-mediated inhibition of the mTOR/p70S6K signaling pathway is responsible for telmisartan-inhibited VSMC proliferation (Fig. 6). Reference: J Korean Med Sci. 2020 Sep 7; 35(35): e289. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7476795/
In vivo activity:
Telmisartan treatment also increased myocardium PPAR-γ expression in hypertensive LVH rats (Supplementary Figure 5), suggesting that the PPAR-γ agonist activity of telmisartan may play an important role in its improvement of myocardial remodeling in hypertensive LVH rats. The Ang II-induced collagen metabolism disorder (increased COL 1A1 and TIMP-1 expression and type 1 collagen secretion, and reduced MMP-1 expression) ameliorated by telmisartan in cardiac fibroblasts could be partly inhibited by pretreatment with the PPAR-γ inhibitor GW9662 (Figure 5(b) to (d)). These results suggest that telmisartan could improve collagen metabolism disorder by activating PPAR-γ as well as by inhibiting leptin autocrine activity induced by Ang II. Reference: Exp Biol Med (Maywood). 2020 Apr; 245(7): 654–666. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7153214/
Solvent mg/mL mM
Solubility
DMSO 7.7 15.04
DMF 1.6 3.11
DMF:PBS (pH 7.2) (1:1) 0.5 0.97
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 514.63 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Hwang YJ, Park JH, Cho DH. Activation of AMPK by Telmisartan Decreases Basal and PDGF-stimulated VSMC Proliferation via Inhibiting the mTOR/p70S6K Signaling Axis. J Korean Med Sci. 2020 Sep 7;35(35):e289. doi: 10.3346/jkms.2020.35.e289. PMID: 32893519; PMCID: PMC7476795. 2. Cortada M, Wei E, Jain N, Levano S, Bodmer D. Telmisartan Protects Auditory Hair Cells from Gentamicin-Induced Toxicity in vitro. Audiol Neurootol. 2020;25(6):297-308. doi: 10.1159/000506796. Epub 2020 May 5. PMID: 32369826. 3. Chen H, Li M, Liu L, Zhu D, Tian G. Telmisartan improves myocardial remodeling by inhibiting leptin autocrine activity and activating PPARγ. Exp Biol Med (Maywood). 2020 Apr;245(7):654-666. doi: 10.1177/1535370220908215. Epub 2020 Feb 19. PMID: 32075431; PMCID: PMC7153214. 4. Ma C, Pu Y, Xue H, Liu Y. Telmisartan suppresses cardiomyocyte and alveolar wall hypertrophy by the PPARγ-ERK-NFAT complex by changing the balance of PPARγ and ERK. Int J Clin Exp Pathol. 2019 Sep 1;12(9):3235-3246. PMID: 31934167; PMCID: PMC6949821.
In vitro protocol:
1. Hwang YJ, Park JH, Cho DH. Activation of AMPK by Telmisartan Decreases Basal and PDGF-stimulated VSMC Proliferation via Inhibiting the mTOR/p70S6K Signaling Axis. J Korean Med Sci. 2020 Sep 7;35(35):e289. doi: 10.3346/jkms.2020.35.e289. PMID: 32893519; PMCID: PMC7476795. 2. Cortada M, Wei E, Jain N, Levano S, Bodmer D. Telmisartan Protects Auditory Hair Cells from Gentamicin-Induced Toxicity in vitro. Audiol Neurootol. 2020;25(6):297-308. doi: 10.1159/000506796. Epub 2020 May 5. PMID: 32369826.
In vivo protocol:
1. Chen H, Li M, Liu L, Zhu D, Tian G. Telmisartan improves myocardial remodeling by inhibiting leptin autocrine activity and activating PPARγ. Exp Biol Med (Maywood). 2020 Apr;245(7):654-666. doi: 10.1177/1535370220908215. Epub 2020 Feb 19. PMID: 32075431; PMCID: PMC7153214. 2. Ma C, Pu Y, Xue H, Liu Y. Telmisartan suppresses cardiomyocyte and alveolar wall hypertrophy by the PPARγ-ERK-NFAT complex by changing the balance of PPARγ and ERK. Int J Clin Exp Pathol. 2019 Sep 1;12(9):3235-3246. PMID: 31934167; PMCID: PMC6949821.
