| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
nNOS (neuronal nitric oxide synthase). Ki = 57 nM. 149-fold selective for nNOS over eNOS; no significant activity against iNOS (IC50 ~180 microM).
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|---|---|
| ln Vitro |
Potent, competitive nNOS inhibitor (Ki = 57 nM). Displays 149-fold selectivity for nNOS over eNOS. No significant in vitro cytotoxicity or non-specific enzyme inhibition reported. The compound directly binds to the active site of nNOS, competing with L-arginine for substrate binding, thereby reducing NO production in neurons.
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| ln Vivo |
Phencyclidine-induced disruption of prepulse inhibition and phencyclidine-induced enhancement of locomotor activity are blocked by Nω-Propyl-L-arginine (N-omega-Propyl-L-arginine) hydrochloride (20 mg/kg; ip) [2].
In male NMRI mice, Nomega-Propyl-L-arginine HCl (20 mg/kg; intraperitoneal, IP) blocks both phencyclidine (PCP)-induced disruption of prepulse inhibition (PPI) and PCP-induced stimulation of locomotor activity. These effects are mediated by inhibition of nNOS and subsequent reduction of NO production in the brain. No in vivo activity against eNOS at this dose. |
| Enzyme Assay |
Not applicable. Inhibitor potency determined by enzyme kinetics using purified nNOS enzyme. Standard cell-free enzyme activity assays measure conversion of [3H]-L-arginine to [3H]-L-citrulline in the presence of NADPH, Ca2+/calmodulin, and varying inhibitor concentrations. Ki (57 nM) determined by Lineweaver-Burk or Dixon plot analysis, confirming competitive mechanism of inhibition.
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| Cell Assay |
Not applicable. The compound is a selective nNOS inhibitor, and its activity is evaluated in enzyme assays. Typical cell-based assays: primary neuronal cultures or nNOS-expressing cell lines treated with Nomega-Propyl-L-arginine HCl (1-100 microM, 1-24h). NO production measured by Griess reagent (nitrite accumulation) or DAF-FM DA fluorescence (intracellular NO). Western blot for nNOS protein levels used to confirm target specificity.
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| Animal Protocol |
Animal/Disease Models: Male NMRI mouse (30-40 g) (phencyclidine-induced stimulation) [2]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection Experimental Results: Dramatically diminished phencyclidine-induced stimulation Prepulse inhibition is disrupted and Dramatically reduces phencyclidine-induced locomotor stimulation activity. Phencyclidine (PCP) mouse model: Male NMRI mice (30-40 g). Nomega-Propyl-L-arginine HCl (20 mg/kg, IP) administered 30 minutes before PCP (5 mg/kg, IP). Prepulse inhibition (PPI) measured 20 min after PCP injection; mice placed in startle chambers; prepulse (74-82 dB) presented 100 ms before 120 dB startle pulse. Locomotor activity measured in automated activity chambers for 30 min. Results: nNOS inhibitor blocks PCP-induced PPI disruption and hyperactivity. |
| ADME/Pharmacokinetics |
Specific PK data for Nomega-Propyl-L-arginine HCl are not detailed in standard references. As a polar, charged arginine analog (molecular weight 252.74), it is expected to be water-soluble, have limited oral bioavailability, and have a short plasma half-life. The compound is typically administered IP in animal studies to achieve rapid systemic exposure. Brain penetration is expected due to the observed CNS effects.
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| Toxicity/Toxicokinetics |
Toxic. Contains a pharmaceutically active ingredient. R28: Very toxic if swallowed. R38: Irritating to skin. R41: Risk of serious damage to eyes. R48: Toxic; danger of serious damage to health by prolonged exposure. Under fire conditions, may decompose and emit toxic fumes. Avoid release into the environment. Standard laboratory personal protective equipment (PPE) should be used; handling should be performed by personnel trained in handling of potent active pharmaceutical ingredients.
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| References |
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| Additional Infomation |
Nomega-Propyl-L-arginine HCl (NPA, NPLA, p-ARG, L-PNA) is a substrate-competitive, reversible, potent, and selective nNOS inhibitor, widely used as a pharmacological probe for nNOS-dependent physiological and pathological processes both in cultures and in animals. It is not approved for human therapeutic use. The compound has been instrumental in demonstrating the role of nNOS in PCP-induced behavioral abnormalities, linking nNOS activity to schizophrenia-like symptoms. Selectivity: 149× for nNOS over eNOS, >3000× over iNOS. Its utility stems from the high selectivity, enabling dissection of nNOS-specific effects from those of other NOS isoforms. Potential therapeutic applications in neurological disorders (stroke, neurodegeneration, pain) remain in preclinical research.
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| Molecular Formula |
C9H21CLN4O2
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|---|---|
| Molecular Weight |
252.741640806198
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| Exact Mass |
252.135
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| CAS # |
2321366-46-3
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| PubChem CID |
91885482
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| Appearance |
Colorless to off-white ointment
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
16
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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.Cl
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| InChi Key |
YTPXYHYMXLUNPN-FJXQXJEOSA-N
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| InChi Code |
InChI=1S/C9H20N4O2.ClH/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);1H/t7-;/m0./s1
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| Chemical Name |
(2S)-2-amino-5-[(N'-propylcarbamimidoyl)amino]pentanoic acid;hydrochloride
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| Synonyms |
NωPropylLarginine HCl; Nω Propyl L arginine HCl
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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) |
DMSO : ~25 mg/mL (~98.92 mM)
H2O : ~25 mg/mL (~98.92 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 | 3.9566 mL | 19.7832 mL | 39.5664 mL | |
| 5 mM | 0.7913 mL | 3.9566 mL | 7.9133 mL | |
| 10 mM | 0.3957 mL | 1.9783 mL | 3.9566 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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