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GSK5182 - 98%, high purity , CAS No.877387-37-6, Antagonist of Estrogen receptor-α;Agonist of Estrogen-related receptor-γ

  • Moligand™
  • ≥98%
Item Number
G412950
Grouped product items
SKUSizeAvailabilityPrice Qty
G412950-5mg
5mg
In stock
$127.90
G412950-10mg
10mg
In stock
$187.90
G412950-25mg
25mg
In stock
$345.90
G412950-50mg
50mg
In stock
$523.90
G412950-100mg
100mg
In stock
$791.90

Estrogen/progestogen Receptor Agonists

Basic Description

Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsGSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeAGONIST, ANTAGONIST
Mechanism of actionAntagonist of Estrogen receptor-α;Agonist of Estrogen-related receptor-γ
Product Description

Information

GSK5182 GSK5182, 4-hydroxytamoxifen analog, is a specific inverse agonist of estrogen-related receptor γ (ERRγ) that inhibits pro-inflammatory cytokine-induced catabolic factors.


Targets

ERRγ

Product Properties

ALogP5.308
HBD Count2
Rotatable Bond10

Associated Targets

CYP1A2 Tchem Cytochrome P450 1A2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2D6 Tclin Cytochrome P450 2D6 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C19 Tchem Cytochrome P450 2C19 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP3A4 Tclin Cytochrome P450 3A4 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ESRRA Tchem Steroid hormone receptor ERR1 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ESRRB Tchem Steroid hormone receptor ERR2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ESRRG Tchem Estrogen-related receptor gamma 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

ESR1 Tclin Estrogen receptor 1 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

CYP2C9 Tchem Cytochrome P450 2C9 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

KCNH2 Tclin Potassium voltage-gated channel subfamily H member 2 0 Activities

Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)

Names and Identifiers

IUPAC Name 4-[(Z)-1-[4-[2-(dimethylamino)ethoxy]phenyl]-5-hydroxy-2-phenylpent-1-enyl]phenol
INCHI InChI=1S/C27H31NO3/c1-28(2)18-20-31-25-16-12-23(13-17-25)27(22-10-14-24(30)15-11-22)26(9-6-19-29)21-7-4-3-5-8-21/h3-5,7-8,10-17,29-30H,6,9,18-20H2,1-2H3/b27-26-
InChi Key ZVSFNBNLNLXEFQ-RQZHXJHFSA-N
Canonical SMILES CN(C)CCOC1=CC=C(C=C1)C(=C(CCCO)C2=CC=CC=C2)C3=CC=C(C=C3)O
Isomeric SMILES CN(C)CCOC1=CC=C(C=C1)/C(=C(/CCCO)\C2=CC=CC=C2)/C3=CC=C(C=C3)O
PubChem CID 6852176
MeSH Entry Terms GSK5182
Molecular Weight 417.54

Certificates

Certificate of Analysis(COA)

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10 results found

Lot NumberCertificate TypeDateItem
G2313699Certificate of AnalysisJun 15, 2023 G412950
G2313701Certificate of AnalysisJun 15, 2023 G412950
G2313704Certificate of AnalysisJun 15, 2023 G412950
G2313706Certificate of AnalysisJun 15, 2023 G412950
G2313719Certificate of AnalysisJun 15, 2023 G412950
G2313720Certificate of AnalysisJun 15, 2023 G412950
G2313721Certificate of AnalysisJun 15, 2023 G412950
G2313724Certificate of AnalysisJun 15, 2023 G412950
G2313732Certificate of AnalysisJun 15, 2023 G412950
G2313736Certificate of AnalysisJun 15, 2023 G412950

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 84 mg/mL (201.17 mM); Ethanol: 84 mg/mL (201.17 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility84
DMSO(mM) Max Solubility201.178330219859
Water(mg / mL) Max Solubility<1

Related Documents

References

1. Kim DK, Gang GT, Ryu D, Koh M, Kim YN, Kim SS, Park J, Kim YH, Sim T, Lee IK et al..  (2013)  Inverse agonist of nuclear receptor ERRγ mediates antidiabetic effect through inhibition of hepatic gluconeogenesis..  Diabetes,  62  (9): (3093-102).  [PMID:23775767]

Solution Calculators