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Chemical Structure| 6631-94-3 Chemical Structure| 6631-94-3

Structure of ML171
CAS No.: 6631-94-3

Chemical Structure| 6631-94-3

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ML171 (2-Acetylphenothiazine; 2-APT) is a potent and selective NADPH oxidase 1 (Nox1) inhibitor that blocks Nox1-dependent ROS generation with an IC50 of 0.25 μM in a HEK293-Nox1 confirmatory assay.

Synonyms: 2-Acetylphenothiazine; 2-APT; Ethanone, 1-(10H-phenothiazin-2-yl)-

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Product Details of ML171

CAS No. :6631-94-3
Formula : C14H11NOS
M.W : 241.31
SMILES Code : CC(C(C=C1N2)=CC=C1SC3=C2C=CC=C3)=O
Synonyms :
2-Acetylphenothiazine; 2-APT; Ethanone, 1-(10H-phenothiazin-2-yl)-
MDL No. :MFCD00005017
InChI Key :JWGBOHJGWOPYCL-UHFFFAOYSA-N
Pubchem ID :81131

Safety of ML171

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H412
Precautionary Statements:P273

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
Human platelets 5 μM Zafirlukast inhibited platelet aggregation and fibrinogen binding with an IC50 of 1.66 μM PMC3909778
Mouse platelets 5 μM 2 minutes ML171 significantly suppressed CRP-induced ROS production without significantly affecting platelet aggregation or αIIbβ3 activation PMC3909778
Vascular smooth muscle cells (VSMCs) 10 μM 24 hours Bay K8644, as an L-type calcium channel agonist, was used to block the SO2-induced reduction of intracellular calcium content in PDGF-stimulated VSMCs. PMC8661704
HCT116 cells 10 μM 48 hours To evaluate the effect of terbinafine on CRC cell viability, results showed that terbinafine significantly reduced the viability of HCT116 cells. PMC10052827
Rat abdominal adipose-derived mesenchymal stromal cells (aASCs) 0.5, 2.5, 5 μM starting at passage 2 NOX1 inhibitor ML171 reduced ROS accumulation, apoptosis, and promoted long-term expansion of aASCs. PMC4650551
Platelets 30 μM TRAP-6 10 minutes To evaluate the effect of Argatroban on VITT IgG binding to PF4, results showed Argatroban at therapeutic concentrations did not significantly inhibit VITT IgG binding to PF4 PMC7985666
Vascular smooth muscle cells (VSMC) 0.5 μM 30 minutes To evaluate the effect of OA-NO2 on Ang II-induced IP3 production and calcium mobilization, results showed OA-NO2 inhibits Ang II-induced IP3 production and calcium mobilization PMC4459031
Human platelets 10 nM-10 μM 10 minutes Zafirlukast inhibited platelet aggregation and fibrinogen binding with an IC50 of 1.66 μM PMC3570016

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice (C57BL/6 background) DEN-induced HCC model Intraperitoneal injection 25 μM (100 μl/mouse) Twice a week for 4 weeks To evaluate the therapeutic effect of the NOX1-specific inhibitor ML171 on DEN-induced HCC. Results showed that ML171 significantly reduced the number and size of HCC nodules and decreased the expression of inflammatory mediators. PMC6409207
Mice Nox2 knockout mice Ex vivo perfusion 5 μM 6 minutes Both Nox1 and Nox2 were required for collagen-mediated thrombus formation at arterial shear PMC3909778
Spontaneously hypertensive rats (SHR) Spontaneous hypertension model Oral 60 mg/kg/day Once daily for 4 weeks ML171 treatment had minor effects on the development of spontaneous hypertension, perivascular inflammation, or vascular fibrosis. PMC8316606

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.14mL

0.83mL

0.41mL

20.72mL

4.14mL

2.07mL

41.44mL

8.29mL

4.14mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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