Catalog No.
Product Name
Application
Product Information
Product Citation
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GnRH antagonist
Abarelix acetate is a synthetic peptide gonadotropin releasing hormone receptor (GnRH) antagonist - KW-8232 free base is an anti-osteoporotic agent, and can reduces the biosynthesis of PGE2.
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Estrogen receptor antagonist
Endoxifen is a secondary metabolite of tamoxifen. It is a primary metabolite responsible for the effectiveness of tamoxifen in ER-positive breast cancer.- Marina Arino Martin, .et al. , Environ Res, 2021, Apr 3;197:111121 PMID: 33823193
- Martin MA, .et al. , Water Res, 2019, Dec 29;171:115451 PMID: 31901682
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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. -
ACE inhibitor
Zofenopril calcium is an angiotensin-converting enzyme ACE inhibitor.- Tomas Jasenovec, .et al. , Biomedicines, 2021, Dec 14;9(12):1902 PMID: 34944718
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estrogen receptor modulator
acolbifene is a substance being studied in the prevention of breast cancer in women at high risk of breast cancer. Acolbifene hydrochloride binds to estrogen receptors in the body and blocks the effects of estrogen in the breast. It is a type of selective estrogen receptor modulator (SERM).- Sumit Bansal, .et al. , J Pharmacol Exp Ther, 2019, June, 369 (3) 389-405 PMID: 30918069
- Lirit N. Franks, .et al. , Front Pharmacol, 2016, 7: 503 PMID: 28066250
- 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. -
angiotensin AT2 receptor antagonist
PD 123319 ditrifluoroacetate is a potent, selective, non-peptide angiotensin AT2 receptor antagonist. IC50 values are 34 and 210 nM in rat adrenal tissue and brain respectively.- Dao-Lai Zhang, .et al. , eLife, 2018, 7: e33432 PMID: 29393851
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Apelin Receptor activator
(Glp1)-Apelin-13 is an activator of Apelin Receptor - Arzoxifene HCl is the hydrochloride salt of arzoxifene, a synthetic aromatic derivative with anti-estrogenic properties. Arzoxifene binds to estrogen receptors as a mixed estrogen agonist/antagonist.
- Sumit Bansal, .et al. , J Pharmacol Exp Ther, 2019, June, 369 (3) 389-405 PMID: 30918069
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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. - Bopindolol malonate is a non-selective, potent, long-acting beta adrenoceptor antagonist. It demonstrates inhibition of H2O2-induced lipid peroxdiation.
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CYP17A1/androgen synthesis inhibitor
Orteronel (TAK700) is an androgen synthesis inhibitor. It selectively inhibits the enzyme CYP17A which is expressed in testicular, adrenal, and prostatic tumor tissues. -
LTA4 hydrolase inhibitor
Captopril Disulfide is a reversible and competitive inhibitor of LTA4 hydrolase (IC50=11 M). Captopril has been shown to be an of angiotensin converting enzyme-1 (ACE1), but not ACE2(IC50 = 22 nM). -
ACE inhibitor
Zofenopril is an angiotensin-converting enzyme (ACE) inhibitor with an IC50 of 81 μM. - Zearalenone is a phytoestrogenic mycotoxin usually produced by Fusarium species, is shown to be a cytotoxic compound, but alos binds to the estrogen receptor (ER) (IC50 values are 166 and 240 nM for ERβ and ERα respectively) and was found to stimulate the transcriptional activity of both subtypes at concentrations between 1 - 10 nM.
- Muthulakshmi S, .et al. , J Appl Toxicol, 2018, Nov;38(11):1388-1397 PMID: 29923290
- Eprosartan (mesylate) is a competitive AT1 receptor antagonist with IC50 values ranging from 1.4 ?€? 3.9 nM and an elimination half-life of five to seven hours.
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GnRH antagonist
Elagolix is a Gonadotropin-Releasing Hormone (GnRH) Antagonist. Elagolix inhibits gonadatropin releasing hormone (GnRH) receptors in the pituitary gland and ultimately reduces circulating sex hormone levels. -
androgen-receptor (AR) antagonist
N-desMethyl EnzalutaMide is used in the treatment of disorders involving androgen, estrogen and progesterone receptors. -
Renin inhibitor
VTP-27999 HCl is a potent inhibitor of renin with IC50 value of 0.3 nM for human renin. -
progesterone receptor antagonist
Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity.- Hirad A. Feridooni, .et al. , Am J Physiol Heart Circ Physiol, 2017, Jan 1; 312(1): H46-H59 PMID: 27793852
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angiotensin II receptor antagonist
BIBS39 is a nonpeptide angiotensin II (AII) receptor antagonists that displaced [125I] AII from its specific binding sites with a K(i) value of 29 +/- 7 nM for the AII subtype I (AT1) receptor and a K(i) value of 480 +/- 110 nM for the AII subtype 2 (AT2) receptor. -
angiotensin receptor-neprilysin inhibitor
LCZ696 is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. -
estrogen receptor modulator
Ospemifene is a non-hormonal selective estrogen receptor modulator (SERM). - Angiotensin I is formed by the action of renin on angiotensinogen.
- Angiotensin (1-7) is an endogenous peptide fragment that can be produced from Ang I or Ang II via endo- or carboxy-peptidases respectively.
- Angiotensin II (Ang II) is an octapeptide hormone that plays a central role in cardiovascular homeostasis.
- Angiotensin III is a hexapeptide formed as a result of a cleavage at the N-terminus of Angiotensin II, a key factor in the Renin-Angiotensin-Aldosterone (RAAS) system by angiotensinases located in red blood cells and the vascular beds of most tissues.
- Angiotensin 1/2 (1-9) is a peptide (ASP-ARG-VAL-TYR-ILE-HIS-PRO-PHE-HIS) containing the amino acids 1-9 that are converted from Angiotensin I/II peptide.
- Acetyl Angiotensinogen (1-14),porcine, The protein encoded by the Angiotensinogen gene is known as pre-angiotensinogen or angiotensinogen precursor.
- Angiotensin 1/2 (1-5) is a peptide that contains the amino acids 1-5 and is converted from Angiotensin I/II.
