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Scutellarin STAT inhibitor

Name: Scutellarin
Brand: Selleck Chemicals
SKU: S3810
Availability: InStock
Rating: 5 (1 reviews)

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.

Chemical Structure

Molecular Weight: 462.36

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Quality Control

Batch: Purity: 99.35%

99.35

Related Targets	EGFR JAK Pim
Other STAT Inhibitors	Napabucasin (BBI608) Stattic NSC 74859 (S3I-201) Cryptotanshinone (Tanshinone C) C188-9 (TTI-101) SH-4-54 BP-1-102 AS1517499 Nifuroxazide HO-3867

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.670mg/ml (3.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 33.3 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	462.36	Formula	C₂₁H₁₈O₁₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	27740-01-8	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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

Mechanism of Action

Targets/IC₅₀/Ki	STAT3 Akt NF-κB
In vitro	Scutellarin protects PC12 cells against H2O2-induced cytotoxicity. It attenuates H2O2-induced intracellular accumulation of ROS and lipid peroxidation. 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. 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.
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 %). 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16250252/ [2] https://pubmed.ncbi.nlm.nih.gov/24423938/ [3] https://pubmed.ncbi.nlm.nih.gov/16931419/ [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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