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Androgen Receptor agonist
Andarine (GTX-007) is an investigational selective androgen receptor modulator (SARM). -
Glucocorticoid Receptor Agonist
Betamethasone dipropionate is a glucocorticoid steroid with anti-inflammatory and immunosuppressive abilities. -
GPR119 agonist
GSK-1292263 is a novel GPR119 agonist.- Inoue A, .et al. , Cell, 2019, Jun 13;177(7):1933-1947 PMID: 31160049
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ERRα and ERRγ inverse agonist
Kaempferol is found to inhibit bovine aorta myosin light chain kinase with a Ki of 0.3-0.5 microM and also is found to inhibit VEGF expression and in vitro angiogenesis through a novel ERK-NFκB-cMyc-p21 pathway.- A O Hamouda, .et al. , Eur Rev Med Pharmacol Sci, 2022, Dec;26(23):8644-8659 PMID: 36524484
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synthetic glucocorticoid receptor agonist
Methylprednisolone is an apoptosis inducer and was also found to inhibit human small cell lung cancer cell growth in vitro. -
Glucocorticoid Receptor agonist
Prednisone reduces mucosal TNF-a production, intestinal permeability and levels of NF-kB expression. -
Glucocorticoid receptor agonist
Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist. -
progesterone receptor agonist
Medroxyprogesterone acetate is a progestin, a synthetic variant of the human hormone progesterone and a potent progesterone receptor agonist.- Xijian Wang, .et al. , 3 Biotech, 2020, Sep;10(9):377 PMID: 32802719
- Xiucui Bao, .et al. , J Anal Methods Chem, 2019, Article ID 5676159
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estrogen agonist
Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist. -
CB2 inverse agonist
SR 144528 is a selective peripheral cannabinoid receptor inverse agonist that displays a Ki value of 0.6 nM for rat spleen and human recombinant CB2 receptors and a Ki value of 400 nM for rat brain and human recombinant CB1 receptors.- Ming Tang, .et al. , Cell Death Dis, 2018, Jun; 9(6): 601 PMID: 29789558
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ERα agonist
Propyl pyrazole triol (PPT) is an estrogen receptor alpha (ERα) agonist. -
GPR3 agonist/NOS/ NADPH oxidases inhibitor
Diphenyleneiodonium chloride has been shown to be a potent irreversible inhibitor of NOS2 (iNOS) from macrophages and NOS3 (eNOS) from endothelial cells. -
GnRH agonist
Leuprolide acetate is a GnRH analog; leuprolide acetate acts as an agonist at pituitary GnRH receptors. -
TRβ agonist
Sobetirome is a thyroid hormone receptor β (TRβ)-specific agonist, Sobetirome is designed to bind selectively to TRβ-1 with EC50 of 0.16 μM. -
Progesterone receptor agonist
Tanaproget is a novel nonsteroidal progesterone receptor agonist which can bind to the PR from various species with a higher relative affinity than reference steroidal progestins. -
GPR139 agonist
JNJ 63533054 is a potent and selective GPR139 agonist with EC50 value of 16nm. -
GPR119 agonist
APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119. -
GnRH agonist
Goserelin is a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH) with antineoplastic activity. -
GnRH agonist
Triptorelin is a gonadotropin-releasing hormone agonist (GnRH agonist) used as the acetate or pamoate salts. -
GPR39 agonist
TC-G-1008 is a GPR39 (zinc receptor) agonist (EC50 values are 0.4 and 0.8 nM for rat and human receptors respectively).- Urszula Doboszewska, .et al. , Cell Mol Life Sci, 2023, Apr 25;80(5):133 PMID: 37185787
- Urszula Doboszewska, .et al. , Cells, 2023, Jan 9;12(2):264 PMID: 36672199
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glucocorticoid receptor agonist
Dexamethasone acetate (Dexamethasone 21-acetate) is a glucocorticoid receptor agonist. -
RORγ agonist
LYC-55716 is novel oral RAR-related orphan receptor γ (RORγ) agonist. -
ERRβ & ERRγ Agonist
GSK4716 is an Estrogen-related receptors ERRβ and ERRγ agonist with minimal activity for ERRα, ERα and ERβ- Sen He, .et al. , Toxicology, 2021, May 4;457:152805 PMID: 33961950
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synthetic glucocorticoid receptor agonist
Methylprednisolone succinate is a synthetic glucocorticoid and widely used as an anti-inflammatory agent. -
Estrogen receptor agonist
(R)-Equol is an agonist of both ERα and ERβ with Kis of 27.4 and 15.4 nM, respectively.- Gao X, .et al. , Toxins (Basel), 2020, Jan 26;12(2) PMID: 31991913
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FAA1 agonist
FAA1 agonist-1 is a potent free fatty acid receptor 1 (FFA1/ GPR40) agonist with a pEC50 of 7.54. -
glucocorticoid receptor agonist
Dexamethasone Phosphate disodium is a is a water-soluble form of the synthetic glucocorticoid dexamethasone. -
glucocorticoid agonist
Beclometasone dipropionate is a potent glucocorticoid agonist; it is a prodrug of the free form, beclometasone. -
GnRH/LHRH receptor agonist
Leuprorelin is a Gonadotropin-releasing hormone (GnRH, luteinizing hormone-releasing hormone, LHRH) receptor agonist. Suppresses estradiol, LH and FSH serum levels and represses the growth of experimental rat endometriosis. -
GnRH agonist
Nafarelin is a gonadotropin-releasing hormone agonist (GnRH agonist) which acts as an analog of GnRH. -
glucocorticoid receptor agonist
Beclometasone, also known as Beclomethasone, is an anti-inflammatory, synthetic glucocorticoid. It is used topically as an anti-inflammatory agent and in aerosol form for the treatment of asthma. -
gonadotropin-releasing hormone agonist
Buserelin Acetate is a gonadotropin-releasing hormone agonist (GnRH agonist). -
TRH-R agonist
Taltirelin (TA0910) is a superagonist at thyrotropin-releasing hormone receptor (TRH-R) with an IC50 of 910 nM and EC50 of 36 nM for stimulating an increase in cytosolic Ca2+ concentration (Ca2+ release).