WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H526979
CAS#: 150591-06-3
Description: TA-993 is a calcium channel antagonist potentially for the treatment of chronic peripheral arterial occlusive. TA-993 has a comparable antithrombotic effect with other antiplatelet agents, and thus it is a possible remedy for thrombotic and embolic diseases. TA-993 may become a clinically useful antiplatelet agent of this structure series.
Hodoodo Cat#: H526979
Name: TA-993 maleate
CAS#: 150591-06-3
Chemical Formula: C27H32N2O7S
Exact Mass: 0.00
Molecular Weight: 528.620
Elemental Analysis: C, 61.35; H, 6.10; N, 5.30; O, 21.19; S, 6.06
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Related CAS #: 150591-06-3 (maleate) 122024-96-8 (free)
Synonym: TA993 maleate, TA993, TA-993, TA 993
IUPAC/Chemical Name: 5-(2-(dimethylamino)ethyl)-8-methyl-4-oxo-2-(p-tolyl)-2,3,4,5-tetrahydrobenzo[b][1,4]thiazepin-3-yl acetate maleate
InChi Key: KILCEIIRMKHOSB-BTJKTKAUSA-N
InChi Code: InChI=1S/C23H28N2O3S.C4H4O4/c1-15-6-9-18(10-7-15)22-21(28-17(3)26)23(27)25(13-12-24(4)5)19-11-8-16(2)14-20(19)29-22;5-3(6)1-2-4(7)8/h6-11,14,21-22H,12-13H2,1-5H3;1-2H,(H,5,6)(H,7,8)/b;2-1-
SMILES Code: O=C1C(OC(C)=O)C(C2=CC=C(C)C=C2)SC3=CC(C)=CC=C3N1CCN(C)C.O=C(/C=C\C(O)=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:
| Biological target: | |
| In vitro activity: | |
| In vivo activity: |
The following data is based on the product molecular weight 528.62 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: Katoh M, Karasawa T, Doi H, Odawara A. Effects of the antiplatelet agent TA-993 and its metabolite MB3 on the hemorheological properties of rat and human erythrocytes. Thromb Res. 2001 Oct 15;104(2):105-12. PubMed PMID: 11672754.
2: Katoh M, Karasawa T, Watanabe A, Takagi M, Ikeo T, Odawara A. Inhibitory effects of TA-993 and its metabolite MB3 on platelet activation induced by collagen and U-46619 in human platelets. Biol Pharm Bull. 2001 May;24(5):501-4. PubMed PMID: 11379769.
3: Doi H, Kaburaki M, Inoue H, Suzumura K, Narita H. Protective effect of TA-993, a novel therapeutic agent for peripheral circulatory insufficiency, on skeletal muscle fatigue in a rat model of hindlimb ischemia. Jpn J Pharmacol. 2000 May;83(1):73-81. PubMed PMID: 10887943.
4: Katoh M, Karasawa T, Doi H, Odawara A, Takagi M, Ikeo T, Narita H. Antiplatelet mechanisms of TA-993 and its metabolite MB3 in ADP-induced platelet aggregation. Eur J Pharmacol. 2000 Jul 7;399(2-3):91-6. PubMed PMID: 10884507.
5: Kaburaki M, Yabana H, Doi H, Nagata K, Narita H, Murata S. The mechanism of the increasing action of TA-993, a new 1,5- benzothiazepine derivative, on limb blood flow in anesthetized dogs: selective suppression of sympathetic nerve activity. J Pharmacol Exp Ther. 1999 Mar;288(3):1167-73. PubMed PMID: 10027855.
6: Kaburaki M, Doi H, Narita H, Odawara A, Yasoshima A, Murata S. Antithrombotic action of TA-993, a new 1,5-benzothiazepine derivative, in a canine model of femoral arterial thrombosis. J Cardiovasc Pharmacol. 1998 Mar;31(3):470-7. PubMed PMID: 9514194.
7: Kaburaki M, Inoue H, Doi H, Yasuhara M, Narita H. Cardiovascular effects of 1,5-benzothiazepine derivatives having a l-cis and d-cis configuration in anesthetized dogs. Biol Pharm Bull. 1998 Jan;21(1):50-5. PubMed PMID: 9477168.
8: Kaburaki M, Narita H, Yabana H, Karasawa T, Doi H, Murata S. Cardiovascular effect of a new 1,5-benzothiazepine derivative TA-993 in anesthetized dogs. J Cardiovasc Pharmacol. 1998 Feb;31(2):240-7. PubMed PMID: 9475265.
9: Odawara A, Kikkawa K, Katoh M, Toryu H, Shimazaki T, Sasaki Y. Inhibitory effects of TA-993, a new 1,5-benzothiazepine derivative, on platelet aggregation. Circ Res. 1996 Apr;78(4):643-9. PubMed PMID: 8635222.
10: Narita H, Kaburaki M, Doi H, Yasoshima A, Murata S. Antithrombotic effect of TA-993, a novel 1,5-benzothiazepine derivative, in conscious rats. Jpn J Pharmacol. 1995 Aug;68(4):397-404. PubMed PMID: 8531414.
