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ARL 17477 dihydrochloride

Selective nNOS inhibitor CAS# 866914-87-6

ARL 17477 dihydrochloride

Catalog No. BCC7647----Order now to get a substantial discount!

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Chemical structure

ARL 17477 dihydrochloride

3D structure

Chemical Properties of ARL 17477 dihydrochloride

Cas No. 866914-87-6 SDF Download SDF
PubChem ID 9824646 Appearance Powder
Formula C20H22Cl3N3S M.Wt 442.83
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble to 50 mM in water and to 100 mM in DMSO
Chemical Name N'-[4-[2-[(3-chlorophenyl)methylamino]ethyl]phenyl]thiophene-2-carboximidamide;dihydrochloride
SMILES C1=CC(=CC(=C1)Cl)CNCCC2=CC=C(C=C2)N=C(C3=CC=CS3)N.Cl.Cl
Standard InChIKey SOXBYIKSUDXMIE-UHFFFAOYSA-N
Standard InChI InChI=1S/C20H20ClN3S.2ClH/c21-17-4-1-3-16(13-17)14-23-11-10-15-6-8-18(9-7-15)24-20(22)19-5-2-12-25-19;;/h1-9,12-13,23H,10-11,14H2,(H2,22,24);2*1H
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of ARL 17477 dihydrochloride

DescriptionSelective neuronal nitrogen oxide synthase (nNOS) inhibitor (IC50 values are 1 and 17 μM for nNOS and endothelial NOS respectively). Reduces ischemic cell damage after middle cerebral artery (MCA) occlusion in rats. Displays a synergistic neuroprotective effect when combined with either an NMDA or AMPA receptor antagonist.

ARL 17477 dihydrochloride Dilution Calculator

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ARL 17477 dihydrochloride Molarity Calculator

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Preparing Stock Solutions of ARL 17477 dihydrochloride

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.2582 mL 11.291 mL 22.582 mL 45.1641 mL 56.4551 mL
5 mM 0.4516 mL 2.2582 mL 4.5164 mL 9.0328 mL 11.291 mL
10 mM 0.2258 mL 1.1291 mL 2.2582 mL 4.5164 mL 5.6455 mL
50 mM 0.0452 mL 0.2258 mL 0.4516 mL 0.9033 mL 1.1291 mL
100 mM 0.0226 mL 0.1129 mL 0.2258 mL 0.4516 mL 0.5646 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on ARL 17477 dihydrochloride

ARL 17477 dihydrochloride is a selective and potent neuronal nitrogen oxide synthase (nNOS) inhibitor with IC50 values of 1 and 17μM for nNOS and endothelial NOS, respectively [1].
Neuronal NOS (nNOS) plays an important role in the development of ischaemic brain necrosis while endothelial NOS (eNOS) protects brain tissue through increasing ischaemic regional cerebral blood flow [1].
In rats after transient MCA occlusion, ARL 17477 (1mg/kg, 3mg/kg and 10mg/kg) reduced ischemic infarct volume by 53%, 23% and 6.5% respectively in a dose-dependent way. ARL 17477 (10 mg/kg) significantly reduced regional cerebral blood flow (rCBF) by 27±5.3% and 24±14.08%. Also, it reduced cortical NOS activity by 86±14.9% and 91±8.9% at 10 min or 3 h, respectively [2]. In the global cerebral ischaemia gerbil model, the combination of MK-801 with ARL 17477 provided 44% greater protection than the total protection or either alone. Likewise, the combination of LY293558 with ARL 17477 provided 35% greater protection than total protection of either compound alone [3].
References:
[1]. O'Neill MJ, Murray TK, McCarty DR, et al. ARL 17477, a selective nitric oxide synthase inhibitor, with neuroprotective effects in animal models of global and focal cerebral ischaemia. Brain Res, 2000, 871(2): 234-244.
[2]. Zhang ZG, Reif D, Macdonald J, et al. ARL 17477, a potent and selective neuronal NOS inhibitor decreases infarct volume after transient middle cerebral artery occlusion in rats. J Cereb Blood Flow Metab, 1996, 16(4): 599-604.
[3]. Hicks CA, Ward MA, Swettenham JB, et al. Synergistic neuroprotective effects by combining an NMDA or AMPA receptor antagonist with nitric oxide synthase inhibitors in global cerebral ischaemia. Eur J Pharmacol, 1999, 381(2-3): 113-119.

