| DC74634 |
Seladelpar free acid |
Seladelpar, also known as MBX-8025 and RWJ-800025, is a selective peroxisome proliferator-activated receptor (SPPAR) -δ receptor agonist. MBX-8025 may have potential use for the treatment of dyslipidemia, metabolic syndrome, type 2 diabetes, and non-alcoholic steatohepatitis. |
|
| DC74635 |
ATH434 mesylate |
ATH434, also known as PBT434, is a novel, brain-penetrant, inhibitor of α-synuclein aggregation. In transgenic animal models of Parkinson disease (A53T) and MSA (PLP-α-Syn), PBT434 reduced α-synuclein aggregation, preserved neurons and improved motor function. Glial cell inclusions were also reduced in a murine MSA model. PBT434 is thought to act by redistributing reactive iron across membranes, thereby blocking intracellular protein aggregation and oxidative stress. The affinity of PBT434 for iron is greater than that of α-synuclein but lower than that of iron trafficking proteins, e.g., ferritin. |
|
| DC74636 |
Bromo-PADAP |
Bromo-PADAP is a dye agent for research use. Bromo-PADAP was reported for the spectrophotometric determination of uranium(VI). Bromo-PADAP is highly sensitive towards uranium, the uranyl complex having a molar absorptivity of 74,000 at 578 nm and pH 7.6. In the presence of a mixed masking solution only a few ions interfere seriously, and the method can be made specific for uranium by a preliminary extraction of uranium into tri-n-octylphosphine oxide, and direct development of the bromo-PADAP colour in the organic phase. Details are given for the determination of uranium in waters, ores, phosphoric acid and phosphate rocks, thorium oxide, and zirconium oxide. |
|
| DC74637 |
Deuremidevir free base |
Deuremidevir, also known as VV116, JT001, and mindeudesivir, is a chemically-modified version of the antiviral remdesivir with oral bioavailability and potent activity against SARS-CoV-2. VV116 is a deuterated, tri-isobutyrate ester prodrug of the RDV parent nucleoside, and is rapidly metabolized into the parent nucleoside (116-N1) in the body. 116-N1 is intracellularly converted to the nucleoside triphosphate active form, which would interfere with the function of RNA-dependent RNA polymerase of SARS-CoV-2, thus exerting antiviral effects. VV116 showed potent activity against a panel of SARS-CoV-2 variants (alpha, beta, delta, and omicron) and excellent therapeutic efficacy in the mice model. Note: the non-labeled analog is called GS621763 (Cat#465727). |
|
| DC74638 |
GLPG3667 |
GLPG3667 is an oral, reversible, and selective tyrosine kinase 2 (TYK2) inhibitor. It is being developed to treat inflammatory and auto-immune diseases. Biochemical assays showed that GLPG3667 displayed nanomolar potency on TYK2 with a selectivity over other JAK kinases >3-fold. In human PBMC, GLPG3667 showed comparable potency on the IFNα and IL-23 pathways (around 50 nM). Selectivity for TYK2 on the IFNα pathway was >14-fold and >19-fold toward the IL-2 and GM-CSF pathways in human PBMC and whole blood, respectively. Dermal ear inflammation in a mouse model of psoriasis driven by IL-23 was prevented by GLPG3667 with a minimal effective dose of 3 mg/kg given orally once daily. This effect was associated with a decrease in neutrophil infiltration and STAT3 phosphorylation at sites of inflammation. In healthy HV, GLPG3667 completely inhibited IFNα-induced STAT1 and STAT3 phosphorylation but did not impact IL-2- and GM-CSF-induced STAT5 phosphorylation. |
|
| DC74639 |
Oligopeptide-10 |
Oligopeptide-10, also known as granactive oligopeptide-10, is a synthetic bio-active peptide composed of 15 amino acids. it can help manage acne-causing bacteria, both on its own and in conjunction with anti-acne superstar exfoliant salicylic acid. |
