LOE 908 hydrochloride
LOE 908 hydrochloride is a non-selective cation channel (NSCC) inhibitor.
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- CAS No.: 143482-60-4
- 화학식: C41H49ClN2O9
- 분자량:749.29
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Calcium Channel Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
12.6 μM
Compound: LOE 908 Hydrochloride
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Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of rat PXR expressed in human HepG2 cells after 24 hrs by luciferase reporter gene based luminescent analysis
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[PMID: 20966043] |
| HepG2 | EC50 |
3.2 μM
Compound: LOE 908 Hydrochloride
|
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis
|
[PMID: 20966043] |
LOE 908 hydrochloride blocks cation conductance in a concentration-dependent manner with an IC50 of 560 nM, and blocks dihydropyridine-sensitive Ba2+ current through voltage-dependent Ca2+ channels with an IC50 of 28 μM in voltage-clamped A7r5 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult male Sprague-Dawley rats, lateral fluid percussion brain injury model[2]
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Dosage:4 mg/kg bolus followed by 160 mg/kg over 24 h or 2 mg/kg bolus followed by 80 mg/kg over 24 h
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Administration:Intravenous administration
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Result:Significantly improved neuromotor function at 48 h postinjury when compared to vehicle treatment.
Chemical Information
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CAS No. 143482-60-4
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분자량 749.29
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화학식 C41H49ClN2O9
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SMILES
COC(C(OC)=C(OC)C=C1)=C1CCN(CCC2=C(C(OC)=C(OC)C=C2)OC)C(C(C3=CC=CC=C3)C4=NCCC5=CC(OC)=C(OC)C=C45)=O.[H]Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[1]. Krautwurst D, et al. The isoquinoline derivative LOE 908 selectively blocks vasopressin-activated nonselective cation currents in A7r5 aortic smooth muscle cells. Naunyn Schmiedebergs Arch Pharmacol. 1994 Mar;349(3):301-7. [Content Brief]
[2]. Cheney JA, et al. The novel compound LOE 908 attenuates acute neuromotor dysfunction but not cognitive impairment or cortical tissue loss following traumatic brain injury in rats. J Neurotrauma. 2000 Jan;17(1):83-91. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)