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MedKoo Cat#: 329627 | Name: Tilisolol HCl

Description:

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

Tilisolol, also known as N-696, is a nonselective beta-adrenergic blocker. Tilisolol hydrochloride dilates coronary arteries through an ATP-sensitive K(+)-channel opening mechanism in dogs. In contrast to propranolol, N-696 lowered blood pressure and heart rate without peripheral vasoconstriction and did not augment forearm vasoconstrictive responses to norepinephrine.

Chemical Structure

Tilisolol HCl
CAS#62774-96-3 (HCl)

Theoretical Analysis

MedKoo Cat#: 329627

Name: Tilisolol HCl

CAS#: 62774-96-3 (HCl)

Chemical Formula: C17H25ClN2O3

Exact Mass: 304.1787

Molecular Weight: 340.85

Elemental Analysis: C, 59.91; H, 7.39; Cl, 10.40; N, 8.22; O, 14.08

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
62774-96-3 (HCl) 85136-71-6 (free base)
Synonym
N-696; N696; N 696; Tilisolol, trade name Selecal.
IUPAC/Chemical Name
1(2H)-Isoquinolinone, 4-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)-2-methyl-, hydrochloride
InChi Key
SGPGESCZOCHFCL-UHFFFAOYSA-N
InChi Code
InChI=1S/C17H24N2O3.ClH/c1-17(2,3)18-9-12(20)11-22-15-10-19(4)16(21)14-8-6-5-7-13(14)15;/h5-8,10,12,18,20H,9,11H2,1-4H3;1H
SMILES Code
O=C1N(C)C=C(OCC(O)CNC(C)(C)C)C2=C1C=CC=C2.[H]Cl
Appearance
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
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