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References on ARL 17477 dihydrochloride

ARL 17477, a selective nitric oxide synthase inhibitor, with neuroprotective effects in animal models of global and focal cerebral ischaemia.[Pubmed:10899290]

Brain Res. 2000 Jul 21;871(2):234-44.

In the present studies, we have evaluated the effects of N-[4-(2- inverted question mark[(3-Chlorophenyl)methyl]amino inverted question markethyl)phenyl]-2-thiophenecarbo ximidamide dihydrochloride (ARL 17477) on recombinant human neuronal NOS (nNOS) and endothelial NOS (eNOS). We then carried out pharmacokinetic studies and measured cortical nitric oxide synthase (NOS) inhibition to determine that the compound crossed the blood brain barrier. Finally, the compound was evaluated in a model of global ischaemia in the gerbil and two models of transient focal ischaemia in the rat. The IC(50) values for ARL 17477 on human recombinant human nNOS and eNOS were 1 and 17 microM, respectively. ARL 17477 (50 mg/kg i.p.) produced a significant reduction in the ischaemia-induced hippocampal damage following global ischaemia when administered immediately post-occlusion, but failed to protect when administration was delayed until 30 min post-occlusion. In the endothelin-1 model of focal ischaemia, ARL 17477 (1 mg/kg i.v.) significantly attenuated the infarct volume when administered at either 0, 1 or 2 h post-endothelin-1 (P<0.05). In the intraluminal suture model, ARL 17477 at both 1 and 3 mg/kg i.v. failed to reduce the infarct volume measured at 1, 3 or 7 days post-occlusion. These results demonstrate that ARL 17477 protects against global ischaemia in gerbils and provides some reduction in infarct volume following transient middle cerebral artery occlusion in rats, indicating that nNOS inhibition may be a useful treatment of ischaemic conditions.

Synergistic neuroprotective effects by combining an NMDA or AMPA receptor antagonist with nitric oxide synthase inhibitors in global cerebral ischaemia.[Pubmed:10554878]

Eur J Pharmacol. 1999 Sep 24;381(2-3):113-9.

We have investigated the neuroprotective effects of combining an NMDA or AMPA receptor antagonist with a nitric oxide synthase (NOS) inhibitor in the gerbil model of global cerebral ischaemia. Ischaemia was induced by occlusion of the common carotid arteries for 5 min. (5R,10S)-(+)-5-methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,1 0-imine (MK-801, 2.5 mg/kg i.p.) or (3S,4aR,6R,8aR)-6-[2-(1(2)H-tetrazole-5-yl)]decahydroisoq uinoline-3-carboxylic acid (LY293558, 20 mg/kg i.p.) and 7-nitroindazole (25 mg/kg i.p.) or N-[4-(2-[[(3-chlorophenyl)methyl]amino]ethyl) phenyl]-2-thiophenecarboximidamide dihydrochloride (ARL17477, 25 mg/kg i.p.) were administered alone or in combination (i.e., MK-801 with 7-nitroindazole or ARL17477 or LY293558 with 7-nitroindazole or ARL17477). In the present studies, both MK-801 and LY293558 provided significant degree of neuroprotection, while 7-nitroindazole and ARL17477 also provided some neuroprotection, which failed to reach significance in every case. However, the combination of MK-801 with 7-nitroindazole or ARL17477 provided 21% or 44% greater protection than the total protection or either alone. Likewise, the combination of LY293558 with 7-nitroindazole or ARL17477 provided 14.5% and 35% greater protection than total protection of either compound alone. These results indicate that several pathways contribute to ischaemic cell death and combining excitatory amino antagonists and NOS inhibitors provides greater protection than either alone. Therefore, combination therapy should be considered as an approach for treating ischaemic conditions.

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