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Scutellarin STAT inhibitor

Cat.No.S3810

Scutellarin (Breviscapine, Breviscapin, Scutellarein-7-glucuronide), the major active principal flavonoids extracted from the Chinese herbal medicines Scutellaria baicalensis and Erigeron breviscapus (Vant.) Hand-Mazz, has many pharmacological effects, such as antioxidant, antitumor, antiviral, and antiinflammatory activities. This compound can down-regulates the STAT3/Girdin/Akt signaling in HCC cells, and inhibits RANKL-mediated MAPK and NF-κB signaling pathway in osteoclasts.
Scutellarin STAT inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 462.36

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 462.36 Formula

C21H18O12

Storage (From the date of receipt)
CAS No. 27740-01-8 Download SDF Storage of Stock Solutions

Synonyms Breviscapine, Breviscapin, Scutellarein-7-glucuronide Smiles C1=CC(=CC=C1C2=CC(=O)C3=C(C(=C(C=C3O2)OC4C(C(C(C(O4)C(=O)O)O)O)O)O)O)O

Solubility

In vitro
Batch:

DMSO : 50 mg/mL (108.14 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 2 mg/mL

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Mass Concentration Volume Molecular Weight

In vivo
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Mechanism of Action

Targets/IC50/Ki
STAT3 [6]
Akt [6]
NF-κB [7]
In vitro

Scutellarin protects PC12 cells against H2O2-induced cytotoxicity. It attenuates H2O2-induced intracellular accumulation of ROS and lipid peroxidation[3]. This compound shows negligible inhibitory effects on the six major CYP isoenzymes in human/rat liver microsomes with almost all of the IC50 values exceeding 100 μM, whereas it shows values of 63.8 μM for CYP2C19 in human liver microsomes, and 63.1 and 85.6 μM for CYP2C7 and CYP2C79 in rat liver microsomes, respectively. It also has weak inhibitory effect on P-gp[4]. This chemical strongly induces MMP-2 activation and mRNA expression in cultured HUVECs in a concentration-dependent manner. It promotes angiogenesis and may form a basis for angiogenic therapy[5].

In vivo

The pharmacokinetic results indicate that scutellarin undergoes rapid and extensive biotransformation in vivo. After intraperitoneal injection. this compound is absorbed rapidly. The relative bioavailability of oral administration is very low (10.67 %±4.78 %)[1]. It has a series of protective effects including dilate blood vessels, improving microcirculation, decreasing the viscosity of blood, reducing the blood platelet count, inhibiting platelet aggregation activity etc[2].

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/24802986/
  • [5] https://pubmed.ncbi.nlm.nih.gov/20709020/
  • [6] https://pubmed.ncbi.nlm.nih.gov/27998773/
  • [7] https://pubmed.ncbi.nlm.nih.gov/27728897/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02559960 Suspended
Adverse Drug Event|Adverse Drug Reaction|Chinese Medicine|Anaphylactic Reaction
Zhong Wang|China Academy of Chinese Medical Sciences
September 2015 --

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