1400W 2HCl

Catalog No.S8337 Batch:S833702

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Technical Data

Formula

C10H15N3.2HCl

Molecular Weight 250.17 CAS No. 214358-33-5
Solubility (25°C)* In vitro DMSO 50 mg/mL (199.86 mM)
Water 50 mg/mL (199.86 mM)
Ethanol 13 mg/mL (51.96 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description 1400W (N-(3-(Aminomethyl)benzyl)acetamidine) is a slow, tight binding, and highly selective inhibitor of inducible nitric-oxide synthase(iNOS).
Targets
iNOS [1]
(Cell-free assay)
nNOS [1]
(Cell-free assay)
eNOS [1]
(Cell-free assay)
<7 nM(Kd) 2 μM(Ki) 50 μM(Ki)
In vitro 1400W is either an irreversible inhibitor or an extremely slowly reversible inhibitor of human iNOS. Inhibition of human iNOS by 1400W is time-dependent. 1400W is competitive with L-arginine. 1400W is not a substrate for iNOS[1].
In vivo 1400W selectively prevents microvasculature injury in rats. 1400W is greater than 50-fold more potent against iNOS than eNOS in a rat model of endotoxin-induced vascular injury. Moreover, 1400W also dose-dependently reduces LPS-induced vascular leakage associated with iNOS induction in the colon, lung, liver, kidney, and heart. The maximal protection is close to 100% for all organs except the kidney (kidney:54%)[1]. 1400W has an ameliorative effect on both oxidative and nitrosative stress in the kidneys against renal I/R injury in rats[2]. Treatment with 1400W can reduce the rate of growth of solid tumors in mice[4].

Protocol (from reference)

Cell Assay:[3]
  • Cell lines

    RAW264.7 cells

  • Concentrations

    100 μM

  • Incubation Time

    16 h

  • Method

    RAW264.7 cells are treated with LPS/IFNγ for 16 h and GAPDH-p300 binding is abolished by the iNOS inhibitor 1400W (100 μM). Cell lysates are immunoprecipitated with an anti-p300 antibody and the immunoprecipitates are analysed by western blotting with an anti-GAPDH antibody.

Animal Study:[1]
  • Animal Models

    Rats

  • Dosages

    0.1-10 mg/kg

  • Administration

    s.c.

Selleck's 1400W 2HCl has been cited by 18 publications

iNOS is necessary for GBP-mediated T. gondii clearance in murine macrophages via vacuole nitration and intravacuolar network collapse [ Nat Commun, 2024, 15(1):2698] PubMed: 38538595
Uncovering therapeutic targets for macrophage-mediated T cell suppression and PD-L1 therapy sensitization [ Cell Rep Med, 2024, S2666-3791(24)00419-1] PubMed: 39181134
Normalization of CF Immune System Reverses Intestinal Neutrophilic Inflammation and Significantly Improves the Survival of CF Mice [ Cell Mol Gastroenterol Hepatol, 2024, S2352-345X(24)00179-6] PubMed: 39510500
Nitric oxide facilitates the S-nitrosylation and deubiquitination of Notch1 protein to maintain cancer stem cells in human NSCLC [ J Cell Mol Med, 2024, 28(21):e70203] PubMed: 39523215
Ninjinyoeito Prevents Onset of Depression-Like Behavior and Reduces Hippocampal iNOS Expression in Senescence-Accelerated Mouse Prone 8 Mice [ Evid Based Complement Alternat Med, 2023, 2023:2151004] PubMed: 37593014
Ninjinyoeito Prevents Onset of Depression-Like Behavior and Reduces Hippocampal iNOS Expression in Senescence-Accelerated Mouse Prone 8 Mice [ Evid Based Complement Alternat Med, 2023, 2023:2151004] PubMed: 37593014
Inducible nitric oxide synthase (iNOS) is necessary for GBP-mediated T. gondii restriction in murine macrophages via vacuole nitration and intravacuolar network collapse [ bioRxiv, 2023, 2023.07.24.549965] PubMed: 37546987
Inducible nitric oxide synthase (iNOS) is necessary for GBP-mediated T. gondii restriction in murine macrophages via vacuole nitration and intravacuolar network collapse [ bioRxiv, 2023, 2023.07.24.549965] PubMed: 37546987
Inflammatory fibroblasts mediate resistance to neoadjuvant therapy in rectal cancer [ Cancer Cell, 2022, 40(2):168-184.e13] PubMed: 35120600
Identification of potential anti-pneumonia pharmacological components of Glycyrrhizae Radix et Rhizoma after the treatment with Gan An He Ji oral liquid [ J Pharm Anal, 2022, 12(6):839-851] PubMed: 36605579

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.