1: Das AK, Tiwaskar M, Abdullakutty J, Pande A, Kumar V, Zalte N, Sugumaran A, Mohanasundaram S, Gogtay J. Effectiveness and Safety of the Telmisartan and Amlodipine Fixed-dose Combination in Managing Hypertension among Indian Patients (TACT India Study): Rationale and Study Design. J Assoc Physicians India. 2024 Nov;72(11):e16-e20. doi: 10.59556/japi.72.0743. PMID: 39563123. 2: Habboush S, Kagita NV, Gadelmawla AF, Elmoursi A, Merza N, Abdo AA, Zahran AHM, Eldeib M, Almarghany AA, Abdelfadil MM, Abdelkarim MA, Shawky I, Mohammed OM, Alharran A, Ali MM, Elbardisy S. Triple Therapy with Telmisartan, Amlodipine, and Rosuvastatin (TAR) Versus Telmisartan/Amlodipine (TA) and Telmisartan/Rosuvastatin (TR) Combinations in Hypertension and Dyslipidemia: A Systematic Review and Meta-analysis. High Blood Press Cardiovasc Prev. 2024 Nov 19. doi: 10.1007/s40292-024-00689-3. Epub ahead of print. PMID: 39557773. 3: Fawzy MG, Abd El-Hay SS, Mostafa AA, Metias YM. Specialized greenness sustainability tools for evaluation of the spectrophotometric methodologies greenness: Spectral signal manipulation for resolving the interfering telmisartan and metoprolol succinate spectra in their bulk and pharmaceutical formulation. Anal Biochem. 2024 Nov 8;697:115711. doi: 10.1016/j.ab.2024.115711. Epub ahead of print. PMID: 39521359. 4: Yang W, Wang F, Que Q, Fang C, Ao F, Xu Z, Chu W. Urban stormwater discharge contributes more micropollutants to surface water in humid regions of China: Comparison with treated wastewater. Water Res. 2024 Oct 29;268(Pt B):122712. doi: 10.1016/j.watres.2024.122712. Epub ahead of print. PMID: 39500004. 5: Hsu J, Fang HH, Su JJ. Telmisartan potentiates the ITE-induced aryl hydrocarbon receptor activity in human liver cell line. Arch Toxicol. 2024 Oct 31. doi: 10.1007/s00204-024-03901-4. Epub ahead of print. PMID: 39480548. 6: B S, Satish Kumar RC, B M, C K KS. A Comprehensive Narrative Review of Drug Interactions Between Traveler's Diarrhea Medications and Chronic Therapies: Implications for Clinical Practice. Cureus. 2024 Sep 25;16(9):e70213. doi: 10.7759/cureus.70213. PMID: 39463598; PMCID: PMC11512002. 7: Bonnet F, Doumbia A, Machault V, Ello FN, Bellecave P, Akpovo CB, Sidibe BT, Fernandez L, Kouamé A, Adjogoua E, Dosso M, Niangoran S, Journot V, Eholié SP. Atorvastatin and telmisartan do not reduce nasopharyngeal carriage of SARS-CoV-2 in mild or moderate COVID-19 in a phase IIb randomized controlled trial. Sci Rep. 2024 Oct 23;14(1):25028. doi: 10.1038/s41598-024-72449-1. PMID: 39443527; PMCID: PMC11500379. 8: Escobar C, Mazón P, Rivadulla C, Chandrappa S. The role of eprosartan in the management of essential hypertension: literature review and expert opinion. Expert Rev Cardiovasc Ther. 2024 Oct;22(10):575-587. doi: 10.1080/14779072.2024.2418298. Epub 2024 Oct 25. PMID: 39435482. 9: Akshayraj Vanrajbhai C, Thorat VM, Patel VS, Patil KP, Chawla LL. Evaluation of Anxiolytic Activity of Angiotensin Receptor Blockers Using Actophotometer Test in Wistar Rats. Cureus. 2024 Sep 20;16(9):e69798. doi: 10.7759/cureus.69798. PMID: 39429389; PMCID: PMC11491137. 10: Rodgers A, Salam A, Schutte AE, Cushman WC, de Silva HA, Di Tanna GL, Grobbee DE, Narkiewicz K, Ojji DB, Poulter NR, Schlaich MP, Oparil S, Spiering W, Williams B, Wright JT Jr, Lakshman P, Uluwattage W, Hay P, Pereira T, Amarasena N, Ranasinghe G, Gianacas C, Shanthakumar M, Liu X, Wang N, Gnanenthiran SR, Whelton PK; GMRx2 Investigators. Efficacy and safety of a novel low-dose triple single-pill combination of telmisartan, amlodipine and indapamide, compared with dual combinations for treatment of hypertension: a randomised, double-blind, active-controlled, international clinical trial. Lancet. 