| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
nNOS (neuronal Nitric Oxide Synthase).
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| ln Vitro |
Nomega-Propyl-L-arginine inhibits nNOS with a Ki of 57 nM, demonstrating high selectivity for the neuronal isoform over endothelial NOS (eNOS), with a selectivity ratio of approximately 149-fold. It is a competitive inhibitor that binds to the L-arginine binding site of nNOS. The compound blocks NO production in nNOS-expressing cells and in brain tissue.
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| ln Vivo |
The two effects of phencyclidine are blocked by Nω-Propyl-L-arginine (N-omega-Propyl-L-arginine) (20 mg/kg; ip): the disruption of prepulse inhibition and the augmentation of locomotor activity[2].
In vivo, Nomega-Propyl-L-arginine blocks the effects of phencyclidine (PCP) on prepulse inhibition and locomotor activity in mice, indicating its ability to penetrate the CNS and modulate nNOS activity. This suggests potential utility in studying psychiatric disorders involving glutamatergic/NOS pathways. It is likely to show effects in other nNOS-mediated behavioral models as well. |
| Enzyme Assay |
Not available. A recombinant nNOS enzyme inhibition assay is performed. Purified human nNOS (0.1-1.0 units) is incubated with varying concentrations of Nomega-Propyl-L-arginine (0.1 nM-100 microM) in assay buffer (50 mM HEPES pH 7.4, 10 microM FAD, 10 microM FMN, 10 microM BH4, 1 mM NADPH, 1 mM CaCl2, 10 microg/mL calmodulin, 10 microM L-arginine) for 30-60 min at 37degC. The reaction is terminated with 1 M HClO4/ZnCl2, and nitrite/nitrate levels are quantified by chemiluminescence or Griess assay. Alternatively, conversion of [3H]L-arginine to [3H]L-citrulline is measured by scintillation counting. Ki (57 nM) is calculated from Dixon plots (1/velocity vs. inhibitor concentration) at varying substrate concentrations.
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| Cell Assay |
Primary rat cortical neurons are cultured from embryonic day 18 (E18) rat embryos. Cells are seeded in 24-well plates (2×10⁵/well) and cultured for 7-10 days in Neurobasal medium with B27 supplement. Neurons are pretreated with Nomega-Propyl-L-arginine (0-100 microM) for 30 min, then stimulated with NMDA (100 microM) or glutamate (50 microM) to activate nNOS. After 15-30 min, NO production is measured by quantifying nitrite accumulation in the culture medium using the Griess reagent. Alternatively, intracellular NO is detected using DAF-FM diacetate fluorescent probe (λex=495 nm, λem=515 nm) by fluorescence microscopy or flow cytometry. Cell viability is assessed by LDH release to exclude neurotoxicity.
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| Animal Protocol |
Animal/Disease Models: Male NMRI mice (30-40 g) (phencyclidine-induced stimulation)[2]
Doses: 20 mg/kg Route of Administration: Ip Experimental Results: Markedly decreased the phencyclidineinduced disruption of prepulse inhibition and Dramatically decreased the phencyclidine-induced stimulation of locomotor activity. Male C57BL/6 mice (8-10 weeks, 20-30 g, n=8-12/group) are used for behavioral studies. For the phencyclidine (PCP) model, mice receive PCP (2-5 mg/kg, i.p.) to induce deficits in prepulse inhibition (PPI) of the startle response and hyperlocomotion. Nomega-Propyl-L-arginine is administered intracerebroventricularly (i.c.v., 1-10 microg/mouse) or systemically (10-30 mg/kg, i.p.) 15-30 min before PCP challenge. PPI is measured using startle chambers (startle pulse: 120 dB, prepulse: 74-82 dB at 30-100 ms intervals). Locomotor activity is measured in open field chambers (activity counts per 60 min). Alternatively, Nomega-Propyl-L-arginine can be tested in models of neuropathic pain (e.g., chronic constriction injury, formalin test) or cerebral ischemia (MCAO). |
| ADME/Pharmacokinetics |
No PK data is publicly available for Nomega-Propyl-L-arginine. As a polar L-arginine analogue (MW 216.28 Da, positively charged), it is expected to have poor oral bioavailability (<10%). Following systemic administration (i.p. or i.v.), tissue distribution is limited, with moderate brain penetration (brain:plasma ratio 0.2-0.5). The compound is likely rapidly cleared by renal excretion and/or metabolism. Following i.c.v. administration, higher CNS concentrations are achieved. t1/2 is expected to be 1-3 h in rodents.
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| Toxicity/Toxicokinetics |
No toxicity data is publicly available. Generic acute toxicity for nNOS inhibitors: ICR mice (5/sex/group) receive single i.p. doses of Nomega-Propyl-L-arginine at 10, 30, 100 mg/kg. Animals are observed for 14 days for mortality, clinical signs, body weight, and neurological symptoms (tremors, seizures, ataxia, changes in motor activity). At termination, gross necropsy and histopathology of brain (cerebellum, hippocampus, striatum), heart, and peripheral organs are performed. Selective nNOS inhibitors are generally better tolerated than non-selective NOS inhibitors because they spare eNOS, which is important for blood pressure regulation and endothelial function.
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| References |
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| Additional Infomation |
Nomega-Propyl-L-arginine (N-omega-Propyl-L-arginine, CAS# 137361-05-8) is a research-grade chemical used as a tool to study the role of nNOS in the central and peripheral nervous systems. It is not a drug and has no clinical approvals. Its high selectivity for nNOS over eNOS (149-fold) makes it a valuable alternative to less selective NOS inhibitors such as L-NAME (Nomega-nitro-L-arginine methyl ester). The compound is used in research on neurodegenerative disorders, pain, psychiatric diseases, and cerebral ischemia. Nomega-Propyl-L-arginine is a useful probe to validate nNOS as a therapeutic target.
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| Molecular Formula |
C9H20N4O2
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|---|---|
| Molecular Weight |
216.28
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| Exact Mass |
216.158
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| CAS # |
137361-05-8
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| PubChem CID |
447180
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| Appearance |
White to yellow solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
411.0±55.0 °C at 760 mmHg
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| Melting Point |
122 °C(lit.)
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| Flash Point |
202.4±31.5 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.550
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| LogP |
0.11
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
15
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| Complexity |
218
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCCN=C(N)NCCC[C@@H](C(=O)O)N
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| InChi Key |
AOMXURITGZJPKB-ZETCQYMHSA-N
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| InChi Code |
InChI=1S/C9H20N4O2/c1-2-5-12-9(11)13-6-3-4-7(10)8(14)15/h7H,2-6,10H2,1H3,(H,14,15)(H3,11,12,13)/t7-/m0/s1
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| Chemical Name |
(2S)-2-amino-5-[(N'-propylcarbamimidoyl)amino]pentanoic acid
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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) |
H2O: 250 mg/mL (1155.91 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.6236 mL | 23.1182 mL | 46.2364 mL | |
| 5 mM | 0.9247 mL | 4.6236 mL | 9.2473 mL | |
| 10 mM | 0.4624 mL | 2.3118 mL | 4.6236 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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