Fulvestrant - ≥99%, high purity , Estrogen receptor antagonist, CAS No.129453-61-8, Estrogen receptor antagonist

Item Number
F125644
Grouped product items
SKUSizeAvailabilityPrice Qty
F125644-25mg
25mg
In stock
$124.90
F125644-100mg
100mg
In stock
$362.90
F125644-250mg
250mg
In stock
$725.90
F125644-1g
1g
In stock
$2,322.90

Estrogen receptor antagonist

Basic Description

SynonymsFaslodex(ICI 182,780) | FULVESTRANT [MI] | ICI 182,789 | Q27274130 | CAS-129453-61-8 | NCGC00164789-02 | NCGC00164789-04 | BI167222 | AS-13024 | CS-1267 | FULVESTRANT (EP MONOGRAPH) | FULVESTRANT [EMA EPAR] | ICI-182780 | P19940 | SCHEMBL8209 | (7R,8R,9S,
Specifications & PurityMoligand™, ≥99%
Biochemical and Physiological MechanismsICI 182,780 is a high affinity estrogen receptor antagonist (IC50 = 0.29 nM), devoid of any partial agonism in vitro and ICI 182,780 is also a high affinity agonist at the membrane estrogen receptor, GPR30.Estrogen receptor antagonist with no partial agon
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeAGONIST, ANTAGONIST
Mechanism of actionEstrogen receptor antagonist
NoteWherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour. Need more advice on solubility, usage and handling? Please visit our frequently asked questions (FAQ) page for more details.

Product Properties

ALogP9.2

Associated Targets(Human)

ESRRA Tchem Steroid hormone receptor ERR1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ESR1 Tclin Estrogen receptor (31 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ESR2 Tclin Estrogen receptor beta (8 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
EPHX2 Tchem Bifunctional epoxide hydrolase 2 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
PGR Tclin Progesterone receptor (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
GPER1 Tchem G-protein coupled estrogen receptor 1 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
ESR1 Tclin Estrogen receptor alpha (17718 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
NR3C1 Tclin Glucocorticoid receptor (14987 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PGR Tclin Progesterone receptor (8562 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRB2 Tclin Beta-2 adrenergic receptor (11824 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM2 Tclin Muscarinic acetylcholine receptor M2 (10671 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRB1 Tclin Beta-1 adrenergic receptor (6630 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR1A Tclin Serotonin 1a (5-HT1a) receptor (14969 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2A Tclin Alpha-2a adrenergic receptor (9450 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AR Tclin Androgen Receptor (11781 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM1 Tclin Muscarinic acetylcholine receptor M1 (12690 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD2 Tclin Dopamine D2 receptor (23596 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GABRA1 Tclin GABA receptor alpha-1 subunit (399 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
MAOA Tclin Monoamine oxidase A (11911 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CNR1 Tclin Cannabinoid CB1 receptor (20913 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD1 Tclin Dopamine D1 receptor (9720 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGS1 Tclin Cyclooxygenase-1 (9233 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A2 Tclin Norepinephrine transporter (10102 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH2 Tclin Histamine H2 receptor (5428 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2A Tclin Serotonin 2a (5-HT2a) receptor (14758 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2C Tclin Serotonin 2c (5-HT2c) receptor (11471 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AVPR2 Tclin Vasopressin V2 receptor (2912 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA1 Tclin Adenosine A1 receptor (17603 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AGTR1 Tclin Type-1 angiotensin II receptor (5176 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A4 Tclin Serotonin transporter (12625 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA1A Tclin Alpha-1a adrenergic receptor (8359 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PTGS2 Tclin Cyclooxygenase-2 (13999 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH1 Tclin Histamine H1 receptor (7573 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRM1 Tclin Mu opioid receptor (19785 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
DRD3 Tclin Dopamine D3 receptor (14368 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PPARG Tclin Peroxisome proliferator-activated receptor gamma (15191 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
AVPR1A Tclin Vasopressin V1a receptor (5412 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRD1 Tclin Delta opioid receptor (15096 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
OPRK1 Tclin Kappa opioid receptor (16155 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR3A Tclin Serotonin 3a (5-HT3a) receptor (3366 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC6A3 Tclin Dopamine transporter (10535 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
GRIN1 Tclin Glutamate (NMDA) receptor subunit zeta 1 (122 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
KCNH2 Tclin HERG (29587 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
PDE3A Tclin Phosphodiesterase 3A (3309 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ESR2 Tclin Estrogen receptor beta (9272 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SLC29A1 Tclin Equilibrative nucleoside transporter 1 (1711 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2B Tclin Alpha-2b adrenergic receptor (4412 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADRA2C Tclin Alpha-2c adrenergic receptor (4876 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
CHRM3 Tclin Muscarinic acetylcholine receptor M3 (7750 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HTR2B Tclin Serotonin 2b (5-HT2b) receptor (10323 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
EDNRA Tclin Endothelin receptor ET-A (5008 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA2A Tclin Adenosine A2a receptor (16305 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ADORA3 Tchem Adenosine A3 receptor (15931 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
BDKRB2 Tclin Bradykinin B2 receptor (3970 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ESRRA Tchem Estrogen-related receptor alpha (573 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
HRH3 Tclin Histamine H3 receptor (10389 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Npy1r Neuropeptide Y receptor type 1 (8 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Cckar Cholecystokinin A receptor (90 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Pde4d Phosphodiesterase 4D (4 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Galc Galactocerebrosidase (11 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Mus musculus (284745 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Rattus norvegicus (775804 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
COS-7 (515 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Ehrlich (1318 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Txnrd1 Thioredoxin reductase 1, cytoplasmic (45279 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
Nfe2l2 Nuclear factor erythroid 2-related factor 2 (214 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
ESR1 Estrogen receptor (4 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
bla Bacterial beta-lactamase TEM (177 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Mechanisms of Action

