MedKoo Cat#: 461125 | Name: Talinolol
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Description:

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

Talinolol is a beta(1)-adrenergic receptor antagonist and a probe drug for P-glycoprotein (P-gp) activity in humans.

Chemical Structure

Talinolol
Talinolol
CAS#57460-41-0

Theoretical Analysis

MedKoo Cat#: 461125

Name: Talinolol

CAS#: 57460-41-0

Chemical Formula: C20H33N3O3

Exact Mass: 363.2522

Molecular Weight: 363.50

Elemental Analysis: C, 66.08; H, 9.15; N, 11.56; O, 13.20

Price and Availability

Size Price Availability Quantity
5mg USD 330.00
10mg USD 570.00
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Related CAS #
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Synonym
Talinolol; Cordanum;
IUPAC/Chemical Name
1-(4-(3-(tert-butylamino)-2-hydroxypropoxy)phenyl)-3-cyclohexylurea
InChi Key
MXFWWQICDIZSOA-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H33N3O3/c1-20(2,3)21-13-17(24)14-26-18-11-9-16(10-12-18)23-19(25)22-15-7-5-4-6-8-15/h9-12,15,17,21,24H,4-8,13-14H2,1-3H3,(H2,22,23,25)
SMILES Code
CC(C)(NCC(COc1ccc(NC(NC2CCCCC2)=O)cc1)O)C
Appearance
Solid powder
Purity
>95% (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
Shelf Life
>3 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
2934.99.03.00
More Info
Certificate of Analysis
Safety Data Sheet (SDS)

