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Tirilazad mesylate

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names：
21-(4-(2,6-di-1-Pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl)-16-methylpregna-1,4,9(11)-triene-3,20-dione monomethanesulfonate
CAS號：
110101-67-2
MDL Number：
MF(分子式)： C39H56N6O5S MW(分子量)： 720.974
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文別名	21-(4-(2,6-di-1-Pyrrolidinyl-4-pyrimidinyl)-1-piperazinyl)-16-methylpregna-1,4,9(11)-triene-3,20-dione monomethanesulfonate
英文別名	U 74006F; U74006F; U-74006F; U 74006; U74006; U-74006; Tirilazad mesylate; tradename Freedox.
CAS號	110101-67-2
Inchi	InChI=1S/C38H52N6O2.CH4O3S/c1-26-22-31-29-9-8-27-23-28(45)10-12-37(27,2)30(29)11-13-38(31,3)35(26)32(46)25-41-18-20-43(21-19-41)34-24-33(42-14-4-5-15-42)39-36(40-34)44-16-6-7-17-44;1-5(2,3)4/h10-12,23-24,26,29,31,35H,4-9,13-22,25H2,1-3H3;1H3,(H,2,3,4)/t26?,29-,31+,35-,37+,38+;/m1./s1
InchiKey	HPZOOQSXPMEJBV-CAGOZALDSA-N
分子式 Formula	C39H56N6O5S
分子量 Molecular Weight	720.974
溶解度Solubility
性狀	Solid powder
儲藏條件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

產品說明	Tirilazad mesylate(CAS:110101-67-2 ):僅限應用于工業或者科學研究過程中非醫療目的，不應用于人類或動物的臨床診斷以及治過程療，該產品非藥用，非食用。
Introduction	Tirilazad, also known as U 74006F, is a lazaroid and potent inhibitor of iron-dependent lipid peroxidation. Tirilazad has shown excellent activity in in vivo models of experimental central nervous system trauma & ischemia. Tirilazad is a drug that has been proposed to treat acute ischaemic stroke. When tested on animal models, tirilazad protects brain tissue, and reduces brain damage. However, the drug fails to treat, and even worsens a stroke when studied on a human being. Tirilazad currently has no usage in the clinical treatment of stroke.
Application1
Application2
Application3

警示圖
危險性	Warning
危險性警示
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[1]Bracken MB, Shepard MJ, Holford TR, Leo-Summers L, Aldrich EF, Fazl M, Fehlings M, Herr DL, Hitchon PW, Marshall LF, Nockels RP, Pascale V, Perot PL Jr, Piepmeier J, Sonntag VK, Wagner F, Wilberger JE, Winn HR, Young W. Administration of methylprednisolone for 24 or 48 hours or tirilazad mesylate for 48 hours in the treatment of acute spinal cord injury. Results of the Third National Acute Spinal Cord Injury Randomized Controlled Trial. National Acute Spinal Cord Injury Study. JAMA. 1997 May 28;277(20):1597-604. PubMed PMID: 9168289.

[2]Zhang S, Wang L, Liu M, Wu B. Tirilazad for aneurysmal subarachnoid haemorrhage. Cochrane Database Syst Rev. 2010 Feb 17;(2):CD006778. doi: 10.1002/14651858.CD006778.pub2. Review. PubMed PMID: 20166088.

[3] Fleishaker JC, Pearson PG, Wienkers LC, Pearson LK, Moore TA, Peters GR. Biotransformation of tirilazad in human: 4. effect of finasteride on tirilazad clearance and reduced metabolite formation. J Pharmacol Exp Ther. 1998 Nov;287(2):591-7. PubMed PMID: 9808685.

[4] Jang YG, Ilodigwe D, Macdonald RL. Metaanalysis of tirilazad mesylate in patients with aneurysmal subarachnoid hemorrhage. Neurocrit Care. 2009;10(1):141-7. doi: 10.1007/s12028-008-9147-y. Epub 2008 Sep 23. PubMed PMID: 18810661.

[5] Fleishaker JC, Pearson PG, Wienkers LC, Pearson LK, Peters GR. Biotransformation of tirilazad in human: 2. Effect of ketoconazole on tirilazad clearance and oral bioavailability. J Pharmacol Exp Ther. 1996 May;277(2):991-8. PubMed PMID: 8627582.

6: Fleishaker JC, Peters GR. Pharmacokinetics of tirilazad and U-89678 in ischemic stroke patients receiving a loading regimen and maintenance regimen of 10 mg/kg/day of tirilazad. J Clin Pharmacol. 1996 Sep;36(9):809-13. PubMed PMID: 8889901.7: Wang Y, Cory AL. A novel stable supersaturated submicron lipid emulsion of tirilazad. Pharm Dev Technol. 1999 Aug;4(3):333-45. PubMed PMID: 10434279.8: Fleishaker JC, Hulst LK, Peters GR. Multiple-dose tolerability and pharmacokinetics of tirilazad mesylate at doses of up to 10 mg/kg/day administered over 5-10 days in healthy volunteers. Int J Clin Pharmacol Ther. 1994 May;32(5):223-30. PubMed PMID: 7921515.9: Wienkers LC, Steenwyk RC, Hauer MJ, Fleishaker JC, Pearson PG. Biotransformation of tirilazad in human: 3. tirilazad A-ring reduction by human liver microsomal 5alpha-reductase type 1 and type 2. J Pharmacol Exp Ther. 1998 Nov;287(2):583-90. PubMed PMID: 9808684.10: Fleishaker JC, Pearson LK, Peters GR. Induction of tirilazad clearance by phenytoin. Biopharm Drug Dispos. 1998 Mar;19(2):91-6. PubMed PMID: 9533108.1

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