WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H526898
CAS#: 105394-80-7 ( fumarate)
Description: KT-362 is a calcium channel antagonist, potassium channel antagonist and sodium channel antagonist. KT-362 is a new antiarrhythmic agent with vasodilating action on intracellular calcium mobilization of atrial muscle.
Hodoodo Cat#: H526898
Name: KT-362 fumarate
CAS#: 105394-80-7 ( fumarate)
Chemical Formula: C26H32N2O7S
Exact Mass: 0.00
Molecular Weight: 516.609
Elemental Analysis: C, 60.45; H, 6.24; N, 5.42; O, 21.68; S, 6.21
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Synonym: KT-362; KT 362; KT362; KT-362 fumarate.
IUPAC/Chemical Name: 1-(3,4-dihydrobenzo[b][1,4]thiazepin-5(2H)-yl)-3-((3,4-dimethoxyphenethyl)amino)propan-1-one fumarate
InChi Key: YIVXAQUBENUHJC-WLHGVMLRSA-N
InChi Code: InChI=1S/C22H28N2O3S.C4H4O4/c1-26-19-9-8-17(16-20(19)27-2)10-12-23-13-11-22(25)24-14-5-15-28-21-7-4-3-6-18(21)24;5-3(6)1-2-4(7)8/h3-4,6-9,16,23H,5,10-15H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+
SMILES Code: O=C(N1CCCSC2=CC=CC=C12)CCNCCC3=CC=C(OC)C(OC)=C3.O=C(O)/C=C/C(O)=O
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: Related CAS# CAS#105394-80-7 (KT-362 fumarate) CAS# 93392-97-3 (KT-362 Free)
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 516.61 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.
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 |
Formulation protocol: | |
In vitro protocol: | |
In vivo protocol: |
1: Ueyama N, Wakabayashi S, Tomiyama T. Change of mechanical activity to contraction from the relaxation induced by the intracellular Ca2+ antagonist KT-362; effects of alkylation of side chain, and substitution of 2,3,4,5-tetrahydro-1,5-benzothiazepine derivatives. Chem Pharm Bull (Tokyo). 1997 Nov;45(11):1761-6. PubMed PMID: 9396151.
2: Tatsukawa Y, Arita M. Effects of KT-362, a sarcolemmal and intracellular calcium antagonist, on calcium transients of cultured neonatal rat ventricular cells: a comparison with gallopamil and ryanodine. Cardiovasc Drugs Ther. 1997 Jan;10(6):667-75. PubMed PMID: 9110109.
3: Erker T. [Studies on the chemistry of thieno-annealed O,N- and S,N-containing heterocyclics. 9. Synthesis and calcium channel blocking action of theino-analogs of KT-362]. Arch Pharm (Weinheim). 1995 Apr;328(4):313-6. German. PubMed PMID: 7611826.
4: Cheng YN, Kiyosue T, Arita M. Effects of KT-362, a new antiarrhythmic agent, on membrane ionic currents of guinea pig ventricular myocytes. J Pharmacol Exp Ther. 1994 Sep;270(3):851-7. PubMed PMID: 7932196.
5: Buljubasic N, Marijic J, Stowe DF, Gross GJ, Kampine JP, Bosnjak ZJ. Comparative cardiac effects of KT-362 and verapamil in isolated heart--correlation to calcium channel current depression. J Cardiovasc Pharmacol. 1991 Oct;18(4):594-604. PubMed PMID: 1724538.
6: Kodama I, Shibata S. Effects of KT-362, a new antiarrhythmic agent with vasodilating action on intracellular calcium mobilization of atrial muscle. J Pharmacol Exp Ther. 1991 Jul 1;258(1):332-8. PubMed PMID: 2072305.
7: Sakata K, Karaki H. Effects of a novel smooth muscle relaxant, KT-362, on contraction and cytosolic Ca2+ level in the rat aorta. Br J Pharmacol. 1991 Jan;102(1):174-8. PubMed PMID: 1710524; PubMed Central PMCID: PMC1917876.
8: Hester RK, Shibata S. KT-362 related effects on intracellular calcium release and associated clinical potential: arrhythmias, myocardial ischemia, and hypertension. Cardiovasc Drugs Ther. 1990 Oct;4(5):1345-54. Review. PubMed PMID: 2278870.
9: Wakabayashi S, Mochizuki S, Tomiyama A, Shibata S. Effects of KT-362, a new calcium release blocker, on vascular selectivity and hemodynamic actions in anesthetized dogs. Jpn J Pharmacol. 1990 Sep;54(1):23-32. PubMed PMID: 2273645.
10: Pieper GM, Gross GJ. Augmented vascular relaxation to KT-362 in diabetic rat aorta: comparison to diltiazem. J Cardiovasc Pharmacol. 1990 Sep;16(3):394-400. PubMed PMID: 1700209.
11: Hashimoto K, Watanabe K, Mochizuki S, Tomiyama A. Effects of KT-362, a new Na and Ca influx and Ca release inhibitor, on canine ventricular arrhythmias. Jpn J Pharmacol. 1989 Dec;51(4):475-82. PubMed PMID: 2559225.
12: Farber NE, Gross GJ. Collateral blood flow following acute coronary artery occlusion: comparison of a new intracellular calcium antagonist (KT-362) and diltiazem. J Cardiovasc Pharmacol. 1989 Jul;14(1):66-72. PubMed PMID: 2475718.
13: Pelc LR, Farber NE, Warltier DC, Gross GJ. Reduction of myocardial ischemia-reperfusion injury by KT-362, a new intracellular calcium antagonist in anesthetized dogs. J Cardiovasc Pharmacol. 1989 Apr;13(4):586-93. PubMed PMID: 2470996.
14: Eskinder H, Hillard CJ, Wilke RA, Gross GJ. Effect of KT-362, a putative intracellular calcium antagonist, on norepinephrine-induced contractions and inositol monophosphate accumulation in canine femoral artery. J Cardiovasc Pharmacol. 1989 Mar;13(3):502-7. PubMed PMID: 2471898.
15: Farber NE, Gross GJ. Cardioprotective effects of a new vascular intracellular calcium antagonist, KT-362, in the stunned myocardium. J Pharmacol Exp Ther. 1989 Jan;248(1):39-43. PubMed PMID: 2536431.
16: Kodama I, Wakabayashi S, Toyama J, Shibata S, Yamada K. Electrophysiological effects of KT-362, a new antiarrhythmic agent with vasodilating action, on isolated guinea pig ventricular muscle. J Cardiovasc Pharmacol. 1988 Jun;11(6):687-93. PubMed PMID: 2457764.
17: Hartman JC, Al-Wathiqui MH, Brooks HL, Gross GJ, Warltier DC. Hemodynamic and electrocardiographic actions of the new intracellular calcium antagonist, KT-362, in the conscious dog. Pharmacology. 1988;37(6):376-84. PubMed PMID: 3244744.
18: Shibata S, Wakabayashi S, Satake N, Hester RK, Ueda S, Tomiyama A. Mode of vasorelaxing action of 5-[3-[[2-(3,4-dimethoxyphenyl)-ethyl]amino]-1-oxopropyl]-2,3,4,5- tetrahydro-1,5-benzothiazepine fumarate (KT-362), a new intracellular calcium antagonist. J Pharmacol Exp Ther. 1987 Jan;240(1):16-22. PubMed PMID: 3100766.