MedKoo Biosciences, Inc.
Tel:   +1-919-636-5577    Fax:   +1-919-980-4831    Email:   sales@medkoo.com
Search
Login Register
Search
MedKoo Cat#: 573677 | Name: Arotinolol free base
Featured

Description:

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

Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. It also acts as a β3 receptor agonist. A 1979 publication suggests arotinolol as having first been described in the scientific literature by Sumitomo Chemical as "β-adrenergic blocking, antiarrhythmic compound S-596".

Chemical Structure

Arotinolol free base
CAS#68377-92-4 (free base)

Theoretical Analysis

MedKoo Cat#: 573677

Name: Arotinolol free base

CAS#: 68377-92-4 (free base)

Chemical Formula: C15H21N3O2S3

Exact Mass: 371.0796

Molecular Weight: 371.53

Elemental Analysis: C, 48.49; H, 5.70; N, 11.31; O, 8.61; S, 25.89

Price and Availability

Size Price Availability Quantity
5mg USD 315.00 2 Weeks
10mg USD 550.00 2 Weeks
Bulk Inquiry
Buy Now
Add to Cart
Related CAS #
68377-92-4 (free base) 68377-91-3 (HCl) 87055-50-3 (R-isomer HCl) 92075-58-6 (R-isomer) 101540-26-5 (S-isomer HCl)
Synonym
Almarl, Arotinolol
IUPAC/Chemical Name
5-(2-((3-(tert-Butylamino)-2-hydroxypropyl)thio)-4-thiazolyl)-2-thiophenecarboxamide
InChi Key
BHIAIPWSVYSKJS-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H21N3O2S3/c1-15(2,3)17-6-9(19)7-21-14-18-10(8-22-14)11-4-5-12(23-11)13(16)20/h4-5,8-9,17,19H,6-7H2,1-3H3,(H2,16,20)
SMILES Code
O=C(C1=CC=C(C2=CSC(SCC(O)CNC(C)(C)C)=N2)S1)N
Appearance
Solid powder
Purity
>97% (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
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 371.53 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
1: Huang P, Song Q, Wang Y, Wang A, Guo L, Zhang H, Zhang Z, Ma X. Effect of arotinolol on chronic heart failure: A systematic review and meta-analysis of randomized controlled trials. Front Cardiovasc Med. 2022 Dec 14;9:1071387. doi: 10.3389/fcvm.2022.1071387. PMID: 36588575; PMCID: PMC9795060. 2: Qian Z, Xu Y, Zheng L, Zhang J, Hong Z, Shen X. Enantiospecific determination of arotinolol in rat plasma by LC-MS/MS: application to a stereoselective pharmacokinetic study. J Pharm Biomed Anal. 2015 Jan;102:299-304. doi: 10.1016/j.jpba.2014.09.034. Epub 2014 Oct 2. PMID: 25459927. 3: Zhou W, Hong M, Zhang K, Chen D, Han W, Shen W, Zhu D, Gao P. Mechanisms of improved aortic stiffness by arotinolol in spontaneously hypertensive rats. PLoS One. 2014 Feb 12;9(2):e88722. doi: 10.1371/journal.pone.0088722. PMID: 24533142; PMCID: PMC3923047. 4: Zhao J, Golozoubova V, Cannon B, Nedergaard J. Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes. Can J Physiol Pharmacol. 2001 Jul;79(7):585-93. PMID: 11478592. 5: Morimoto S, Miyawaki N, Sasaki Y, Matsumura Y. Effects of arotinolol, an alpha- and beta-adrenoceptor antagonist, on renin release from rat kidney cortical slices. Clin Exp Pharmacol Physiol. 1986 Jun;13(6):505-10. doi: 10.1111/j.1440-1681.1986.tb00931.x. PMID: 2428551. 6: Fang H, Chen W, Liu X, Xu W. The efficacy and safety of arotinolol combined with a different calcium channel blocker in the treatment of Chinese patients with essential hypertension: a one-year follow-up study. Clin Exp Hypertens. 2014;36(8):590-5. doi: 10.3109/10641963.2014.897714. Epub 2014 Mar 28. PMID: 24678807. 7: Lee DB, Woo YS, Bahk WM. Use of Arotinolol Pharmacotherapy to Treat Drug- induced Tremor: A Report of Three Cases. Pharmacopsychiatry. 2015 Jul;48(4-5):176-8. doi: 10.1055/s-0035-1549931. Epub 2015 May 13. PMID: 25970026. 