1. Metabolic Enzyme/Protease
  2. 11β-HSD
  3. Methyl glycyrrhetinate

Methyl glycyrrhetinate, a 18β-glycyrrhetinic acid analogue, is a dual inhibitor of 11β-HSD1 and 11β-HSD2.

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Methyl glycyrrhetinate

Methyl glycyrrhetinate Chemical Structure

CAS No. : 1477-44-7

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Description

Methyl glycyrrhetinate, a 18β-glycyrrhetinic acid analogue, is a dual inhibitor of 11β-HSD1 and 11β-HSD2[1].

Cellular Effect
Cell Line Type Value Description References
518A2 EC50
>30 μM
Compound: 5
Cytotoxicity against human 518A2 cells assessed as cell survival after 96 hrs by SRB assay
Cytotoxicity against human 518A2 cells assessed as cell survival after 96 hrs by SRB assay
[PMID: 26177446]
518A2 EC50
30 μM
Compound: 5
Cytotoxicity against human 518A2 cells assessed as cell survival after 96 hrs by SRB assay
Cytotoxicity against human 518A2 cells assessed as cell survival after 96 hrs by SRB assay
[PMID: 26177446]
518A2 IC50
27.54 μM
Compound: 1
Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay
Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay
[PMID: 20932766]
518A2 IC50
27.54 μM
Compound: GA-Me
Cytotoxicity against human 518A2 cells by SRB assay
Cytotoxicity against human 518A2 cells by SRB assay
[PMID: 24361520]
518A2 IC50
27.54 μmol
Compound: 1
Cytotoxicity against human 518A2 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human 518A2 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
8505C EC50
>30 μM
Compound: 5
Cytotoxicity against human 8505C cells assessed as cell survival after 96 hrs by SRB assay
Cytotoxicity against human 8505C cells assessed as cell survival after 96 hrs by SRB assay
[PMID: 26177446]
8505C IC50
26.07 μM
Compound: 1
Cytotoxicity against human 8505C cells after 96 hrs by SRB assay
Cytotoxicity against human 8505C cells after 96 hrs by SRB assay
[PMID: 20932766]
8505C IC50
26.07 μM
Compound: GA-Me
Cytotoxicity against human 8505C cells by SRB assay
Cytotoxicity against human 8505C cells by SRB assay
[PMID: 24361520]
8505C IC50
26.07 μmol
Compound: 1
Cytotoxicity against human 8505C cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human 8505C cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
A253 cell line IC50
19.42 μM
Compound: 1
Cytotoxicity against human A253 cells after 96 hrs by SRB assay
Cytotoxicity against human A253 cells after 96 hrs by SRB assay
[PMID: 20932766]
A253 cell line IC50
19.42 μM
Compound: GA-Me
Cytotoxicity against human A253 cells by SRB assay
Cytotoxicity against human A253 cells by SRB assay
[PMID: 24361520]
A253 cell line IC50
19.42 μmol
Compound: 1
Cytotoxicity against human A253 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human A253 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
A2780 IC50
25.54 μM
Compound: 1
Cytotoxicity against human A2780 cells after 96 hrs by SRB assay
Cytotoxicity against human A2780 cells after 96 hrs by SRB assay
[PMID: 20932766]
A2780 IC50
25.54 μmol
Compound: 1
Cytotoxicity against human A2780 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human A2780 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
A-431 IC50
25.28 μM
Compound: 1
Cytotoxicity against human A431 cells after 96 hrs by SRB assay
Cytotoxicity against human A431 cells after 96 hrs by SRB assay
[PMID: 20932766]
A549 EC50
>30 μM
Compound: 5
Cytotoxicity against human A549 cells assessed as cell survival after 96 hrs by SRB assay
Cytotoxicity against human A549 cells assessed as cell survival after 96 hrs by SRB assay
[PMID: 26177446]
A549 IC50
>100 μM
Compound: GA-1
Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human A549 cells after 48 hrs by CCK-8 assay
[PMID: 26343825]
A549 IC50
23.5 μM
Compound: 1
Cytotoxicity against human A549 cells after 96 hrs by SRB assay
Cytotoxicity against human A549 cells after 96 hrs by SRB assay
[PMID: 20932766]
A549 IC50
23.5 μmol
Compound: 1
Cytotoxicity against human A549 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human A549 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
DLD-1 IC50
26.12 μM
Compound: 1
Cytotoxicity against human DLD1 cells after 96 hrs by SRB assay
Cytotoxicity against human DLD1 cells after 96 hrs by SRB assay
[PMID: 20932766]
DLD-1 IC50
26.12 μM
Compound: GA-Me
Cytotoxicity against human DLD1 cells by SRB assay
Cytotoxicity against human DLD1 cells by SRB assay
[PMID: 24361520]
DLD-1 IC50
26.12 μmol
Compound: 1
Cytotoxicity against human DLD1 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human DLD1 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
FaDu IC50
23.41 μM
Compound: 1
Cytotoxicity against human FADU cells after 96 hrs by SRB assay
Cytotoxicity against human FADU cells after 96 hrs by SRB assay
[PMID: 20932766]
FaDu IC50
23.41 μmol
Compound: 1
Cytotoxicity against human FADU cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human FADU cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
HCT-116 IC50
22.1 μM
Compound: 1
Cytotoxicity against human HCT116 cells after 96 hrs by SRB assay
Cytotoxicity against human HCT116 cells after 96 hrs by SRB assay
[PMID: 20932766]
HCT-116 IC50
22.1 μmol
Compound: 1
