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TS-011

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Chemical Structure| 339071-18-0 同义名 : -
CAS号 : 339071-18-0
货号 : A729731
分子式 : C11H14ClN3O2
纯度 : 97%
分子量 : 255.701
MDL号 : MFCD21603938
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(977.71 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 TS-011, an inhibitor of 20-Hydroxyeicosatetraenoic acid synthesis, reduces infarct volume and improves neurological deficits in animal stroke models. TS-011 significantly inhibited both the decrease and the increase in the blood flow velocities in the peri-infarct microvessels seen in the vehicle-treated mice after reperfusion. In addition, TS-011 significantly inhibited the reduction in the microvascular perfusion area after reperfusion, compared with the vehicle-treated group. Moreover, TS-011 significantly reduced the infarct volume by 40% at 72 h after middle cerebral artery occlusion[3]. TS-011 (0.1 mg/kg, iv) reduced cortical infarct volume by approximately 70% and total infarct volume by 55%. TS-011 had no effect on the volume at risk or CBF during or up to 30 mins after the ischemic period. TS-011 reduced the delayed fall in CBF seen 2 h after reperfusion[4]. Blockade of the synthesis of 20-HETE with TS-011 (0.1 mg/kg iv) prevented the sustained fall in CBF produced by an icv injection of blood and the transient vasoconstrictor response to Hb. Hb (0.1%) reduced the diameter of the basilar artery (BA) of rats in vitro by 10 +/- 2%. This response was reversed by TS-011 (100 nM) [5].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.91mL

0.78mL

0.39mL

19.55mL

3.91mL

1.96mL

39.11mL

7.82mL

3.91mL
参考文献

[1]Marumo T, et al. The inhibitor of 20-HETE synthesis, TS-011, improves cerebral microcirculatory autoregulation impaired by middle cerebral artery occlusion in mice. Br J Pharmacol. 2010 Nov;161(6):1391-402.

[2]Hacein-Bey L, et al. Reversal of delayed vasospasm by TS-011 in the dual hemorrhage dog model of subarachnoid hemorrhage. AJNR Am J Neuroradiol. 2006 Jun-Jul;27(6):1350-4.

[3]Marumo T, Eto K, Wake H, Omura T, Nabekura J. The inhibitor of 20-HETE synthesis, TS-011, improves cerebral microcirculatory autoregulation impaired by middle cerebral artery occlusion in mice. Br J Pharmacol. 2010 Nov;161(6):1391-402

[4]Renic M, Klaus JA, Omura T, Kawashima N, Onishi M, Miyata N, Koehler RC, Harder DR, Roman RJ. Effect of 20-HETE inhibition on infarct volume and cerebral blood flow after transient middle cerebral artery occlusion. J Cereb Blood Flow Metab. 2009 Mar;29(3):629-39

[5]Takeuchi K, Miyata N, Renic M, Harder DR, Roman RJ. Hemoglobin, NO, and 20-HETE interactions in mediating cerebral vasoconstriction following SAH. Am J Physiol Regul Integr Comp Physiol. 2006 Jan;290(1):R84-9