8: Mori T, Handa K, Terao Y, Tanaka H, Kiyonaga A, Shindo M, Matsunaga A, Sasaki J, Arakawa K. Effects of arotinolol on exercise capacity and humoral factors during exercise in normal subjects. Cardiovasc Drugs Ther. 1992 Aug;6(4):387-90. doi: 10.1007/BF00054186. PMID: 1381611. 9: Miyagishi A, Nakahara H, Hara Y. Adrenoceptor blocking effects of arotinolol, a new combined alpha- and beta-adrenoceptor blocking agent. Arch Int Pharmacodyn Ther. 1984 Oct;271(2):249-62. PMID: 6210068. 10: Suzuki-Kusaba M, Hisa H, Kimura T, Satoh S. Effects of arotinolol on hemodynamics and adrenergically induced renin release and renal vasoconstriction. Arzneimittelforschung. 1988 May;38(5):671-7. PMID: 2458109. 11: Kuno S, Mizuta E, Nishida J, Takechi M. Therapeutic effects of arotinolol, a beta-adrenergic blocker, on tremor in MPTP-induced parkinsonian monkeys. Clin Neuropharmacol. 1992 Oct;15(5):381-6. doi: 10.1097/00002826-199210000-00005. PMID: 1384970. 12: Nakagawa Y, Nakahara H, Chin WP, Imai S. Alpha-blockade and vasodilatation induced by nipradilol, arotinolol and labetalol in pithed rats. Jpn J Pharmacol. 1985 Dec;39(4):481-5. doi: 10.1254/jjp.39.481. PMID: 2419612. 13: Lee KS, Kim JS, Kim JW, Lee WY, Jeon BS, Kim D. A multicenter randomized crossover multiple-dose comparison study of arotinolol and propranolol in essential tremor. Parkinsonism Relat Disord. 2003 Aug;9(6):341-7. doi: 10.1016/s1353-8020(03)00029-4. PMID: 12853233. 14: Nakashima M, Uematsu T, Takiguchi Y, Hashimoto H, Watanabe I, Morioka S, Hibino T. Effect of ophthalmic administration of S-596 (Arotinolol) on intraocular pressure and haemodynamics in health volunteers: comparison with timolol. Eur J Clin Pharmacol. 1985;28(4):391-6. doi: 10.1007/BF00544356. PMID: 2411566. 15: Hashimoto H, Asano M, Hayashi T, Oguro K, Takiguchi Y, Nakashima M. Hemodynamic effects of arotinolol in anesthetized dogs and its affinities for adrenoceptors in vitro. Arch Int Pharmacodyn Ther. 1984 Jan;267(1):23-34. PMID: 6202253. 16: Kuroda Y, Kakigi R, Shibasaki H. Treatment of essential tremor with arotinolol. Neurology. 1988 Apr;38(4):650-2. doi: 10.1212/wnl.38.4.650. PMID: 2451192. 17: Qian Z, Le J, Chen X, Li S, Song H, Hong Z. High-throughput LC-MS/MS method with 96-well plate precipitation for the determination of arotinolol and amlodipine in a small volume of rat plasma: Application to a pharmacokinetic interaction study. J Sep Sci. 2018 Feb;41(3):618-629. doi: 10.1002/jssc.201700784. Epub 2017 Dec 11. PMID: 29115741. 18: Noguchi K, Kato T, Kinjo N, Moromizato H, Sakanashi M. Comparative effects of arotinolol, labetalol and propranolol on regional myocardial dysfunction induced by flow-limiting coronary stenosis in anesthetized dogs. Jpn J Pharmacol. 1990 Jul;53(3):381-91. doi: 10.1254/jjp.53.381. PMID: 1697348. 19: Miyauchi E, Matsumoto M, Kimura Y, Hattori H, Tsukio Y, Tsuchiya H, Takasaki M, Munehira J, Yamada K, Iwai K, Kawanishi K, Hoshino T, Murai H. [Clinical effect of arotinolol hydrochloride and its influence on renal function in elderly patients with essential hypertension]. Nihon Ronen Igakkai Zasshi. 1999 Aug;36(8):542-6. Japanese. doi: 10.3143/geriatrics.36.542. PMID: 10554561. 20: Watanabe H, Kakihana M, Ohtsuka S, Sugishita Y. Preventive effects of carvedilol on nitrate tolerance--a randomized, double-blind, placebo-controlled comparative study between carvedilol and arotinolol. J Am Coll Cardiol. 1998 Nov;32(5):1201-6. doi: 10.1016/s0735-1097(98)00398-2. PMID: 9809926.