AZD9496
CAS 1639042-08-2
AZD9496 is a potent and selective estrogen receptor (ERα) antagonist with an IC50 of 0.28 nM.
Metabolism & Endocrinology
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
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Ebselen
CAS 60940-34-3
Ebselen is a small-molecule capsid Inhibitor of HIV-1 replication.Target:Ebselen is an organoselenium compound, as an inhibitor of HIV-1 capsid CTD dimerization. Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming…
ORM-15341(Ketodarolutamide)
CAS 1297537-33-7
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.IC50 value: 38…
AZ-1
CAS 803735-54-8
AZ-1 is a small molecule inducer of ABCA1 and apoE that act through indirect activation of the LXR pathway, shows purinergic receptor P2X7 antagonist activity; upregulates ABCA1 across multiple CNS cell types, including human astrocytes, pericytes, and…
PF05175157
CAS 1301214-47-0
PF-05175157 is broad spectrum acetyl-CoA carboxylase (ACC) inhibitor with IC50s of 27.0, 33.0, 23.5 and 50.4 nM for ACC1 (human), ACC2 (human), ACC1 (rat), ACC2 (rat), respectively.
JNJ-10229570
CAS 524923-88-4
JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells…
CAY10415(MSDC-0160)
CAS 146062-49-9
Mitoglitazone, also known as CAY10415, is a novel peroxisome proliferator-activated receptor (PPAR)γ ligand. CAY10415 induced cell death and ROS generation in a PPARγ-independent manner. CAY10415 enhanced γ-radiation-induced apoptosis and caspase-3-mediated…
Ursocholic acid
CAS 2955-27-3
Ursocholic acid, a bile acid found predominantly in bile of mammals, is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α.
Avasimibe
CAS 166518-60-1
Avasimibe is an oral inhibitor of acyl-Coenzyme A:cholesterol acyltransferase (ACAT) with IC50s of 24 and 9.2 µM for ACAT1 and ACAT2, respectively.
PF-05231023
CAS 1037589-69-7
PF-05231023, a long-acting fibroblast growth factor 21 (FGF21) analog, is a FGF21-receptor agonist, suitable for development as a potential treatment for T2DM[1][5].
CYN 154806
CAS 183658-72-2
CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively[1][2].
EDP-305
CAS 1933507-63-1
EDP-305 is a novel and potent farnesoid X receptor (FXR) agonist, with no/minimal cross-reactivity to TGR5 or other nuclear receptors.
AS1842856
CAS 836620-48-5
AS1842856 is a potent and cell-permeable Foxo1 inhibitor with an IC50 of 30 nM.
AP-III-a4 hydrochloride
CAS 2070014-95-6
ENOblock Hcl(AP-III-a4 Hcl) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.
SRT2104
CAS 1093403-33-8
SRT 2104 is a brain-permeable activator of SIRT1, used for the research of type 2 diabetes mellitus and Huntington's disease.
KGA-2727
CAS 666842-36-0
KGA-2727 is a potent, selective SGLT1 inhibitor with Ki of 97.4 nM, >100-fold selectivity over SGLT2; attenuates the elevation of plasma glucose after glucose loading in streptozotocin-induced diabetic rats, preserves glucose-stimulated insulin secretion and…
JZL184
CAS 1101854-58-3
JZL 184 is a potent and selective inhibitor of MAGL with IC50 of 8 nM and 4 μM for inhibition of MAGL and FAAH in mouse brain membranes respectively.IC50 value: 8 nM [1]Target: MAGL inhibitorin vitro: JZL184 prolongs DSE in Purkinje neurons in cerebellar…
Ostarine(MK-2286)
CAS 841205-47-8
Ostarine(MK-2866; GTX-024) is a modulator of human androgen receptor.IC50 value:Target: androgen receptorOstarine (MK-2866) is an androgen receptor modulator (SARM) with an ED50 of 0.44 mg/day. Ostarine (MK-2866) has anabolic activity. Lack of PSA increases…
Enzalutamide (MDV3100)
CAS 915087-33-1
Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC50 of 36 nM in LNCaP prostate cells.
ARV-110
CAS 2222112-77-6
ARV-110 is an orally active, specific androgen receptor (AR) PROTAC degrader. ARV-110 promotes ubiquitination and degradation of AR. ARV-110 can be used for the research of prostate cancer.
FEBUXOSTAT
CAS 144060-53-7
Febuxostat(TEI 6720;TMX 67 ) is selective xanthine oxidase inhibitor with Ki of 0.6 nM.
Lesinurad (RDEA594）
CAS 878672-00-5
Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with Km values of 0.85 and 2 µM, respectively.
PF-06409577
CAS 1467057-23-3
PF-06409577 is a potent and selective allosteric activator of AMPK α1β1γ1 isoform with an EC50 of 7 nM.
BAY-2402234
CAS 2225819-06-5
BAY-2402234 is a selective dihydroorotate dehydrogenase (DHODH) inhibitor for the treatment of myeloid malignancies.
AG-270
CAS 2201056-66-6
AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC50 of 14 nM.
Navoximod (GDC-0919; NLG-919)
CAS 1402837-78-8
Navoximod is a potent IDO (indoleamine-(2,3)-dioxygenase) pathway inhibitor with Ki/EC50 of 7 nM/75 nM.