Preparing Stock Solutions

The following data is based on the product molecular weight 340.85 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: Kawakami S, Ohshima N, Hirayama R, Al MH, Kitahara T, Sakaeda T, Mukai T, Nishida K, Nakamura J, Nakashima M, Sasaki H. Biodistribution and pharmacokinetics of O-palmitoyl tilisolol, a lipophilic prodrug of tilisolol, after intravenous administration in rats. Biol Pharm Bull. 2002 Aug;25(8):1072-6. PubMed PMID: 12186412. 2: Sakanaka K, Kawazu K, Nishida K, Nakamura J, Nakashima M, Nakamura T, Oshita A, Ichikawa N, Sasaki H. Transport of timolol and tilisolol in rabbit corneal epithelium. Biol Pharm Bull. 2006 Oct;29(10):2143-7. PubMed PMID: 17015968. 3: Sasaki H, Ichikawa M, Kawakami S, Yamamura K, Nishida K, Nakamura J. In situ ocular absorption of tilisolol through ocular membranes in albino rabbits. J Pharm Sci. 1996 Sep;85(9):940-3. PubMed PMID: 8877883. 4: Hayase N, Chiba K, Abiko Y, Ichihara K. Effects of tilisolol on ischemic myocardial metabolism in dogs. Eur J Pharmacol. 1994 Aug 1;260(2-3):183-90. PubMed PMID: 7988643. 5: Sakai F, Kawano S, Hiraoka M. Electrophysiologic Effects of Beta-blocking Agent, Tilisolol, on Isolated Guinea Pig Ventricular Myocytes. J Cardiovasc Pharmacol Ther. 1996 Jan;1(1):41-48. PubMed PMID: 10684398. 6: Sugai T, Kojima K, Iwakami N, Suzuki Y. Vasorelaxant and hypotensive effects of tilisolol hydrochloride (N-696) in isolated rat thoracic aorta and pithed rats. Jpn J Pharmacol. 1991 Nov;57(3):367-75. PubMed PMID: 1687596. 7: Sasaki H, Yamamura K, Mukai T, Nishida K, Nakamura J, Nakashima M, Ichikawa M. Characterization of ocular pharmacokinetics of tilisolol after instillation into anesthetized rabbits. Biol Pharm Bull. 1999 Nov;22(11):1253-5. PubMed PMID: 10598041. 8: Takagi S, Kihara Y, Mitsuiye T, Wang Z, Sasayama S. Effects of tilisolol, a nonselective beta-adrenergic blocker, on the membrane currents of isolated guinea pig ventricular myocytes. J Cardiovasc Pharmacol. 1997 May;29(5):593-8. PubMed PMID: 9213200. 9: Miyauchi H, Horiki S, Horio T. Clinical and experimental photosensitivity reaction to tilisolol hydrochloride. Photodermatol Photoimmunol Photomed. 1994 Dec;10(6):255-8. PubMed PMID: 7727282. 10: Kawakami S, Nishida K, Mukai T, Yamamura K, Nakamura J, Sakaeda T, Nakashima M, Sasaki H. Controlled release and ocular absorption of tilisolol utilizing ophthalmic insert-incorporated lipophilic prodrugs. J Control Release. 2001 Oct 19;76(3):255-63. PubMed PMID: 11578740. 11: Kawakami S, Nishida K, Mukai T, Yamamura K, Kobayashi K, Sakaeda T, Nakamura J, Nakashima M, Sasaki H. Ocular absorption behavior of palmitoyl tilisolol, an amphiphilic prodrug of tilisolol, for ocular drug delivery. J Pharm Sci. 2001 Dec;90(12):2113-20. PubMed PMID: 11745770. 12: Imaizumi T, Takeshita A, Nakamura N, Hirooka Y, Suzuki S, Yoshida M, Nakamura M. Vasodilating effect of the new beta-blocker tilisolol hydrochloride in humans. Arzneimittelforschung. 1988 Sep;38(9):1342-4. PubMed PMID: 2906248. 13: Yamamura K, Sasaki H, Nakashima M, Ichikawa M, Mukai T, Nishida K, Nakamura J. Characterization of ocular pharmacokinetics of beta-blockers using a diffusion model after instillation. Pharm Res. 1999 Oct;16(10):1596-601. PubMed PMID: 10554103. 14: Sasaki H, Nagano T, Sakanaka K, Kawakami S, Nishida K, Nakamura J, Ichikawa N, Iwashita J, Nakamura T, Nakashima M. One-side-coated insert as a unique ophthalmic drug delivery system. J Control Release. 2003 Oct 30;92(3):241-7. PubMed PMID: 14568405. 15: Sasaki H, Kashiwagi S, Mukai T, Nishida K, Nakamura J, Nakashima M, Ichikawa M. Topical delivery system of ophthalmic drugs by periocular injection with viscous solution. Biol Pharm Bull. 1999 Sep;22(9):961-5. PubMed PMID: 10513621. 16: Sasaki H, Nagano T, Yamamura K, Nishida K, Nakamura J. Ophthalmic preservatives as absorption promoters for ocular drug delivery. J Pharm Pharmacol. 1995 Sep;47(9):703-7. PubMed PMID: 8583378. 17: Kawakami S, Yamamura K, Mukai T, Nishida K, Nakamura J, Sakaeda T, Nakashima M, Sasaki H. Sustained ocular delivery of tilisolol to rabbits after topical administration or intravitreal injection of lipophilic prodrug incorporated in liposomes. J Pharm Pharmacol. 2001 Aug;53(8):1157-61. PubMed PMID: 11518027. 18: Sasaki H, Yamamura K, Mukai T, Nishida K, Nakamura J, Nakashima M, Ichikawa M. Pharmacokinetic prediction of the ocular absorption of an instilled drug with ophthalmic viscous vehicle. Biol Pharm Bull. 2000 Nov;23(11):1352-6. PubMed PMID: 11085365. 19: Liu Q, Nakae I, Takahashi M, Takaoka A, Kinoshita M. Tilisolol hydrochloride dilates coronary arteries through an ATP-sensitive K(+)-channel opening mechanism in dogs. Cardiovasc Drugs Ther. 1996 Mar;10(1):23-30. PubMed PMID: 8723167. 20: Sasaki H, Kashiwagi S, Mukai T, Nishida K, Nakamura J, Nakashima M, Ichikawa M. Drug absorption behavior after periocular injections. Biol Pharm Bull. 1999 Sep;22(9):956-60. PubMed PMID: 10513620.

View History

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