| Size | Price | Stock | Qty |
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| 250mg |
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| 500mg |
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| 1g |
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TS-011 (TS 011; TS011) is a novel and potent inhibitor of 20-Hydroxyeicosatetraenoic acid synthesis. It can improve cerebral microcirculatory autoregulation impaired by middle cerebral artery occlusion in mice.
| ln Vivo |
The synthesis of 20-hydroxyeicosatetraenoic acid is selectively inhibited by TS-011. At 0.3 mg/kg, TS-011 prevented the drop in blood flow velocity at 1 and 7 hours following reperfusion (P<0.001). Furthermore, 24 hours following reperfusion, TS-011 reduced the rise in blood flow velocity (P<0.01). Microvascular perfusion regions are shielded from the loss shown in mice treated with vehicles by TS-011. TS-011 at 0.3 mg/kg (P<0.05) can also reduce infarct volume by about 40% [1]. Acute inhibition of 20-HETE production with TS-011 (1 mg/kg IV) significantly increased basilar artery diameter by 39% in 9 dogs with delayed vasospasm [2].
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| References |
[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 |
| Molecular Formula |
C₁₁H₁₄CLN₃O₂
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|---|---|
| Molecular Weight |
255.70
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| Exact Mass |
255.077
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| CAS # |
339071-18-0
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| PubChem CID |
9816527
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| Appearance |
Typically exists as solid at room temperature
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| Boiling Point |
477.8±55.0°C
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| LogP |
2.271
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
17
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| Complexity |
259
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| Defined Atom Stereocenter Count |
0
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| SMILES |
ClC1C([H])=C(C([H])=C([H])C=1N1C([H])([H])C([H])([H])OC([H])([H])C1([H])[H])/N=C(\[H])/N([H])O[H]
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| InChi Key |
ZTXADXBIGLLOFX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H14ClN3O2/c12-10-7-9(13-8-14-16)1-2-11(10)15-3-5-17-6-4-15/h1-2,7-8,16H,3-6H2,(H,13,14)
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| Chemical Name |
N'-(3-chloro-4-morpholin-4-ylphenyl)-N-hydroxymethanimidamide
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| Synonyms |
TS-011 TS 011TS011
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~977.71 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (8.13 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9108 mL | 19.5542 mL | 39.1083 mL | |
| 5 mM | 0.7822 mL | 3.9108 mL | 7.8217 mL | |
| 10 mM | 0.3911 mL | 1.9554 mL | 3.9108 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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