Mechanism of ActionAction Typetarget IDTarget NameTarget TypeTarget OrganismBinding Site NameReferences

Names and Identifiers

Pubchem Sid488187370
Pubchem Sid Urlhttps://pubchem.ncbi.nlm.nih.gov/substance/488187370
IUPAC Name (7R,8R,9S,13S,14S,17S)-13-methyl-7-[9-(4,4,5,5,5-pentafluoropentylsulfinyl)nonyl]-6,7,8,9,11,12,14,15,16,17-decahydrocyclopenta[a]phenanthrene-3,17-diol
INCHI InChI=1S/C32H47F5O3S/c1-30-17-15-26-25-12-11-24(38)21-23(25)20-22(29(26)27(30)13-14-28(30)39)10-7-5-3-2-4-6-8-18-41(40)19-9-16-31(33,34)32(35,36)37/h11-12,21-22,26-29,38-39H,2-10,13-20H2,1H3/t22-,26-,27+,28+,29-,30+,41?/m1/s1
InChi Key VWUXBMIQPBEWFH-WCCTWKNTSA-N
Canonical SMILES CC12CCC3C(C1CCC2O)C(CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F
Isomeric SMILES C[C@]12CC[C@H]3[C@H]([C@@H]1CC[C@@H]2O)[C@@H](CC4=C3C=CC(=C4)O)CCCCCCCCCS(=O)CCCC(C(F)(F)F)(F)F
WGK Germany 3
RTECS KG7623000
PubChem CID 104741
Molecular Weight 606.77

Certificates

Certificate of Analysis(COA)

Enter Lot Number to search for COA:

Find and download the COA for your product by matching the lot number on the packaging.

17 results found

Lot NumberCertificate TypeDateItem
B23091184Certificate of AnalysisNov 14, 2024 F125644
B2309974Certificate of AnalysisNov 06, 2024 F125644
B2309959Certificate of AnalysisNov 06, 2024 F125644
G2221124Certificate of AnalysisMay 22, 2024 F125644
L2305224Certificate of AnalysisNov 24, 2023 F125644
L2305220Certificate of AnalysisNov 24, 2023 F125644
G2315629Certificate of AnalysisJul 07, 2023 F125644
G2315632Certificate of AnalysisJul 07, 2023 F125644
G2315633Certificate of AnalysisJul 07, 2023 F125644
G2315635Certificate of AnalysisJul 07, 2023 F125644
G2315646Certificate of AnalysisJul 07, 2023 F125644
G1714045Certificate of AnalysisFeb 07, 2023 F125644
B2309978Certificate of AnalysisJan 04, 2023 F125644
B2309833Certificate of AnalysisJan 04, 2023 F125644
B23091015Certificate of AnalysisJan 04, 2023 F125644
G2221212Certificate of AnalysisJun 02, 2022 F125644
G2221213Certificate of AnalysisJun 02, 2022 F125644

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Chemical and Physical Properties

Solubility≥30.35 mg/mL in DMSO; insoluble in H2O; ≥58.9 mg/mL in EtOH
Melt Point(°C)104 - 112 °C

Safety and Hazards(GHS)

Pictogram(s) GHS08,   GHS09,   GHS07
Signal Danger
Hazard Statements

H319:Causes serious eye irritation

H373:Causes damage to organs through prolonged or repeated exposure

H413:May cause long lasting harmful effects to aquatic life

H302:Harmful if swallowed

H400:Very toxic to aquatic life

H410:Very toxic to aquatic life with long lasting effects

H360:May damage fertility or the unborn child

H362:May cause harm to breast-fed children

Precautionary Statements

P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.

