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Nuclear Receptors

The list of compounds below either mimic or block the activity of endogenous ligands of nuclear receptors.  Broadly, nuclear receptors can be grouped into steroid and non-steroid hormone receptors that are regulated by endogenous agonists. Thirdly, nuclear receptors  with unknown ligand and mode of action are known as orphan receptors. Ligand-bound nuclear receptors undergo conformational changes and act as transcription factors. These bind to DNA response elements in promoters of target genes to regulate transcription. These compounds have therapeutic potential in reproductive, metabolic and proliferative diseases.

Code Cas No Product Description
BA164136 55079-83-9

Acitretin

Retinoid;activates nuclear retinoid acid receptor; antineoplastic; anti-psoratic
BA164138 106685-40-9

Adapalene

Agonist of retinoic acid receptors (RAR-β and RAR-γ); pro-apoptotic
FD17242 171746-21-7

AGN 193109

Pan-retinoic acid receptor (RAR) antagonist
FA137469 102121-60-8

AM 580

Retinoic acid receptor (RARα) agonist; induces cell differentiation
FA64943 956104-40-8

ARN 509

Androgen receptor antagonist; prostate cancer treatment
FA103981 1240299-33-5

AZD 3514

Androgen receptor antagonist; has therapeutic application in prostate cancer
BZ162710 42422-68-4

Beta-Zearalanol

Estrogen receptor agonist
BZ162711 71030-11-0

Beta-Zearalenol

Estrogen receptor agonist; macrolide
BB164246 153559-49-0

Bexarotene

Retinoid X receptor agonist; antineoplastic
BB166159 41859-67-0

Bezafibrate

Peroxisome proliferator-activated receptor agonist; hypolipidemic drug
FB18583 113299-38-0

(S)-Bicalutamide

Androgen receptor antagonist; anti-cancer agent
FB18582 113299-40-4

(R)-Bicalutamide

Androgen receptor antagonist; anti-cancer agent
BB166739 627530-84-1

BMS 564929

Androgen receptor modulator
BB164267 51333-22-3

Budesonide

Glucocorticoid receptor agonist; anti-inflammatory
FC09794 32222-06-3

Calcitriol

Vitamin D3 analog, regulates calcium and bone growth
FC166171 976-71-6

Canrenone - 97%

Mineralocorticoid (aldosterone) receptor antagonist
FC19935 302-22-7

Chlormadinone acetate

Progesterone receptor agonist; androgen receptor antagonist; oral contraceptive
FC20428 126544-47-6

Ciclesonide

Glucocorticoid; anti-inflammatory; anti-asthmatic agent
BD164311 52214-84-3

Ciprofibrate

Agonist of peroxisome proliferator-activated receptor PPARα ; hypolipidemic
FC20501 50-41-9

Clomiphene citrate (cis-trans mixture)

Estrogen receptor modulator; used to treat infertility
FC20764 427-51-0

Cyproterone acetate

Androgen receptor antagonist; apoptotic in hepatic cells
FD64992 1110813-31-4

Dacomitinib

Pan-EGFR inhibitor (HER1, HER2 and HER4); antineoplastic
FD156781 17230-88-5

Danazol

Anti-gonadotropin; therapy for endometriosis
FD161413 1297538-32-9

Darolutamide

Androgen receptor antagonist; therapy for endometriosis
BD162804 1361504-77-9

DG 172 2HCl

Agonist of peroxisome proliferator-activated receptors PPARβ/δ 
FB66440 1428-67-7

DPN

Estrogen ERβ receptor agonist; regulates GluR1, GluR2 and GluR3 expression
FD22620 67392-87-4

Drospirenone

Progestogen; anti-androgen; anti-mineralocorticoid
BD166530 67392-87-4

Drospirenone

Progestogen; anti-androgen; anti-mineralocorticoid
BE163306 923978-27-2

Elafibranor

Dual agonist of PPARα and PPARδ receptors
FE15969 112093-28-4

Endoxifen

Estrogen receptor antagonist; tamoxifen metabolite; breast cancer therapy
FC65076 915087-33-1

Enzalutamide

Androgen receptor antagonist
BE164415 107724-20-9

Eplerenone

Aldosterone blocker
FE22865 434-03-7

Ethisterone

Progesterone receptor agonist
FE23206 54350-48-0

Etretinate

Used to treat psoriasis; teratogenic
FF23253 49562-28-9

Fenofibrate

PPARα agonist; hypolipidemic agent
FF23268 65646-68-6

Fenretinide

Modulator of RBP protein; activator of sphingomyelinase; pro-apoptotic
FF15770 67-73-2

Fluocinolone acetonide

Corticosteroid; anti-inflammatory; treats dermatological conditions
BF166239 13311-84-7

Flutamide

Non-steroidal androgen receptor antagonist
FF23515 80474-14-2

Fluticasone propionate

Glucocorticoid receptor agonist; anti-inflammatory
BF160362 80474-14-2

Fluticasone propionate - micronised pharma grade

Glucocorticoid receptor agonist; anti-inflammatory
BF161262 80474-14-2

Fluticasone propionate - pharma grade

Glucocorticoid receptor agonist; anti-inflammatory
FT65187 851983-85-2

Galeterone

CYP17 lyase inhibitor; androgen receptor antagonist
FG137678 1365888-06-7

GDC 0810

Estrogen receptor degrader; therapeutic use in breast cancer
BG166429 1642297-01-5

GDC 0927

Degrader of estrogen receptor
BG164505 60282-87-3

Gestodene

Synthetic progestin; contraceptive
FG137681 1346572-63-1

GSK 503

Inhibits EZH2 methyltransferase; antineoplastic
FG23723 317318-84-6

GW 0742

Peroxisome proliferator-activated receptor PPARβ/δ agonist
FG23720 278779-30-9

GW 4064

Farnesoid X receptor agonist
FM23721 317318-70-0

GW 501516

PPAR β/δ agonist; modulates lipid catabolism; anti-obesity agent
FC20132 22978-25-2

GW 9962

PPARγ antagonist
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