(Rac)-Pinostrobin
(Rac)-Pinostrobin ((±)-Pinostrobin) is a dual agonist of TGR5 and PPARγ. (Rac)-Pinostrobin specifically activates TGR5 without acting on other endogenously expressed GPCRs. (Rac)-Pinostrobin exhibits moderate PPARγ activation activity. (Rac)-Pinostrobin possesses metabolic regulatory activity. (Rac)-Pinostrobin can be used in research related to obesity and type 2 diabetes.
For research use only. We do not sell to patients.
- CAS No.: 75291-74-6
- Formula: C16H14O4
- Molecular Weight:270.28
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
TGR5 |
PPARγ |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| J774.A1 | IC50 |
37.46 μM
Compound: 84
|
Antiinflammatory activity against mouse J774.A1 cells assessed as inhibition of LPS-stimulated TNF-alpha level by ELISA method
Antiinflammatory activity against mouse J774.A1 cells assessed as inhibition of LPS-stimulated TNF-alpha level by ELISA method
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[PMID: 37683361] |
| J774.A1 | IC50 |
19.63 μM
Compound: 84
|
Antiinflammatory activity against mouse J774.A1 cells assessed as inhibition of LPS-stimulated IL-1beta level by ELISA method
Antiinflammatory activity against mouse J774.A1 cells assessed as inhibition of LPS-stimulated IL-1beta level by ELISA method
|
[PMID: 37683361] |
| RAW264.7 | IC50 |
22 μM
Compound: 84
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Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of TNF-alpha production incubated for 18 hrs by ELISA analysis
Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of TNF-alpha production incubated for 18 hrs by ELISA analysis
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[PMID: 37683361] |
| RAW264.7 | IC50 |
40 μM
Compound: 84
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Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of IL-1beta level incubated for 18 hrs by ELISA analysis
Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of IL-1beta level incubated for 18 hrs by ELISA analysis
|
[PMID: 37683361] |
| RAW264.7 | IC50 |
23.51 μM
Compound: 84
|
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-stimulated TNF-alpha level by ELISA method
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-stimulated TNF-alpha level by ELISA method
|
[PMID: 37683361] |
| RAW264.7 | IC50 |
17.28 μM
Compound: 84
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Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-stimulated IL-1beta level by ELISA method
Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-stimulated IL-1beta level by ELISA method
|
[PMID: 37683361] |
In Vitro
(Rac)-Pinostrobin ((±)-Pinostrobin) (13-100 μM; up to 40 h) activates TGR5 in TGR5-expressing HepG2 cells, producing significant, dose-dependent activation across concentrations from 13 to 100 μM[1].
(Rac)-Pinostrobin (13-100 μM; up to 40 h) acts as a modest PPARγ activator in A9 cells, producing significant activation only at concentrations from 13 to 44 μM, with no detectable activity at higher concentrations[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 75291-74-6
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Molecular Weight 270.28
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Formula C16H14O4
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SMILES
O=C1C=2C(O)=CC(OC)=CC2OC(C=3C=CC=CC3)C1
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Synonyms
(±)-Pinostrobin
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Structure Classification
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(Rac)-Pinostrobin Related Classifications
HY-N2127A Related Classifications
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