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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
Vascular smooth muscle cells (VSMC) 0.5 μM 30 minutes To evaluate the effect of ML171 on vascular contractile responses, results showed ML171 reduced AngII-induced vascular contraction Br J Pharmacol. 2015 Jun;172(12):3159-76.
Human platelets 10 nM-10 μM 10 minutes To assess the effect of 2-APT on superoxide ion generation in platelets. Results showed that 2-APT significantly inhibited collagen- and fibrinogen-dependent superoxide ion generation with IC50 values of 306 nM and 227 nM, respectively. Br J Pharmacol. 2013 Jan;168(1):212-24.
Human platelets 5 μM ML171 significantly suppressed ROS and TxA2 production from GPVI-activated human platelets Redox Biol. 2014 Jan 13;2:178-86.
Mouse platelets 5 μM 2 minutes ML171 significantly suppressed CRP-induced ROS production without significantly affecting platelet aggregation or αIIbβ3 activation Redox Biol. 2014 Jan 13;2:178-86.
Vascular smooth muscle cells (VSMCs) 10 μM 24 hours ML171 (a NOX1 inhibitor) inhibited VSMCs migration and proliferation in SHR, similar to the effects of RND3 overexpression. Redox Biol. 2021 Dec 6;48:102204.
HCT116 cells 10 μM 48 hours ML171, as a NOX1 inhibitor, was used to investigate the source of ROS induced by p20BAP31. Results showed that ML171 had a minor effect on p20BAP31-induced ROS production, while the NOX2 inhibitor apocynin significantly attenuated ROS production. Cell Mol Biol Lett. 2023 Mar 28;28(1):25.
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. Cell Death Dis. 2015 Apr 16;6(4):e1728.

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. Gastroenterology. 2019 Mar;156(4):1156-1172.e6
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 Redox Biol. 2014 Jan 13;2:178-86.
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. Pharmacol Res. 2020 Nov;161:105235

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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