Catalog No.
Product Name
Application
Product Information
Citations
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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 PMID: 31827972
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GPR agonist
TAK-875 is a potent, selective, and orally bioavailable GPR40 agonist.- Ying Liu, .et al. , Nucleic Acids Res, 2018, Oct 12; 46(18): 9864-9874 PMID: 30219861
- Deborah A. Goldspink, .et al. , Mol Metab, 2018, Jan; 7: 90-101 PMID: 29167062
- Hodaka Yamada, .et al. , Sci Rep, 2016, 6: 25912 PMID: 27180622
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Aromatase inhibitor
Fulvestrant is an estrogen receptor antagonist with no agonist effects, which works both by down-regulating and by degrading the estrogen receptor.- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Samy A. F. Morad, .et al. , Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Kaneyasu Nishimura, .et al. , Stem Cell Reports, 2016, Apr 12; 6(4): 511-524 PMID: 26997644
- Alejandro S. Cazzulino, .et al. , Hippocampus, 2016, Jun; 26(6): 752-762 PMID: 26662713
- Rie Mukai, .et al. , Am J Physiol Regul Integr Comp Physiol, 2016, Dec 1;311(6):R1022-R1031 PMID: 27629889
- Sakanashi M, .et al. , Circ J. , 2013, 77(7):1827-37. PMID: 23615023
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Estrogen receptor antagonist
(E/Z)-4-hydroxy Tamoxifen is the active metabolite of tamoxifen and a selective estrogen receptor (ER) modulator that is widely used in the therapeutic and chemopreventive treatment of breast cancer.- Yuanqin Zhang, .et al. , Cancers (Basel), 2023, Dec 2;15(23):5691 PMID: 38067394
- Takashi Azuma, .et al. , SEP PURIF TECHNOL, 2019, Apr; 212: 483-489
- Azuma T, .et al. , Environ Sci Pollut Res Int, 2017, Aug;24(23):19021-19030 PMID: 28660504
- Azuma T, .et al. , Sci Total Environ, 2016, Apr 1;548-549:189-197 PMID: 26802347
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human AR (hAR) antagonist
ORM-15341 is a potent and full antagonist for human AR (hAR) with IC50 values of 38 nM as shown by transactivation assays in AR-HEK293 cells stably expressing full-length hAR and an androgen-responsive luciferase reporter gene construct. -
GPR4 antagonist
GPR4 antagonist 1 is a GPR4 antagonist, with an IC50 of 189 nM. -
GPR35/CXCR8 agonist
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability. -
androgen receptor modulator
GSK-2881078 is a selective androgen receptor modulator (SARM) that is being evaluated for effects on muscle growth and strength in subjects with muscle wasting to improve their physical function. - Human parathyroid hormone (hPTH) peptide fragment; contains the 34 N-terminal residues of hPTH. Agonist at parathyroid 1 (PTH1) and parathyroid 2 (PTH2) receptors.
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GnRH antagonist
Degarelix acetate is a gonadotropin releasing hormone (GnRH) receptor antagonist. - Ganirelix is an injectable competitive gonadotropin-releasing hormone antagonist (GnRH antagonist)
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Apelin Receptor activator
(Glp1)-Apelin-13 is an activator of Apelin Receptor -
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. -
AT1 receptor antagonist
Eprosartan is an angiotensin II receptor antagonist used for the treatment of high blood pressure. -
HMG-CoA reductase inhibitor
Rosuvastatin is a member of the drug class of statins, used to treat high cholesterol and related conditions, and to prevent cardiovascular disease. -
renin inhibitor
Aliskiren hemifumarate is a hemifumarate salt form of Aliskiren, which is a direct renin inhibitor approved for the treatment of essential hypertension. -
CYP17 inhibitor
TOK-001 (Galeterone) is both an androgen receptor antagonist and CYP17A1 inhibitor. -
HMG-CoA Reductase inhibitor
Clinofibrate is a lipid clearing agent that appears to modify lipid metabolism, diminishing the steroid induced accumulation of lipids within osteocytes. It also can effectively reduce the plasma fibrinogen level.
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ACE inhibitor/Beta blocker
Moxonidine is a new-generation centrally-acting antihypertensive drug. It may have a role when thiazides, beta-blockers, ACE inhibitors and calcium channel blockers are not appropriate or have failed to control blood pressure. In addition, it demonstrates favourable effects on parameters of the insulin resistance syndrome, apparently independent of blood pressure reduction. - Calcifediol-D6 is the deuterated form of Calcifediol(25-hydroxy Vitamin D3), which is a prehormone that is produced in the liver by hydroxylation of vitamin D3 (cholecalciferol) by the enzyme cholecalciferol 25-hydroxylase.
- Calcitriol D6 is the deuterated form of Calcitriol(1,25-Dihydroxyvitamin D3; Rocaltrol ), which is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
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Androgen Receptor antagonist
Cyproterone acetate is a synthetic derivative of 17-hydroxyprogesterone, and acts as an androgen receptor antagonist as well as a weak progesterone receptor agonist with weak progestational and glucocorticoid activity. - Falecalcitriol(Fulstan; Hornel) is an analog of calcitriol; has a higher potency both in vivo and in vitro systems, and longer duration of action in vivo.
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Glucocorticoid receptor agonist
Glucocorticoid receptor agonist is a potent Glucocorticoid receptor agonist. - Seocalcitol is a vitamin D analog, binds vitamin D receptor protein from human osteosarcoma MG-63 cells with Kd of 0.27 nM.
- Levothyroxine, also L-thyroxine or T4, is a synthetic form of the thyroid hormone thyroxine, which is normally secreted by the follicular cells of the thyroid gland.
- Prednisolone is a synthetic glucocorticoid, a derivative of cortisol, which is used to treat a variety of inflammatory and auto-immune conditions.
- Meclizine is a human pregnane X receptor (hPXR) agonist. It possesses anticholinergic, central nervous system depressant, and local anesthetic effects. Its antiemetic and antivertigo effects are not fully understood, but its central anticholinergic properties are partially responsible.
- Quinapril inhibits angiotensin converting enzyme, an enzyme which catalyses the formation of angiotensin II from its precursor, angiotensin I.
- Moexipril hydrochloride is a potent orally active non-sulfhydryl angiotensin converting enzyme inhibitor (ACE) which is used for the treatment of hypertension and congestive heart failure.
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ACE inhibitor
Cilazapril is a pyridazine angiotensin-converting enzyme inhibitor (ACE inhibitor) used for the treatment of hypertension and congestive heart failure.