Cytotoxicity against human HCT116 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human HCT116 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
HCT-8 IC50
24.36 μM
Compound: 1
Cytotoxicity against human HCT8 cells after 96 hrs by SRB assay
Cytotoxicity against human HCT8 cells after 96 hrs by SRB assay
[PMID: 20932766]
HCT-8 IC50
24.36 μmol
Compound: 1
Cytotoxicity against human HCT8 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human HCT8 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
HeLa IC50
>100 μM
Compound: GA-1
Antiproliferative activity against human HeLa cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human HeLa cells after 48 hrs by CCK-8 assay
[PMID: 26343825]
HepG2 2.2.15 CC50
>1744.29 μM
Compound: 6
Cytotoxicity against human HepG2(2.2.15) cells
Cytotoxicity against human HepG2(2.2.15) cells
[PMID: 22520261]
HepG2 2.2.15 IC50
>1744.29 μM
Compound: 6
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction in hepatitis B e-antigen release
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction in hepatitis B e-antigen release
[PMID: 22520261]
HepG2 2.2.15 IC50
>443.57 μM
Compound: 6
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction in viral DNA replication
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as reduction in viral DNA replication
[PMID: 22520261]
HT-29 EC50
>30 μM
Compound: 5
Cytotoxicity against human HT-29 cells assessed as cell survival after 96 hrs by SRB assay
Cytotoxicity against human HT-29 cells assessed as cell survival after 96 hrs by SRB assay
[PMID: 26177446]
HT-29 IC50
27.54 μM
Compound: 1
Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay
Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay
[PMID: 20932766]
HT-29 IC50
27.54 μmol
Compound: 1
Cytotoxicity against human HT-29 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human HT-29 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
J774 IC50
>100 μM
Compound: 14
Antiinflammatory activity in mouse J774 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method
Antiinflammatory activity in mouse J774 cells assessed as inhibition of LPS-induced NO production after 24 hrs by Griess method
[PMID: 24268542]
KB 3-1 IC50
>100 μM
Compound: 14
Cytotoxicity against human KB-3-1 cells assessed as cell survival after 24 hrs by MTT assay
Cytotoxicity against human KB-3-1 cells assessed as cell survival after 24 hrs by MTT assay
[PMID: 24268542]
MCF7 EC50
>30 μM
Compound: 5
Cytotoxicity against human MCF7 cells assessed as cell survival after 96 hrs by SRB assay
Cytotoxicity against human MCF7 cells assessed as cell survival after 96 hrs by SRB assay
[PMID: 26177446]
MCF7 IC50
>100 μM
Compound: GA-1
Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
Antiproliferative activity against human MCF7 cells after 48 hrs by CCK-8 assay
[PMID: 26343825]
MCF7 IC50
22.14 μM
Compound: 1
Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay
Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay
[PMID: 20932766]
MCF7 IC50
22.14 μM
Compound: GA-Me
Cytotoxicity against human MCF7 cells by SRB assay
Cytotoxicity against human MCF7 cells by SRB assay
[PMID: 24361520]
MCF7 IC50
22.14 μmol
Compound: 1
Cytotoxicity against human MCF7 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human MCF7 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
NIH3T3 IC50
22.81 μM
Compound: 1
Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay
Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay
[PMID: 20932766]
NIH3T3 IC50
22.81 μM
Compound: GA-Me
Cytotoxicity against mouse NIH/3T3 cells by SRB assay
Cytotoxicity against mouse NIH/3T3 cells by SRB assay
[PMID: 24361520]
SW-1736 IC50
34.87 μM
Compound: 1
Cytotoxicity against human SW1736 cells after 96 hrs by SRB assay
Cytotoxicity against human SW1736 cells after 96 hrs by SRB assay
[PMID: 20932766]
SW-1736 IC50
34.87 μM
Compound: GA-Me
Cytotoxicity against human SW1736 cells by SRB assay
Cytotoxicity against human SW1736 cells by SRB assay
[PMID: 24361520]
SW-1736 IC50
34.87 μmol
Compound: 1
Cytotoxicity against human SW1736 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human SW1736 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
SW480 IC50
16.08 μM
Compound: 1
Cytotoxicity against human SW480 cells after 96 hrs by SRB assay
Cytotoxicity against human SW480 cells after 96 hrs by SRB assay
[PMID: 20932766]
SW480 IC50
16.08 μmol
Compound: 1
Cytotoxicity against human SW480 cells after 96 hrs by sulforhodamine B assay
Cytotoxicity against human SW480 cells after 96 hrs by sulforhodamine B assay
[PMID: 20884085]
In Vitro

Methyl glycyrrhetinate (compound 34) (10 μM) inhibits rat liver microsomal 11β-HSD1 and rat kidney microsomal 11β-HSD2, with 85% and 105% inhibition respectively at 10 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

484.71

Formula

C31H48O4

CAS No.
SMILES

C[C@@]1(CC[C@]2([C@@]([H])(C1)C([C@]3(CC2)C)=CC([C@]4([C@]3(CC[C@@]5([C@@]4(CC[C@@H](C5(C)C)O)C)[H])C)[H])=O)C)C(OC)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Methyl glycyrrhetinate Related Classifications

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Methyl glycyrrhetinate
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