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> Telmisartan-d3 [1189889-44-8]

Telmisartan-d3 [1189889-44-8]

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Référence HY-13955S-10mg

Conditionnement : 10mg

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Telmisartan-d3 is the deuterium labeled Telmisartan. 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[1][2].

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Telmisartan-d<sub>3</sub> Chemical Structure

Telmisartan-d3 Chemical Structure

CAS No. : 1189889-44-8

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Based on 1 publication(s) in Google Scholar

Other Forms of Telmisartan-d3:

  • Telmisartan In-stock
  • Telmisartan-d7 In-stock
  • Telmisartan-d4 Obtenir un devis
  • Telmisartan-13C,d3 Obtenir un devis

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Description

Telmisartan-d3 is the deuterium labeled Telmisartan. 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[1][2].

In Vitro

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Telmisartan-d3 Related Antibodies
Masse moléculaire

517.64

Formule

C33H27D3N4O2
CAS No.

1189889-44-8
Unlabeled Cas

144701-48-4
Appearance

Solid

Color

White to off-white

SMILES

CC1=CC(C2=NC3=C(N2C([2H])([2H])[2H])C=CC=C3)=CC4=C1N=C(N4CC5=CC=C(C=C5)C6=CC=CC=C6C(O)=O)CCC
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMF : ≥ 1.6 mg/mL (3.09 mM)

DMSO : ≥ 1 mg/mL (1.93 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

DMF:PBS (pH 7.2) (1:1) : ≥ 0.5 mg/mL (0.97 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9318 mL 9.6592 mL 19.3184 mL
5 mM --- --- ---
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Volume (start)

V1

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Concentration (final)

C2

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V2

In Vivo Dissolution Calculator
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Calculation results:
Working solution concentration: mg/mL
Pureté et documentation
Références

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

    [2]. Maillard MP, et al. In vitro and in vivo characterization of the activity of telmisartan: an insurmountable angiotensin II receptor antagonist. J Pharmacol Exp Ther. 2002 Sep;302(3):1089-95.  [Content Brief]

    [3]. Xuan H, et al. Inhibition or deletion of angiotensin II type 1 receptor suppresses elastase-induced experimental abdominal aortic aneurysms. J Vasc Surg. 2017 Apr 20. pii: S0741-5214(17)30100-3.  [Content Brief]

    [4]. Torika N, et al. Intranasal telmisartan ameliorates brain pathology in five familial Alzheimer's disease mice. Brain Behav Immun. 2017 Apr 3.  [Content Brief]

    [5]. Aswar U, et al. Telmisartan attenuates diabetes induced depression in rats. Pharmacol Rep. 2017 Apr;69(2):358-364.  [Content Brief]

    [6]. Fujihara S, et al. The angiotensin II type 1 receptor antagonist telmisartan inhibits cell proliferation and tumor growth of esophageal adenocarcinoma via the AMPKα/mTOR pathway in vitro and in vivo. Oncotarget. 2017 Jan 31;8(5):8536-8549.  [Content Brief]

  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

    [2]. Maillard MP, et al. In vitro and in vivo characterization of the activity of telmisartan: an insurmountable angiotensin II receptor antagonist. J Pharmacol Exp Ther. 2002 Sep;302(3):1089-95.

    [3]. Xuan H, et al. Inhibition or deletion of angiotensin II type 1 receptor suppresses elastase-induced experimental abdominal aortic aneurysms. J Vasc Surg. 2017 Apr 20. pii: S0741-5214(17)30100-3.

    [4]. Torika N, et al. Intranasal telmisartan ameliorates brain pathology in five familial Alzheimer's disease mice. Brain Behav Immun. 2017 Apr 3.

    [5]. Aswar U, et al. Telmisartan attenuates diabetes induced depression in rats. Pharmacol Rep. 2017 Apr;69(2):358-364.

    [6]. Fujihara S, et al. The angiotensin II type 1 receptor antagonist telmisartan inhibits cell proliferation and tumor growth of esophageal adenocarcinoma via the AMPKα/mTOR pathway in vitro and in vivo. Oncotarget. 2017 Jan 31;8(5):8536-8549.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / DMF 1 mM 1.9318 mL 9.6592 mL 19.3184 mL 48.2961 mL
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Telmisartan-d3 Related Classifications

  • GPCR/G Protein Autophagy
  • Angiotensin Receptor Autophagy
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Telmisartan-d31189889-44-8Angiotensin ReceptorAutophagyInhibitorinhibitorinhibit