2. Immunology/Inflammation
  3. NO Synthase
  4. nNOS-IN-6

nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS Ki of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS Ki of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma.

For research use only. We do not sell to patients.

nNOS-IN-6

nNOS-IN-6 Chemical Structure

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

nNOS-IN-6 Related Antibodies

Top Publications Citing Use of Products

View All NO Synthase Isoform Specific Products:

View All Isoforms
nNOS iNOS eNOS

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS Ki of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS Ki of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma[1].

IC50 & Target

nNOS

16 nM (Ki)

In Vitro

nNOS-IN-6 (compound 16) potently inhibits human neuronal nitric oxide synthase (hnNOS) with a Ki of 16 nM, and exhibits approximately 1800-fold selectivity over human endothelial nitric oxide synthase (heNOS) and approximately 2900-fold selectivity over human inducible nitric oxide synthase (hiNOS)[1].
nNOS-IN-6 (200 μM; 17 h) exhibits high effective permeability (13.04×10-6 cm/s) in the PAMPA-BBB assay, demonstrating potent central nervous system penetration potential[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

nNOS-IN-6 Related Antibodies
Parmacokinetics
Species Dose Route C0/Cmax Tmax (Plasma) AUClast T1/2 Vss Bioavailability Cmax Tmax (Brain) CL
Mice[1] 3 mg/kg i.v. 654.08 ng/mL 0.083 h 654.03 ng·h/mL 2.49 h 16.08 L/kg / / / 74.6 mL/min/kg
Mice[1] 10 mg/kg p.o. 86.51 ng/mL 1.0 h 356.54 7.96 h 222.69 L/kg 16.4 % 172.0 ng/g 12.0 h /
In Vivo

nNOS-IN-6 (compound 16) (3-10 mg/kg; i.v., p.o.; single dose) exhibits high systemic clearance, low oral bioavailability, large volume of distribution, and delayed, measurable brain penetration in male C57BL/6 mice after single intravenous and oral doses[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice (male)[1]
Dosage: 3 mg/kg (i.v.);
10 mg/kg (p.o.)
Administration: i.v.; single dose; p.o.; single dose
Result: Exhibited initial plasma concentration (C0) of 654.08 ng/mL at 0.083 h, AUClast of 654.03 h·ng/mL, terminal half-life (t1/2) of 2.49 h, systemic clearance of 74.6 mL/min/kg, steady-state volume of distribution (Vss) of 16.08 L/kg after intravenous administration.
Reached plasma Cmax of 86.51 ng/mL at 1.0 h, AUClast of 356.54 h·ng/mL, t1/2 of 7.96 h, Vss of 222.69 L/kg, oral bioavailability of 16.4% after oral administration.
Achieved brain Cmax of 172.0 ng/g at 12.0 h, brain-Kp (AUClast) of 24.0 after oral administration.
Molecular Weight

370.25

Formula

C17H18Cl2FN3O
SMILES

CC1=C2C=C(C(C3=CC=C(C(CN)=C3)O)=CC2=NC(N)=C1)F.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

nNOS-IN-6 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

nNOS-IN-6NO SynthaseNitric oxide synthasesNOShuman eNOSrat nNOSmale C57BL/6 micePAMPA-BBB assaysmousemelanomahuman neuronal nitric oxide synthasehuman iNOSneurodegenerative diseasesblood-brain barrierInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Requested Quantity *

Applicant Name *

 

Salutation

Email Address *

 

Phone Number *

Department

 

Organization Name *

City

State

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
nNOS-IN-6
Cat. No.:
HY-181711
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

SAFETY DATA SHEET (SDS)

Request for HNMR Report

We have received your request and will respond to you as soon as possible.