P273:Avoid release to the environment.

P280:Wear protective gloves/protective clothing/eye protection/face protection.

P405:Store locked up.

P501:Dispose of contents/container to ...

P264:Wash hands [and …] thoroughly after handling.

P260:Do not breathe dust/fume/gas/mist/vapors/spray.

P270:Do not eat, drink or smoke when using this product.

P391:Collect spillage.

P330:Rinse mouth.

P263:Avoid contact during pregnancy/while nursing.

P203:Obtain, read and follow all safety instructions before use.

P264+P265:Wash hands [and …] thoroughly after handling. Do not touch eyes.

P301+P317:IF SWALLOWED: Get medical help.

P318:if exposed or concerned, get medical advice.

P337+P317:If eye irritation persists: Get medical help.

P319:Get medical help if you feel unwell.

WGK Germany 3
RTECS KG7623000

Related Documents

Citations of This Product

1. Hong Liu, Yang Huang, Jing Yang, Xuejiao Xu, Qiaomei Dai, Yuwei Zhang, Li Zhao, Mengdi Zhang, Jing Zhang, Tonghui Liu, Lili Zhong.  (2023)  Involvement of estrogen receptor activation in kaempferol-3-O-glucoside's protection against aging-related cognition impairment and microglial inflammation.  EXPERIMENTAL CELL RESEARCH,    (113849).  [PMID:37926343] [10.1016/j.yexcr.2023.113849]
2. Xiu Yanghui, Su Yu, Gao Lihua, Yuan Hui, Xu Sennan, Liu Ying, Qiu Yan, Liu Zhen, Li Yuhang.  (2023)  Corylin accelerated wound healing through SIRT1 and PI3K/AKT signaling: a candidate remedy for chronic non-healing wounds.  Frontiers in Pharmacology,  14    [PMID:37266148] [10.3389/fphar.2023.1153810]

References

1. Xu X et al..  (2019)  17ß-Estradiol nongenomically induces vascular endothelial H2S release by promoting phosphorylation of cystathionine ?-lyase..  J Biol Chem,  294  (43): (15577-15592).  [PMID:31439665]
2. Schennink A et al..  (2013)  A novel first exon directs hormone-sensitive transcription of the pig prolactin receptor..  J Mol Endocrinol,  51  (1-13).  [PMID:23576686]
3. Bao C et al..  (2022)  A novel oncogenic enhancer of estrogen receptor-positive breast cancer..  Mol Ther Nucleic Acids,  29  (836-851).  [PMID:36159594]
4. Keil KP et al..  (2017)  In vivo and in vitro sex differences in the dendritic morphology of developing murine hippocampal and cortical neurons..  Sci Rep,  (8486).  [PMID:28814778]
5. Xiao L et al..  (2014)  Induction of the CLOCK gene by E2-ERa signaling promotes the proliferation of breast cancer cells..  PLoS One,  (5): (e95878).  [PMID:24789043]
6. Xiao L et al..  (2019)  Profile of melatonin and its receptors and synthesizing enzymes in cumulus-oocyte complexes of the developing sheep antral follicle-a potential estradiol-mediated mechanism..  Reprod Biol Endocrinol,  17  (1).  [PMID:30606208]
7. Traboulsi T et al..  (2019)  Role of SUMOylation in differential ERa transcriptional repression by tamoxifen and fulvestrant in breast cancer cells..  Oncogene,  38  (7): (1019-1037).  [PMID:30190545]
8. Wang Z et al..  (2018)  The in vitro estrogenic activity of the crude drugs found in Japanese herbal medicines prescribed for menopausal syndrome was enhanced by combining them..  BMC Complement Altern Med,  18  (107).  [PMID:29566679]
9. Hong Liu, Yang Huang, Jing Yang, Xuejiao Xu, Qiaomei Dai, Yuwei Zhang, Li Zhao, Mengdi Zhang, Jing Zhang, Tonghui Liu, Lili Zhong.  (2023)  Involvement of estrogen receptor activation in kaempferol-3-O-glucoside's protection against aging-related cognition impairment and microglial inflammation.  EXPERIMENTAL CELL RESEARCH,    (113849).  [PMID:37926343] [10.1016/j.yexcr.2023.113849]
10. Xiu Yanghui, Su Yu, Gao Lihua, Yuan Hui, Xu Sennan, Liu Ying, Qiu Yan, Liu Zhen, Li Yuhang.  (2023)  Corylin accelerated wound healing through SIRT1 and PI3K/AKT signaling: a candidate remedy for chronic non-healing wounds.  Frontiers in Pharmacology,  14    [PMID:37266148] [10.3389/fphar.2023.1153810]

Solution Calculators