ARL 17477 dihydrochloride |
| Catalog No.GC14802 |
Selective nNOS inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 866914-87-6
Sample solution is provided at 25 µL, 10mM.
;)
_1-7.$$$37316672@70.jpg');)
;)
;)
_273-287.$$$36806353@46.jpg');)
_1-16.$$$37156877@44.jpg');)
;)
;)
;)
_1124-1138.$$$35908550@30.jpg');)
_766-780.$$$37100057@30.jpg');)
_418-432.$$$36893736@30.jpg');)
_240-255.$$$35108512@29.jpg');)
_533-545.$$$36543525@28.jpg');)
_264-276.$$$36600053@22.jpg');)
_2214998.$$$@0.jpg');)
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.
| Cas No. | 866914-87-6 | SDF | |
| Chemical Name | (Z)-N'-(4-(2-((3-chlorobenzyl)amino)ethyl)phenyl)thiophene-2-carboximidamide dihydrochloride | ||
| Canonical SMILES | ClC1=CC=CC(CNCCC2=CC=C(/N=C(N)/C3=CC=CS3)C=C2)=C1.Cl.Cl | ||
| Formula | C20H20ClN3S.2HCl | M.Wt | 442.83 |
| Solubility | <22.14mg/ml in Water; <44.28mg/ml in DMSO | Storage | Desiccate at RT |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.2582 mL | 11.291 mL | 22.582 mL |
| 5 mM | 0.4516 mL | 2.2582 mL | 4.5164 mL |
| 10 mM | 0.2258 mL | 1.1291 mL | 2.2582 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *