An inhibitor of 20-HETE synthesis
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TS-011

Item No. 9002862

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3-chloro-4-(4-morpholinyl)phenyl]-N′-hydroxy-methanimidamide
CAS Number
339071-18-0
Molecular Formula
C11H14ClN3O2
Formula Weight
255.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMF: 3 mg/mlDMSO: 2 mg/mlEthanol: insolPBS (pH 7.2): insol
λmax
213, 271 nm
SMILES
ClC1=CC(N=CNO)=CC=C1N2CCOCC2
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)
InChi Key
ZTXADXBIGLLOFX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    50 mg

    $124

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    250 mg

    $490

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    Product Description

    TS-011 is an inhibitor of 20-hydroxyeicosatetraenoic acid (20-HETE) synthesis.1 It inhibits 20-HETE synthesis in human and rat renal microsomes (IC50s = 8.42 and 9.19 nM, respectively), as well as by the cytochrome P450 (CYP) isoforms CYP4F2, CYP4F3A, CYP4F3B, and CYP4A11 in cell-free assays (IC50s = 30.4, 42.6, 43.0, and 188 nM, respectively). It is selective for these CYPs over CYP1A2, CYP2C9, CYP2C19, CYP2D6, and CYP3A4 (IC50s = >60 µM for all), as well as a panel of receptors and other enzymes at 1 µM. TS-011 (0.01-1 mg/kg, i.v.) reverses decreases in cerebral blood flow and increases in cerebrospinal fluid 20-HETE levels in a rat model of subarachnoid hemorrhage. It also reduces infarct volume and prevents neurological deficits in a rat model of stroke induced by middle cerebral artery occlusion (MCAO).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Miyata, N., Seki, T., Tanaka, Y., et al. Beneficial effects of a new 20-hydroxyeicosatetraenoic acid synthesis inhibitor, TS-011 [N-(3-chloro-4-morpholin-4-yl) phenyl-N'-hydroxyimido formamide], on hemorrhagic and ischemic stroke. J. Pharmacol. Exp. Ther. 314(1), 77-85 (2005).

    2. Omura, T., Tanaka, Y., Miyata, N., et al. Effect of a new inhibitor of the synthesis of 20-HETE on cerebral ischemia reperfusion injury. Stroke 37(5), 1307-1313 (2006).