Metabolism & Endocrinology

Benitrobenrazide

CAS 2454676-05-0

Benitrobenrazide is a novel selective hexokinase 2 (HK2) inhibitor, blocking cancer cells growth by targeting glycolysis.

A1120

CAS 1152782-19-8

A 1120 is a high affinity non-retinoid ligand for retinol-binding protein 4 (RBP4) with the ki value of 8.3 nM[1].

Calcitonin salmon

CAS 47931-85-1

Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption. Sequence:…

Tirzepatide (LY3298176)

CAS 2023788-19-2

Tirzepatide (LY3298176, GIP/GLP-1 RA, TZP) is a dual GIP/GLP-1 receptor agonist. Tirzepatide differentially induces internalization of the GIP and GLP-1 receptors with EC50 values of 18.2 nM and 18.1 nM, respectively.

AR 231453

CAS 733750-99-7

AR231453 is a potent and selective small molecule agonist of GPR119 that enhances glucose-dependent insulin secretion and glucagon-like peptide 1 (GLP-1) release; Antidiabetic agent.

Bazedoxifene-Acetate

CAS 198481-33-3

Bazedoxifene acetate is a third generation selective estrogen receptor modulator (SERM) with IC50s of 26 and 99 nM for ERα and ERβ, respectively.

LGD2226

CAS 328947-93-9

LGD-2226 is a selective and orally active androgen receptor modulator with an EC50 of 0.2 nM and a Ki of 1.5 nM for human androgen receptor. LGD-2226 shows tissue selectivity in animal models, with reduced effects on prostate compared to muscle. LGD-2226 can…

RHC 80267

CAS 83654-05-1

RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC…

Sebetralstat

CAS 1933514-13-6

Sebetralstat is a plasma kallikrein inhibitor (WO2016083820). Sebetralstat can be used for the research of metabolic diseases.

Anamorelin

CAS 249921-19-5

Anamorelin is a novel ghrelin receptor agonist with EC50 value of 0.74 nM in the FLIPR assay.

FX-909

CAS 2924573-90-8

FX-909（FX 909） is a first-in-class inverse agonist of the peroxisome proliferator-activated receptor gamma (PPARG) lineage transcription factor with EC50 of 1 nM and shows >2000-fold selectivity for PPARG over PPARA/PPARD - acting through a mechanism that…

LDC203974(IMT1B)

CAS 2304621-06-3

LDC203974(IMT1B) is a highly specific inhibitor of human mitochondrial RNA polymerase (POLRMT) with improved pharmacokinetic profiles than LDC195943(IMT1).

Substance P

CAS 33507-63-0

Substance P is a neuropeptide, acting as a neurotransmitter and as a neuromodulator.The endogenous receptor for substance P is neurokinin 1 receptor (NK1-receptor, NK1R). Sequence: Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH2.

MTDIA

CAS 1399840-35-7

MTDIA, also known as MT-DADMe-ImmA, and Methylthio-DADMe-Immucillin A, is a MTAP inhibitor. Human 5'-methylthioadenosine phosphorylase (MTAP) is solely responsible for 5'-methylthioadenosine (MTA) metabolism to permit S-adenosylmethionine salvage.…

DC_AC50

CAS 497061-48-0

DC_AC50 is a dual inhibitor of Atox1 and CCS (copper chaperones). Inhibiting intracellular copper chaperones as a means of reducing/preventing acquired chemotherapy resistance[1].

Endoxifen

CAS 112093-28-4

Endoxifen Z-isomer is the most important Tamoxifen metabolite responsible for eliciting the anti-estrogenic effects of this drug in breast cancer cells expressing estrogen receptor-alpha (ERα). Endoxifen inhibits hERG tail currents at 50 mV in a…

Vepdegestrant (ARV-471)

CAS 2229711-68-4

ARV-471 is a best-in-class, orally active estrogen receptor (ER) PROTAC degrader. ARV-471 is developed for the research of breast cancer.

amyloid P-IN-1(GSK3039294)

CAS 1819986-22-5

pharmaceutical compositions comprising the same and the use of the same for treatment of diseases or disorders wherein depletion of serum amyloid P component (SAP) would be beneficial, including amyloidosis, Alzheimer's disease, type 2 diabetes mellitus and…

Perhexiline maleate

CAS 6724-53-4

Perhexiline maleate is a potent carnitine palmitoyltransferase 1 (CPT 1) inhibitor with IC50s of 77 and 148 μM for rat heart and liver CPT 1, respectively.

