PF-04457845
CAS 1020315-31-4
PF-04457845 is a highly efficacious and selective FAAH inhibitor with IC50 values is 7.2±0.63 nM and 7.4±0.62 nM for hFAAH and rFAAH, respectively.
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Other Research Tools (75) · Additional reagents, building blocks and specialized research tools.
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GW4869
CAS 6823-69-4
GW4869 is a noncompetitive neutral sphingomyelinase inhibitor with an IC50 of 1 μM.
Ibiglustat(Genz-682452）
CAS 1401090-53-6
Ibiglustat (Venglustat) is an inhibitor of glucosylceramide synthase extracted from patent WO 2015089067 A1, compound example 64.
Devazepide
CAS 103420-77-5
Devazepide is a potent, and orally active CCK1 (CCK-A) receptor antagonist that displays appetite-stimulant effects. It blocks the anorectic response to CCK-8 and increases food intake in rats following systemic and i.c.v administration.
Degarelix (acetate)
CAS 214766-78-6
Degarelix is a competitive and reversible gonadotropin-releasing hormone receptor (GnRHR) antagonist.
Balaglitazone
CAS 199113-98-9
Balaglitazone is a selective partial PPARγ agonist with an EC50 of 1.351 μM for human PPARγ.
APD668
CAS 832714-46-2
APD668 is a potent GPR119 agonist with EC50 of 2.7 nM and 33 nM for hGPR119 and ratGPR119 respectively.Chronic treatment withAPD668 showed for the first time that blood glucose and glycated hemoglobin (HbA1c) levels could be significantly reduced in Zucker…
OSS-128167(SIRT6-IN-1)
CAS 887686-02-4
OSS_128167 is a selective SIRT6 inhibitor with IC50s of 89, 1578 and 751 μM for SIRT6, SIRT1 and SIRT2, respectively.
SC-26196
CAS 218136-59-5
SC-26196 is a potent, orally active Delta6 desaturase (D6D) inhibitor (IC50=0.2 µM in a rat liver microsomal assay). Antiinflammatory properties[1].
PF-9366
CAS 72882-78-1
PF-9366 is a human methionine adenosyltransferase 2A (Mat2A) inhibitor, with an IC50 of 420 nM and a Kd of 170 nM.
Elamipretide (TFA salt)
CAS 736992-21-5
Elamipretide is a cardiolipin peroxidase inhibitor and mitochondria-targeting peptide.
ONO-7300243
CAS 638132-34-0
ONO-7300243 is a novel, potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM.
PF-06835919
CAS 2102501-84-6
PF-06835919, also known as MDK1846, is a potent ketohexokinase (KHK) inhibitor. PF-06835919 is reported in patent US 20170183328 A1, example 4. Increased fructose consumption and its subsequent metabolism have been implicated in hepatic steatosis,…
MK-3903
CAS 1219737-12-8
MK-3903 is a potent and selective AMP-activated protein kinase (AMPK) activator with an EC50 of 8 nM.
GLPG-1690(Ziritaxestat)
CAS 1628260-79-6
GLPG1690 is a first-in-class autotaxin (ATX) inhibitor, with an IC50 of 131 nM and Ki of 15 nM.
GRA Ex-25
CAS 307983-31-9
GRA Ex-25 is an inhibitor of glucagon receptor, with IC50 of 56 and 55 nM for rat and human glucagon receptors, respectively.
NLG919(GDC-0919)
CAS 1402836-58-1
IDO-IN-7 (NLG-919 analogue) is a a potent IDO1 inhibitor with an IC50 of 38 nM.
SR 8278
CAS 1254944-66-5
SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm[1][2].
preQ1 Dihydrochloride
CAS 86694-45-3
preQ1 is a precursor in the biosynthesis of queuosine, a bacterial nucleoside incorporated into tRNA by tRNA transglycosylase. preQ1 binds to an aptamer domain on tRNA that acts as a riboswitch to repress gene expression.
SR9011
CAS 1379686-29-9
SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.
Apalutamide（ARN509）
CAS 956104-40-8
Apalutamide (ARN-509) is a potent and competitive androgen receptor (AR) antagonist, binding AR with an IC50 of 16 nM.
BAY-876
CAS 1799753-84-6
BAY-876 is the first highly selective GLUT1 inhibitor with IC50 of 0.002 uM. show good metabolic stability in vitro and high oral bioavailability in vivo.
Fadrozole (hydrochloride)
CAS 102676-31-3
Fadrozole hydrochloride is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
U-104
CAS 178606-66-1
U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki of 45.1 nM and 4.5 nM; low inhibition for CA I and CA II.
Tropifexor (LJN452)
CAS 1383816-29-2
Tropifexor is a novel and highly potent agonist of FXR with an EC50 of 0.2 nM.
