A β1-adrenergic receptor blocker
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(±)-Talinolol

Item No. 16116

Technical Information
Formal Name
N-cyclohexyl-N'-[4-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]phenyl]-urea
CAS Number
57460-41-0
Molecular Formula
C20H33N3O3
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:20): 0.05 mg/mlDMSO: 15 mg/mlEthanol: 10 mg/ml
λmax
203, 245, 292 nm
SMILES
O=C(NC1CCCCC1)NC2=CC=C(OCC(O)CNC(C)(C)C)C=C2
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)
InChi Key
MXFWWQICDIZSOA-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    (±)-Talinolol is a β1-selective adrenoceptor antagonist well known for its cardioprotective and antihypertensive activity.1 By blocking β1-adrenergic receptors, talinolol delays the conduction of stimuli in the AV node, reduces the sino-atrial conduction time, and impedes the sinus node automaticity.1 Because its metabolism in human liver microsomes is well understood, (±)-talinolol is useful for examining the activity of the drug-transporting MDR1 gene product P-glycoprotein.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Abmann, I. The actions of talinolol, a β1-selectiveβblocker, in cardiac arrhythmia and acute myocardial infarction. Curr. Med. Res. Opin. 13(6), 325-342 (1995).

    2. Trausch, B., Oertel, R., Richter, K., et alDisposition and bioavailability of the β1-adrenoceptor antagonist talinolol in man. Biopharm. Drug Dispos. 16(5), 403-414 (1995).

    3. Zschiesche, M., Lemma, G.L., Klebingat, K.J., et alStereoselective disposition of talinolol in man. J. Pharm. Sci. 91(2), 303-311 (2002).

    4. Schwarz, U.I., Seemann, D., Oertel, R., et alGrapefruit juice ingestion significantly reduces talinolol bioavailability. Clin. Pharmacol. Ther. 77(4), 291-301 (2005).