2024 Oct 19;404(10462):1536-1546. doi: 10.1016/S0140-6736(24)01744-6. PMID: 39426836. 11: Xu D, Cai F, Hu J, Zeng Z. Study on PINK1 Expression and Its Clinical Value in Diabetic Nephropathy. Iran J Kidney Dis. 2024 Oct 18;18(5). doi: 10.5254/0x69c976. PMID: 39423108. 12: Qian J, Zhang M, Chen Z. A Systematic Literature Review and Network Meta- analysis of Azilsartan Medoxomil Compared to Other Anti-hypertensives Efficacy in Lowering Blood Pressure Amongst Mild to Moderate Hypertensive Patients. Adv Ther. 2024 Dec;41(12):4498-4517. doi: 10.1007/s12325-024-02997-5. Epub 2024 Oct 16. PMID: 39412629; PMCID: PMC11550241. 13: Zhang Y, Ma J, Wei F, Gong J, Zhuang L, Zhang N, Cui Z. Polyenylphosphatidylcholine alleviates cardiorenal fibrosis, injury and dysfunction in spontaneously hypertensive rats by regulating Plpp3 signaling. Front Cardiovasc Med. 2024 Sep 30;11:1458173. doi: 10.3389/fcvm.2024.1458173. PMID: 39403590; PMCID: PMC11472324. 14: Machado CA, Oliveira BDS, de Barros JLVM, Fernandes HB, de Brito Toscano EC, Kangussu LM, Guimarães PPG, Simões E Silva AC, Teixeira AL, de Miranda AS. Involvement of Renin-Angiotensin system (RAS) components in mild traumatic brain injury. Brain Res. 2024 Oct 5;1846:149266. doi: 10.1016/j.brainres.2024.149266. Epub ahead of print. PMID: 39374839. 15: Elbardisy S, Alotaibi MN, Saad AR, Alhatm M, Alharbi OH, Alyaqout FB, Elshaer OE, Alazmi AM, Kagita NV, Allam IM, Bhutta AI, Habboush S, Sindi R, Aswad Y, Alharran AM. Single-Pill Combination Therapy of Amlodipine, Telmisartan, and Chlorthalidone in the Management of Hypertension: A Systematic Review of Randomized Controlled Trials. Cureus. 2024 Sep 6;16(9):e68802. doi: 10.7759/cureus.68802. PMID: 39371805; PMCID: PMC11456305. 16: Sattar OIA, Abuseada HHM, Ramzy S, Abuelwafa MM. Three spectrophotometric quantitative analysis of bisoprolol fumarate and telmisartan in fixed-dose combination utilizing ratio spectra manipulation methods. Sci Rep. 2024 Oct 2;14(1):22899. doi: 10.1038/s41598-024-72525-6. PMID: 39358387; PMCID: PMC11447042. 17: Almukainzi M, El-Masry TA, Ibrahim HA, Saad HM, El Zahaby EI, Saleh A, El- Nagar MMF. Ameliorative Effect of Chitosan/Spirulina platensis Ethanolic Extract Nanoformulation against Cyclophosphamide-Induced Ovarian Toxicity: Role of PPAR-γ/Nrf-2/HO-1 and NF-kB/TNF-α Signaling Pathways. Mar Drugs. 2024 Aug 30;22(9):395. doi: 10.3390/md22090395. PMID: 39330276; PMCID: PMC11433581. 18: Muambo KE, Kim MG, Kim DH, Park S, Oh JE. Pharmaceuticals in raw and treated water from drinking water treatment plants nationwide: Insights into their sources and exposure risk assessment. Water Res X. 2024 Sep 3;24:100256. doi: 10.1016/j.wroa.2024.100256. PMID: 39291270; PMCID: PMC11406100. 19: Williams K, MacDonald-Dickinson V, Matsuyama A. The incidence and trends of proteinuria, azotemia and hypertension in cats receiving toceranib phosphate. J Feline Med Surg. 2024 Sep;26(9):1098612X241266418. doi: 10.1177/1098612X241266418. PMID: 39287178; PMCID: PMC11418616. 20: Kuroki M, Suzuki H, Onodera Y, Nakane M, Kawamae K. Association Between Long- Versus Short-Acting Angiotensin II Receptor Antagonists and Hypotension During Anesthesia Induction: A Retrospective Study. Asian J Anesthesiol. 2024 Sep 16. doi: 10.6859/aja.202409/PP.0001. Epub ahead of print. PMID: 39278723.