|
| DC74640 |
Ganirelix acetate |
Ganirelix is is an antagonist of GnRH that competitively antagonizes the gonadotropic GnRH receptor, thereby mutating the pathway and causing rapid and reversible inhibition of gonadotropin (luteinizing hormone LH and follicle stimulating hormone FSH) secretion. Ganirelix Acetate acts by competitively blocking the GnRH receptors on the pituitary gonadotroph and subsequent transduction pathway. It induces a rapid, reversible suppression of gonadotropin secretion. The suppression of pituitary LH secretion by Ganirelix Acetate is more pronounced than that of FSH. |
|
| DC74641 |
HC-258 |
HC-258 is a Covalent Acrylamide TEAD Inhibitor That Reduces Gene Expression and Cell Migration. HC-258 reduces the CTGF, CYR61, AXL, and NF2 transcript levels and inhibits the migration of MDA-MB-231 breast cancer cells. Co-crystallization with hTEAD2 confirmed that HC-258 binds within TEAD’s PA pocket, where it forms a covalent bond with its cysteine. |
|
| DC74642 |
Mtb ATP synthase-IN-1 |
Mtb ATP synthase-IN-1 is a potent Mycobacterium tuberculosis (Mtb) ATP synthase inhibitor, with MIC of 0.452-0.499 μg/mL against Mtb. |
|
| DC74643 |
PSMA I＆T |
PSMA I＆T is a ligand for making 177Lu-PSMA-I&T for Treatment of Metastatic Castration-Resistant Prostate Cancer. |
|
| DC74644 |
PSMA-I&F |
PSMA-I&F is a ligand for making 68Ga/177Lu-PSMA-I&F, which is a PSMA-Targeted Hybrid Tracer. PSMA-I&F is a useful agent for Nuclear and Fluorescence Imaging of Prostate Cancer. |
|
| DC74645 |
OXA-06 HCl |
OXA-06 is a potent ROCK inhibitor(IC50 = 10 nM). OXA-06 suppresses pMYPT1 and pCofilin levels in non-small cell lung carcinoma (NSCLC) cell lines. OXA-06 also inhibits anchorage-independent growth of NSCLC cell lines in vitro. |
|
| DC74646 |
EB-PSMA-617 |
EB-PSMA-617 is an Evans blue-modified prostate-specific membrane antigen (PSMA) 617 ligand for making 177Lu-EB-PSMA, which is potential useful for Metastatic Castration-Resistant Prostate Cancer. |
|
| DC74647 |
Neladalkib |
Neladalkib, also known as NVL-655, and NUV-655, is a selective, brain-penetrant ALK inhibitor with antitumor activity against the lorlatinib-resistant G1202R/L1196M compound mutation. NUV-655 (NVL-655) inhibited the kinase activity of ALK and ALK G1202R/L1196M with Kiapp < 5 nM in the presence of 1 mM ATP and with selectivity over TRKB. Across a panel of 335 wild-type kinases, NUV-655 (NVL-655) inhibited only 5 other kinases by >50% within 10-fold of its IC50 for ALK. NUV-655 (NVL-655) also selectively inhibited ALK in cells. It inhibited the growth of Ba/F3 cells driven by expression of EML4-ALK variant 1 (v1) with either wild-type kinase domain or drug-resistance mutations G1202R, G1202R/L1196M, or G1202R/G1269A at IC50 values < 10 nM and with selectivity over TRKB. In vivo, NUV-655 (NVL-655) induced regression at well-tolerated doses in a Ba/F3 EML4-ALKv1 G1202R/L1196M xenograft model. Furthermore, NUV-655 (NVL-655) demonstrated brain penetrance in rodent pharmacokinetic studies. |
|
| DC74648 |
Demethyleneberberine chloride |
Demethyleneberberine, a berberine metabolite, is a mitochondria-targeted antioxidant isolated from Cortex Phellodendri chinensis that exhibits multiple pharmacological activities including anti-microbial, anti-inflammatory, anti-diarrhea and anti-cancer. |
|
| DC74649 |
NOTA-TATE
Featured
|
|
|
| DC74650 |
NOTA-NFB |
NOTA-NFB is a ligand for making radioactive complex 68Ga-NOTA-NFB, which is am imaging agent and a tracer for CXCR4 evaluation in glioma patients after measuring the dosimetry of 68Ga-NOTA-NFB in healthy volunteers. |