ML-348(ML348)
CAS 899713-86-1
ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor (IC50 = 210 nM), Exhibits 14-fold selectivity for LYPLA1 over LYPLA2, Also selective over a panel of ~30 other serine hydrolases.target: LYPLA1 [1]IC 50： 210 nM [1]
Sinogliatin (HMS5552, RO5305552)
CAS 1191996-10-7
Sinogliatin (HMS5552, RO5305552) is a mall molecule glucokinase (GCK; GK) activator.
DANUGLIPRON（PF-06882961）
CAS 2230198-02-2
PF-06882961 is a potent, orally bioavailable agonist of the glucagon-like peptide-1 receptor (GLP-1R)
iGOT1-01
CAS 882256-55-5
iGOT1-01 is a small molecule inhibitor of aspartate aminotransferase 1 (glutamate oxaloacetate transaminase 1 (GOT1)) with IC50 of 11.3 uM.
GOT1 inhibitor 2c
CAS 732973-87-4
GOT1 inhibitor 2c is a first-in-class, non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with IC50 of 8.2 uM.
EMD638683
CAS 1181770-72-8
EMD638683 is a potent SGK1 inhibitor with an IC50 of 3 uM. The serum- and glucocorticoid-inducible kinase 1 (SGK1) is transcriptionally upregulated by mineralocorticoids and activated by insulin. EMD638683 could serve as a template for drugs counteracting…
BAR 502
CAS 1612191-86-2
BAR502 is a dual FXR and GPBAR1 agonist with IC50 values of 2 μM and 0.4 μM, respectively.
ACU4429,ACU 4429,ACU-4429
CAS 1141934-97-5
Emixustat hydrochloride strongly inhibits 11-cis-retinol production with IC50 values of 232 ± 3 nM.Emixustat hydrochloride is a novel visual cycle modulator, in healthy volunteers. Oral Emixustat was safe and well tolerated when administered once daily for 14…
Pasireotide
CAS 396091-73-9
Pasireotide(SOM 230) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively).
LXRβ agonist 17
CAS 1878259-00-7
A novel, potent, orally active liver X receptor β (LXRβ) agonist with Ki/EC50 of 3/21 nM, displays 27-fold selectivity over LXRα; also exhibits excellent selectivity against other nuclear hormone receptors (>3,000-fold); induces the expression of LXR target…
Mavorixafor(AMD-070)
CAS 558447-26-0
AMD-070 is a potent, selective and orally available CXCR4 antagonist, with an IC50 value of 13 nM against CXCR4 125I-SDF binding, and also inhibits the replication of T-tropic HIV-1 (NL4.3 strain) in MT-4 cells and PBMCs with an IC50 of 1 and 9 nM,…
R162
CAS 64302-87-0
R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1), with anti-cancer properties.
CVT-10216
CAS 1005334-57-5
CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduces excessive alcohol drinking in alcohol-preferring rats…
2-NBDG
CAS 186689-07-6
2-NBDG is a fluorescent indicator for direct glucose uptake measurement and also is an indicator of cell viability.
AM095
CAS 1345614-59-6
AM095 is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively. AM095 is an LPA1 receptor antagonist with good oral exposure and antifibrotic activity in rodent models. In vitro, AM095…
SLC25A1 inhibitor CTPI-2
CAS 68003-38-3
CTPI-2 is a third-generation mitochondrial citrate carrier SLC25A1 inhibitor with a KD of 3.5 μM. CTPI-2 inhibits glycolysis, PPARγ, and its downstream target the glucose transporter GLUT4. CTPI-2 halts salient alterations of NASH reverting steatosis,…
Atosiban
CAS 90779-69-4
Atosiban(RW22164; Tractocile) is a nonapeptide, desamino-oxytocin analogue, and a competitive vasopressin/oxytocin receptor antagonist (VOTra). Atosiban inhibits the oxytocin-mediated release of inositol trisphosphate from the myometrial cell membrane.As a…
Ganirelix
CAS 124904-93-4
Ganirelix is a man-made form of a protein that reduces the amount of certain hormones in the body, including estrogen.
Pramlintide
CAS 151126-32-8
Pramlintide is a polypeptide analogue of human amylin. Pramlintide, an antidiabetic agent, is antineoplastic in colorectal cancer.
PF-05221304(Clesacostat)
CAS 1370448-25-1
PF-05221304 is an orally bioavailable, liver-directed and dual ACC1 (and ACC2) inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2, 12.4 nM for human ACC1 and 8.7 nM for human ACC2. PF-05221304 is a substrate for organic anion transport…
MK-0557
CAS 328232-95-7
MK-0557 is a highly selective, orally available neuropeptide Y5 receptor antagonist with a Ki of 1.6 nM.
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