SB-334867 HCl
CAS 249889-64-3
SB-334867 is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. IC50 value: 7.2 (pKb) Target: orexin OX1 receptor in vitro: SB-334867-A inhibited the orexin-A (10 nM) and orexin-B (100 nM)-induced calcium responses…
Sotagliflozin (LX-4211)
CAS 1018899-04-1
LX-4211 is a potent dual SGLT2/1 inhibitor; Antidiabetic agents.IC50 value:Target: SGLT1/2LX4211 enhanced urinary glucose excretion by inhibiting SGLT2-mediated renal glucose reabsorption; markedly and significantly improved multiple measures of glycemic…
Enpp-1-IN-1
CAS 2289728-58-9
Enpp-1-IN-1 is a Ectonucleotide pyrophosphatase-phosphodiesterase 1 (enpp-1) inhibitor extracted from patent WO2019046778, Example 55[1].
ABT-702
CAS 1188890-28-9
ABT-702 dihydrochloride is a potent adenosine kinase (AK) inhibitor (IC50=1.7 nM).
Alexamorelin
CAS 196808-85-2
Alexamorelin is a new synthetic heptapeptide which inhibits GHS binding in vitro.
TVB-3166
CAS 1533438-83-3
TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor…
Histrelin acetate
CAS 220810-26-4
Histrelin is a synthetic gonadotropin-releasing hormone (GNRH) agonist that binds to the GNRH receptor (GNRHR; Ki = 0.2 nM in CHO cells expressing the human receptor).
ASC-J9
CAS 917813-54-8
For the detailed information about the solubility of ASC-J9 in water, the solubility of ASC-J9 in DMSO, the solubility of ASC-J9 in PBS buffer, the animal experiment（test） of ASC-J9, the in vivo,in vitro and clinical trial test of ASC-J9, the cell…
SR3335
CAS 293753-05-6
SR3335 (ML-176) is a selective RORα synthetic ligand, directly binds to RORα, but not other RORs, and functions as a selective partial inverse agonist of RORα in cell-based assays. Furthermore, SR3335 suppresses the expression of endogenous RORα target genes…
LEI 110
CAS 2313525-90-3
LEI110 (LEI－110) is a potent Phospholipase A2 group XVI (PLA2G16) inhibitor with Ki of 20 nM, also has activity on HRASLS2, RARRES3 and iNAT (pIC50=6.8-7.6); reduces cellular arachidonic acid levels and oleic acid-induced lipolysis in human HepG2 cells;…
PF 429242
CAS 947303-87-9
PF-429242 is a potent inhibitor of S1P (cellular proprotein convertase sterol regulatory element-binding protein (SREBP) site 1 protease) that reduces expression levels of hepatic SREBP target genes and lower rates of cholesterol and fatty acid synthesis in…
Giredestrant
CAS 1953133-47-5
Giredestrant (GDC-9545), a non-steroidal ER ligand, is an orally active and selective estrogen receptor (ER) antagonist. Giredestrant potently competes with estradiol for binding and induces a conformational change within the ER ligand binding domain.…
5-IODOTUBERCIDIN
CAS 24386-93-4
5-Iodotubercidin (Itu) has been shown to inhibit mitogen-activated protein kinase (ERK2) (Ki = 525 nM), adenosine kinase (ADK) (Ki = 30 nM), casein kinases 1 & 2 (CSNK1A1 & CSNK2A1), protein kinase A (PKA) and insulin receptor kinase (IC50 ranging from 0.
IM156
CAS 1422365-93-2
IM156, a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation. IM156 blocks oxidative phosphorylation (OXPHOS) through the inhibition of complex I and increases apoptosis. IM156 ameliorates various types of fibrosis and…
Denifanstat (TVB-2640)
CAS 1399177-37-7
TVB-2640(FASN-IN-2) is a Fatty Acid Synthase (FASN) inhibitor extracted from patent WO2012122391A1, compound 152, has an IC50 of 0.052 μM and an EC50 of 0.072 μM[1].
Semaglutide (sodium salt)
CAS 910463-68-2
Semaglutide, a long-acting GLP-1 analogue, is a glucagon-like peptide-1 (GLP-1) receptor agonist that can be used in the treatment of type 2 diabetes.
Octreotide acetate (SMS 201-995 (acetate))
CAS 79517-01-4
Octreotide acetate, a long-acting synthetic analog of native somatostatin, inhibits growth hormone, glucagon, and insulin more potently.
Cedazuridine
CAS 1141397-80-9
Cedazuridine (E7727) is a Cytidine Deaminase (CDA) inhibitor with an IC50 value of 0.4 μM[1].
TAK-875(Fasiglifam)
CAS 1000413-72-8
Fasiglifam (TAK-875) is a potent, selective and orally bioavailable GPR40 agonist with EC50 of 72 nM.
ML349
CAS 890819-86-0
ML349 is a potent and specific acyl protein thioesterase 2 (APT-2) inhibitor with a Ki of 120 nM. ML349 is also an inhibitor of LYPLA2 with an IC50 of 144 nM.
Apararenone
CAS 945966-46-1
Apararenone (MT-3995) is a novel non-steroidal mineralocorticoid receptor antagonists under development for the treatment of diabetic nephropathies and non-alcoholic steatohepatitis.
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