Preparing Stock Solutions

The following data is based on the product molecular weight 363.50 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
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Gene. 2024 Jun 5;910:148321. doi: 10.1016/j.gene.2024.148321. Epub 2024 Feb 28. PMID: 38428621. 4: Chu J, Panfen E, Wang L, Marino A, Chen XQ, Fancher RM, Landage R, Patil O, Desai SD, Shah D, Xue Y, Sinz M, Shen H. Evaluation of Encequidar as An Intestinal P-gp and BCRP Specific Inhibitor to Assess the Role of Intestinal P-gp and BCRP in Drug-Drug Interactions. Pharm Res. 2023 Nov;40(11):2567-2584. doi: 10.1007/s11095-023-03563-4. Epub 2023 Jul 31. PMID: 37523014. 5: Azimi M, Yee SW, Riselli A, Silva DB, Giacomini CP, Giacomini KM, Brett CM. Characterization of P-glycoprotein orthologs from human, sheep, pig, dog, and cat. J Vet Pharmacol Ther. 2023 Nov;46(6):401-412. doi: 10.1111/jvp.13386. Epub 2023 May 17. PMID: 37198956. 6: Saito A, Kito T, Ishiguro N, Takatani M, Kudo T, Bister B, Kusuhara H. Impact of Direction of Transport on the Evaluation of Substrate Recognition of Mouse Multidrug and Toxin Extrusion Protein 1. Drug Metab Dispos. 2023 May;51(5):583-590. doi: 10.1124/dmd.122.001115. Epub 2023 Jan 20. PMID: 36669855. 7: Weiss M, D'Argenio DZ, Siegmund W. Analysis of Complex Absorption After Multiple Dosing: Application to the Interaction Between the P-glycoprotein Substrate Talinolol and Rifampicin. Pharm Res. 2022 Dec;39(12):3293-3300. doi: 10.1007/s11095-022-03397-6. Epub 2022 Sep 26. PMID: 36163409; PMCID: PMC9780127. 8: Streekstra EJ, Kiss M, van den Heuvel J, Nicolaï J, van den Broek P, Botden SMBI, Stommel MWJ, van Rijssel L, Ungell AL, van de Steeg E, Russel FGM, de Wildt SN. A proof of concept using the Ussing chamber methodology to study pediatric intestinal drug transport and age-dependent differences in absorption. Clin Transl Sci. 2022 Oct;15(10):2392-2402. doi: 10.1111/cts.13368. Epub 2022 Aug 12. PMID: 35962572; PMCID: PMC9579398. 9: Asaumi R, Nunoya KI, Yamaura Y, Taskar KS, Sugiyama Y. Robust physiologically based pharmacokinetic model of rifampicin for predicting drug-drug interactions via P-glycoprotein induction and inhibition in the intestine, liver, and kidney. CPT Pharmacometrics Syst Pharmacol. 2022 Jul;11(7):919-933. doi: 10.1002/psp4.12807. Epub 2022 Jun 6. PMID: 35570332; PMCID: PMC9286720. 10: Miyake T, Tsutsui H, Haraya K, Tachibana T, Morimoto K, Takehara S, Ayabe M, Kobayashi K, Kazuki Y. Quantitative prediction of P-glycoprotein-mediated drug- drug interactions and intestinal absorption using humanized mice. Br J Pharmacol. 2021 Nov;178(21):4335-4351. doi: 10.1111/bph.15612. Epub 2021 Sep 6. PMID: 34232502. 11: Bouchard J, Shepherd G, Hoffman RS, Gosselin S, Roberts DM, Li Y, Nolin TD, Lavergne V, Ghannoum M; EXTRIP workgroup. Extracorporeal treatment for poisoning to beta-adrenergic antagonists: systematic review and recommendations from the EXTRIP workgroup. Crit Care. 2021 Jun 10;25(1):201. doi: 10.1186/s13054-021-03585-7. PMID: 34112223; PMCID: PMC8194226. 12: Igarashi F, Nakagawa T, Shinohara Y, Tachibana T. Analysis of Non-linear Pharmacokinetics of P-Glycoprotein Substrates in a Microfluidic Device Using a Mathematical Model that Includes an Unstirred Water Layer (UWL) Compartment. Pharm Res. 2021 Jun;38(6):1031-1039. doi: 10.1007/s11095-021-03054-4. Epub 2021 May 19. PMID: 34009624. 13: Pala Kara Z, Ozturk Civelek D, Ozturk N, Okyar A. The effects of P-glycoprotein inhibitor zosuquidar on the sex and time-dependent pharmacokinetics of parenterally administered talinolol in mice. Eur J Pharm Sci. 2021 Jan 1;156:105589. doi: 10.1016/j.ejps.2020.105589. Epub 2020 Oct 10. PMID: 33049306. 14: Kawasaki T, Shiozaki Y, Nomura N, Kawai K, Uwai Y, Nabekura T. Investigation of Fluorescent Substrates and Substrate-Dependent Interactions of a Drug Transporter Organic Anion Transporting Polypeptide 2B1 (OATP2B1). Pharm Res. 2020 Jun 1;37(6):115. doi: 10.1007/s11095-020-02831-x. PMID: 32483763. 15: Kara ZP, Ozturk D, Ozturk N, Orman MN, Baktir G, Okyar A. Effects of atorvastatin on talinolol absorption: A potential drug-drug interaction. Pharmazie. 2020 Mar 20;75(2):70-74. doi: 10.1691/ph.2020.9904. PMID: 32213237. 16: Yamazaki S, Costales C, Lazzaro S, Eatemadpour S, Kimoto E, Varma MV. Physiologically-Based Pharmacokinetic Modeling Approach to Predict Rifampin- Mediated Intestinal P-Glycoprotein Induction. CPT Pharmacometrics Syst Pharmacol. 2019 Sep;8(9):634-642. doi: 10.1002/psp4.12458. Epub 2019 Sep 5. PMID: 31420942; PMCID: PMC6765699. 17: Brueck S, Bruckmueller H, Wegner D, Busch D, Martin P, Oswald S, Cascorbi I, Siegmund W. Transcriptional and Post-Transcriptional Regulation of Duodenal P-Glycoprotein and MRP2 in Healthy Human Subjects after Chronic Treatment with Rifampin and Carbamazepine. Mol Pharm. 2019 Sep 3;16(9):3823-3830. doi: 10.1021/acs.molpharmaceut.9b00458. Epub 2019 Aug 9. PMID: 31361500. 18: Okyar A, Kumar SA, Filipski E, Piccolo E, Ozturk N, Xandri-Monje H, Pala Z, Abraham K, Gomes ARGJ, Orman MN, Li XM, Dallmann R, Lévi F, Ballesta A. Sex-, feeding-, and circadian time-dependency of P-glycoprotein expression and activity - implications for mechanistic pharmacokinetics modeling. Sci Rep. 2019 Jul 19;9(1):10505. doi: 10.1038/s41598-019-46977-0. PMID: 31324853; PMCID: PMC6642159. 19: Hiesinger K, Kramer JS, Achenbach J, Moser D, Weber J, Wittmann SK, Morisseau C, Angioni C, Geisslinger G, Kahnt AS, Kaiser A, Proschak A, Steinhilber D, Pogoryelov D, Wagner K, Hammock BD, Proschak E. Computer-Aided Selective Optimization of Side Activities of Talinolol. ACS Med Chem Lett. 2019 May 29;10(6):899-903. doi: 10.1021/acsmedchemlett.9b00075. PMID: 31223445; PMCID: PMC6580380. 20: Kazi M, Al-Swairi M, Ahmad A, Raish M, Alanazi FK, Badran MM, Khan AA, Alanazi AM, Hussain MD. 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