| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 500mg | |||
| 1g | |||
| Other Sizes |
| Targets |
L-NIL HCl targets inducible nitric oxide synthase (iNOS), an enzyme that catalyzes the production of nitric oxide (NO) from L-arginine. iNOS is induced by inflammatory stimuli such as LPS and cytokines and produces large amounts of NO that contribute to inflammation and tissue damage. By selectively inhibiting iNOS, L-NIL HCl reduces the production of NO in inflammatory conditions. The compound shows selectivity for iNOS over eNOS and nNOS, which are constitutively expressed and have important physiological functions.
|
|---|---|
| ln Vitro |
L-NIL is significantly more effective in inhibiting mouse inducible NOS (miNOS) than rat brain constitutive NOS (rcNOS), and it does so in a concentration-dependent manner. According to the IC50 values of 3.3 and 92 pM for L-NIL with miNOS and rcNOS, respectively, L-NIL is 28 times more selective for miNOS. Furthermore, compared to L-NMA or L-NNA, L-NIL has a roughly 6-fold higher efficacy for miNOS[2].
In vitro, L-NIL HCl is a relatively selective inhibitor of iNOS with IC50 values of 0.4-3.3 µM for iNOS, 8-38 µM for eNOS, and 17-92 µM for nNOS. It effectively inhibits iNOS activity in cell-based assays. The compound's ability to inhibit iNOS has been confirmed in various cell types stimulated with LPS or inflammatory cytokines. L-NIL HCl has anti-inflammatory activity through the reduction of NO production. |
| ln Vivo |
In mice with renal IR, L-NIL (10 and 30 mg/kg, IP) inhibits autophagy, oxidative stress, and inflammation[1].
In vivo, L-NIL HCl effectively inhibits iNOS activity and has been used to demonstrate a critical role for iNOS in the immune response to infection by the protozoan L. major. It has anti-inflammatory activity in animal models. However, specific in vivo efficacy data in animal models are not extensively detailed in the available literature. The compound is a research tool for studying the role of iNOS in inflammation and immune responses. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for L-NIL HCl are iNOS inhibition assays using purified iNOS, eNOS, and nNOS enzymes. Each enzyme is incubated with L-arginine and cofactors in the presence of varying concentrations of L-NIL HCl, and the production of nitric oxide (NO) is measured using the Griess assay or chemiluminescence. The IC50 for inhibition of each NOS isoform is determined from dose-response curves.
|
| Cell Assay |
In vitro cellular assays for L-NIL HCl are performed using macrophages (RAW 264.7) or other cell types that express iNOS upon stimulation. Cells are treated with L-NIL HCl and stimulated with LPS or IFN-γ. Nitric oxide production is measured by the Griess assay. iNOS expression is assessed by Western blotting or quantitative PCR. Cell viability is evaluated using MTT assays to ensure that the observed inhibition of NO production is not due to cytotoxicity.
|
| Animal Protocol |
Animal/Disease Models: Adult male Balb/c (20-25 g)[1].
Doses: 10 and 30 mg/kg. Route of Administration: Intraperitoneally at the end of CLP and at 6 h after sepsis induction. Experimental Results: Led to a negligible increase in plasma NGAL compared to sham mice. Led to a significant decrease in both TLR4 and IL1β Protein contents and clusterin transcript. demonstrated an increase in NFAT5 mRNA levels, as compared with mice treated with vehicle. Promoted a decrease in AR protein expression, as compared with animals treated with vehicle. In vivo animal experiments for L-NIL HCl are conducted in rodent models of inflammation and infection. Mice are administered L-NIL HCl via oral or intraperitoneal injection, and inflammatory markers or pathogen load are assessed. In models of L. major infection, L-NIL HCl has been used to demonstrate a critical role for iNOS in the immune response. However, detailed protocols are not extensively documented in the available literature. |
| ADME/Pharmacokinetics |
L-NIL HCl has a molecular weight of 260.16 g/mol and a molecular formula of C8H19Cl2N3O2. It is a relatively selective iNOS inhibitor. The compound should be stored under recommended conditions. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As a research compound, L-NIL HCl is primarily used in in vitro and in vivo studies.
|
| Toxicity/Toxicokinetics |
The toxicological profile of L-NIL HCl has not been extensively characterized. As an iNOS inhibitor, the compound may have potential effects on immune function and NO-mediated physiological processes. No significant toxicity has been reported in the available literature. Standard toxicology studies would be necessary to establish its safety profile. The compound is a research tool and is not intended for human use.
|
| References |
|
| Additional Infomation |
N(6)-acetimidoyl-L-lysine dihydrochloride is a hydrochloride prepared from N(6)-acetimidoyl-L-lysine and two equivalents of hydrogen chloride. It is a selective inhibitor of inducible nitric oxide synthase and belongs to EC 1.14.13.39 (nitric oxide synthase) inhibitors. It contains the N(6)-acetimidoyl-L-lysine (2+) ion.
L-NIL HCl is a relatively selective inhibitor of inducible nitric oxide synthase (iNOS). It is also known as N-Iminoethyl-L-lysine dihydrochloride. L-NIL HCl exhibits IC50 values of 0.4-3.3 µM for iNOS, as opposed to 8-38 µM for eNOS and 17-92 µM for nNOS. It has been used to demonstrate a critical role for iNOS in the immune response to infection. L-NIL HCl is a research compound with potential applications in inflammation and immunology. |
| Molecular Formula |
C8H19CL2N3O2
|
|---|---|
| Molecular Weight |
260.15
|
| Exact Mass |
259.085
|
| CAS # |
159190-45-1
|
| Related CAS # |
L-NIL;53774-63-3;L-NIL hydrochloride;150403-89-7
|
| PubChem CID |
2733505
|
| Appearance |
Typically exists as solid at room temperature
|
| Boiling Point |
369ºC at 760 mmHg
|
| Flash Point |
177ºC
|
| LogP |
2.95
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
15
|
| Complexity |
192
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC(=NCCCC[C@@H](C(=O)O)N)N.Cl.Cl
|
| InChi Key |
OQIBCXRAFAHXMM-KLXURFKVSA-N
|
| InChi Code |
InChI=1S/C8H17N3O2.2ClH/c1-6(9)11-5-3-2-4-7(10)8(12)13;;/h7H,2-5,10H2,1H3,(H2,9,11)(H,12,13);2*1H/t7-;;/m0../s1
|
| Chemical Name |
(2S)-2-amino-6-(1-aminoethylideneamino)hexanoic acid;dihydrochloride
|
| Synonyms |
L-NIL HCl N-Iminoethyl-L-lysine dihydrochloride
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 3.8439 mL | 19.2197 mL | 38.4394 mL | |
| 5 mM | 0.7688 mL | 3.8439 mL | 7.6879 mL | |
| 10 mM | 0.3844 mL | 1.9220 mL | 3.8439 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