|
| DC74651 |
Alfatide II |
Alfatide II is ligand for making 18F-Alfatide II PET/CT for Identification of Breast Cancer: A Preliminary Clinical Study. 18F-alfatide II has been proven to have excellent clinical translational potential. |
|
| DC74652 |
DOTA-c(RGDyK) |
DOTA-c(RGDyK) is useful ligand for making 225Ac-DOTA-c(RGDyK), which is a potential radiopharmaceutical for targeted alpha particle therapy. |
|
| DC74653 |
Caspase-1 Inhibitor IV |
Caspase-1 Inhibitor IV controls the biological activity of Caspase-1. This small molecule/inhibitor is primarily used for Cancer applications. |
|
| DC74654 |
NOTA-E(cRGDfK)2 |
NOTA-E(cRGDfK)2 is a ligand to making 68Ga-DOTA-E[c(RGDfK)]2, which is a PET Imaging agent of SHARPIN-Regulated Integrin Activity. E[c(RGDfk)]2 = glutamic acid-[cyclo(arginyl-glycyl-aspartic acid-D-phenylalanine-lysine). |
|
| DC74655 |
NOTA-P2-RM26 |
NOTA-P2-RM26 is a high-affinity NOTA-conjugated bombesin antagonist for GRPR-targeted tumor imaging |
|
| DC74656 |
NOTA-cyclic RGDyK |
NOTA-cyclic RGDyK is a ligand to bind 68Ga for molecular imaging of αvβ3 integrin overexpressing tumor. |
|
| DC74657 |
NVP-CGM097 free base |
NVP-CGM097 is a potent and selective MDM2 inhibitor. P53 wild type GOT1 cells were sensitive to NVP-CGM097, p53mutated BON1 and p53mutated NCI-H727 cells were resistant to NVP-CGM097. Incubation of GOT1 cells with NVP-CGM097 at 100, 500, and 2,500 nM for 96 h caused a significant decline in cell viability to 84.9 ± 9.2% (p < 0.05), 77.4 ± 6.6% (p < 0.01), and 47.7 ± 9.2% (p < 0.01). NVP-CGM097 can inhibit the proliferation of tumor cells. NVP-CGM097 could reverse ABCB1-mediated MDR by directly blocking the ABCB1-mediated drug efflux and raising the accumulation of chemotherapeutic drugs in cancer cells. NVP-CGM097 tended to bind to the inhibitory site, which led to slight but critical conformational changes in the transporter and reduced the ATPase activity. |
|
| DC74658 |
NOTA-JR-11 |
NOTA-JR-11 is a somatostatin receptor (SSTR) antagonist. |
|
| DC74659 |
DOTA-LM3 |
DOTA-LM3 is a somatostatin receptor ( SSTR ) antagonist. |
|
| DC74660 |
Monlunabant |
Monlunabant, also known as INV-202, is a potent CB1R inverse agonist. INV-202 demonstrated weight loss potential in a phase 1b trial and is currently in a phase 2 trial for diabetic kidney disease (DKD). INV-202 reduced glomerular injury, preserved podocyte structure and function, reduced injury to PTECs, and ultimately reduced renal fibrosis in a streptozotocin-induced diabetic nephropathy mouse model. |
|
| DC74661 |
HEC96719 |
HEC96719 is a tricyclic farnesoid X receptor agonist (FXR agonist) for treatment of non-alcoholic steatohepatitis. HEC96719 exhibits excellent potency superior to GW4064 and obeticholic acid in in vitro and in vivo assays of FXR activation. It also shows higher FXR selectivity and more favorable tissue distribution dominantly in liver and intestine. Preclinical data on pharmacokinetic properties, efficacy, and safety profiles overall indicate that HEC96719 is a promising drug candidate for NASH treatment. |
|
| DC74662 |
CHK1-IN-3 |
CHK1-IN-3 is a Checkpoint Kinase 1 (CHK1) inhibitor with an IC50 of 0.4 nM. |
|
| DC74663 |
DOTA |
DOTA is an azamacrocyle in which four nitrogen atoms at positions 1, 4, 7 and 10 of a twelve-membered ring are each substituted with a carboxymethyl group. It has a role as a chelator and a copper chelator. It derives from a hydride of a 1,4,7,10-tetraazacyclododecane. It is a a metal chelate in use in medical diagnostics. |
|