SW222746

CAS 2241676-74-2

SW222746 (SW 222746) is a potent selective, orally active inhibitor of 15-Prostaglandin dehydrogenase (15-PGDH) with IC50 of 3 nM.

TH9619

CAS 2379556-22-4

TH9619 (TH-9619) is a potent and selective inhibitor of folate metabolism enzyme MTHFD2 with IC50 of 47 nM.TH9619 demonstrated efficacy on HL-60 cell viability with EC50 of 11 nM.TH9619 potently inhibits related MTHFD proteins MTHFD2L and MTHFD1-(DC) with…

Ver-246608

CAS 1684386-71-7

Novel pan-isoform ATP competitive inhibitor of pyruvate dehydrogenase kinase, disrupting Warburg metabolism and inducing context-dependent cytostasis in cancer cells

4-Butylresorcinol

CAS 18979-61-8

In Vitro It shows that 4-Butylresorcinol (4-n-butylresorcinol) significantly inhibits melanin synthesis in a concentration-dependent manner. In addition, it is also found to inhibit the activity of tyrosinase, the rate-limiting melanogenic enzyme.…

YB-537

CAS 2844306-40-5

YB-537 (YB537) is a potent, highly specific quinone reductase 2 (QR2) inhibitor with IC50 of 3 nM, shows no activity against QR1 (IC50>10 uM).

Dorsomorphin dihydrochloride

CAS 1219168-18-9

Dorsomorphin dihydrochloride (BML-275 dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109±16 nM.

SMS1-IN-1

CAS 1807943-38-9

SMS1-IN-1, compound SAPA 1j, is a novel and the most potent sphingomyelin synthase 1 (SMS1) inhibitor with an IC50 value of 2.1 μM. SMS1-IN-1 has the potential for the treatment of atherosclerosis[1].

Alfacalcidol

CAS 41294-56-8

Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) is a non-selective VDR activator medication. IC50 value: Target: VDR activatorAlfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3) improves mechanical bone…

BCAT-IN-2

CAS 1800024-45-6

BCAT-IN-2 is a potent, selective and orally active inhibitor of mitochondrial branched-chain aminotransferase (BCATm), with a pIC50 of 7.3. BCAT-IN-2 shows selectivity for BCATm over BCATc (pIC50=6.6). BCAT-IN-2 can be used for the research of obesity and…

RGT1383

CAS 2428641-93-2

RGT1383 is a novel GLP-1R agonist, an analog of PF-06882961.

TTC-352

CAS 1607819-68-0

TTC-352 is a synthetic selective estrogen mimic acts as estrogen receptor (ER) partial agonist for the treatment of endocrine-resistant breast cancer.TTC-352 yields an H-bond with Glu353, allows Asp351-to-helix 12 (H12) interaction, sealing ERα's…

ITX-5061 hydrochloride

CAS 1252679-52-9

ITX-5061 is a scavenger receptor B1 antagonist that promotes high-density lipoprotein (HDL) levels; inhibits SR-BI-dependent uptake of HDL-CE in transfected cells, decreases the fractional catabolic rate of HDL-CE and reduced its hepatic uptake in mice;…

PF 6260933 dihydrochloride

CAS 1883548-86-4

PF 6260933 is a potent, selective and orally bioavailable MAP4K4 inhibitor with kinase IC50 of 3.7 nM, cell IC50 of 160 nM; possesses excellent kinome selectivity and suitable properties for in vivo pharmacological characterization; significantly improves…

Bremelanotide

CAS 189691-06-3

A peptide, non-selective melanocortin receptor agonist for treatment for female sexual dysfunction; selectively stimulates solicitational behaviors in the female rat, without affecting lordosis, pacing, or other sexual behaviors, does not cause generalized…

Evacetrapib (LY2484595)

CAS 1186486-62-3

Evacetrapib is a potent and selective of CETP inhibitor, which inhibits human recombinant CETP protein (IC50 5.5 nM) and CETP activity in human plasma (IC50 36 nM) in vitro.

Sirpiglenastat (Synonyms: DRP-104)

CAS 2079939-05-0

Sirpiglenastat (DRP-104) is a broad acting glutamine antagonist. Sirpiglenastat has anticancer effects by directly targeting tumor metabolism and simultaneously inducing a potent antitumor immune response.

SBI-797812

CAS 2237268-08-3

SBI-797812 is an orally active nicotinamide phosphoribosyltransferase (NAMPT) activator. SBI-797812 shifts NAMPT to NMN formation, increases NAMPT affinity for ATP, stabilizes phosphorylated NAMPT, promotes consumption of the pyrophosphate by-product, and…

JNJ-74856665

JNJ-74856665 is an orally bioavailable, potent, and selective DHODH inhibitor with IC50 of 0.40 nM. JNJ-74856665 shows favorable physicochemical properties and has been selected for clinical development in patients with AML and myelodysplastic syndromes (MDS).

VU0364739

CAS 1244639-78-8

VU0364739 is a selective inhibitor of phospholipase D2 (PLD2) with an IC50 value of 22 nM. Phospholipase D (PLD) enzymes, including PLD1 and PLD2, are involved in various cellular processes, such as signal transduction, membrane trafficking, and cytoskeletal…

(R)-GNE-140

CAS 2003234-63-5

(R)-GNE-140 (GNE-140) is a novel potent, selective lactate dehydrogenase (LDH) inhibitor with IC50 of 3, 5, and 5 nM for LDHA, LDHB, and LDHC, respectively; displays no inhibition on malate MDH-1, MDH-2 (IC50>10 uM for both enzymes), and no appreciable…

LSN3318839

CAS 2764704-18-7

LSN3318839 is an orally efficacious positive allosteric modulator of the glucagon-like peptide-1 receptor (GLP-1R).

AD-5591

CAS 1804942-45-7

AD-5591 (AD5591) is a potent, selective, new generation small molecule ALDH2 activator, has the improved biological activities and pharmacological properties compared to Alda-1. AD-5591 (100 μM) significantly increases the enzymatic activity of recombinant WT…

Cagrilintide

CAS 1415456-99-3

Cagrilintide is an investigational novel long-acting acylated amylin analogue, acts as nonselective amylin receptors (AMYR) and calcitonin G protein-coupled receptor (CTR) agonist. Cagrilintide induces significant weight loss and reduces food intake.…

Stenabolic (SR9009)

CAS 1379686-30-2

SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.

UT-59

CAS 1111234-96-8

UT-59 is a specific inhibitor that targets the cholesterol-sensing membrane protein Scap (SREBP cleavage-activating protein). It functions by binding to Scap's cholesterol-binding site, which prevents Scap from interacting with SREBPs (sterol regulatory…

Org 274179-0

CAS 1421683-12-6

Org 274179-0 is a highly potent, allosteric antagonist of the thyroid-stimulating hormone receptor (TSH receptor), inhibits bTSH-, hTSH- and M22-mediated CRE-luciferase transactivation in the CHO cell line.

PF-07328948

CAS 2936625-34-0

PF-07328948 is a first-in-class branched-chain ketoacid dehydrogenase kinase (BDK) inhibitor with IC50 of 15 nM and shows a high degree selectivity over a number of kinases and other off-targets. PF-07328948 is the first known selective BDK inhibitor…

DG-172 dihydrochloride

CAS 1361504-77-9

DG-172 is a novel PPARβ/δ-selective ligand showing high binding affinity (IC50= 27 nM) and potent inverse agonistic properties; inhibits agonist-induced activity of PPARβ/δ, enhances transcriptional corepressor recruitment; down-regulates transcription of the…

J-2156 TFA

CAS 2387505-73-7

J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalg