md

Osanetant HCl is the (R)-enantiomer; neurokinin-3 receptor antagonist

MD-224 is a highly potent and efficacious MDM2 degrader based on the proteolysistargeting chimera (PROTAC) concept,and as a new class of anticancer agent.

MD-265 is a PROTAC degrader that targets and degrades MDM2, leading to the activation of p53 in cancer cells with wild-type p53. MD-265 achieves complete tumor regression and enhances long-term survival in leukemic mice.

MD-4251 is an orally active MDM2 PROTAC degrader. It potently degrades MDM2 in RS4;11 cells (DC50: 0.2 nM) and activates p53. MD-4251 exhibits strong antiproliferative activity against acute leukemia cells with wild-type p53, but shows limited efficacy in mutant cells. In RS4;11 xenograft mouse models, MD-4251 induces complete tumor regression.

Terazosin-md (compound TZ-md) is a derivative of Alfuzosin and Terazosin, functioning as an orally active α1-adrenergic receptor antagonist. It enhances mitochondrial metabolism, degrades various pathological protein deposits, and improves vascular endothelial cell function. Moreover, Terazosin-md has shown activity in mouse models of Alzheimer's disease. This compound can be utilized in the research of Alzheimer's disease, its complications, and disorders associated with protein aggregation and metabolic imbalances.

Anticytokinin activity was evaluated by 50% of the callus growth on the medium with kinetin but without anti-cytokinin

MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice.References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019). MD001 is a dual agonist of peroxisome proliferator-activated receptor α (PPARα) and PPARγ.1 It binds to PPARα and PPARγ (Kds = 9.55 and 0.14 μM, respectively) but does not bind to PPARβ/δ at concentrations up to 500 μM. It increases transcriptional activity of PPARα and PPARγ in a cell-based luciferase reporter assay when used at a concentration of 10 μM. MD001 (10 μM) increases expression of PPARα, PPARγ, and retinoid X receptor (RXR), as well as PPARα and PPARγ target genes, in HepG2 cells. It increases glucose consumption as well as expression of GLUT2 and GLUT4 in HepG2 and 3T3-L1 cells, respectively, in a concentration-dependent manner. MD001 (20 mg/kg) decreases levels of glucose, insulin, free fatty acids, triglycerides, LDL, alanine aminotransferase (ALT), and aspartate aminotransferase (AST) in blood and reduces the size and number of hepatic lipid droplets in diabetic db/db mice. References1. Kim, S.-H., Hong, S.H., Park, Y.-J., et al. MD001, a novel peroxisome proliferator-activated receptor α/γ agonist, improves glucose and lipid metabolism. Sci. Rep. 9(1), 1656 (2019).

MD-222, a pioneering, highly potent PROTAC degrader targeting MDM2, efficiently mediates the rapid degradation of MDM2 protein and activates wild-type p53 within cells, showcasing significant anticancer effects[1][2].

MD2-IN-1 is a Myeloid differentiation protein 2 (MD2) inhibitor with a KD of 189  μM for the recombinant human MD2 (rhMD2).

MD 780236 is a monoamine oxidase-B inhibitor.

MD 220661 is an inhibitor of semicarbazide-sensitive amine oxidase (SSAO), and a substrate of the enzyme.

MD-230254 is an inhibitor of MAO-B.

MD2-TLR4-IN-1 is a myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex inhibitor.

MD102 is a potent inhibitor of Transglutaminase 2 (IC₅₀ ≈ 0.35 μM). By inhibiting TG2 activity, MD102 modulates cancer-related signaling pathways. In cellular models, its effects are associated with p53 stabilization and downregulation of p-AKT and p-mTOR signaling, and it induces apoptosis in cancer cells.

MD13 is a macrophage migration inhibitor (MIF) oriented PROTAC (Ki value: 71 nM). MD13 can be used to study cancer.

MD 770222, the principal plasma O-demethylated metabolite of Cimoxatone, is an orally active selective and reversible inhibitor of MAO A. The potency of MD 770222 is lower than that of Cimoxatone.

MD-700 is an innovative isobenzofuranone that increases LDL receptor expression in HepG2 cells within 4 hours at a concentration of 0.03 microg/ml. MD-700 selectively reduces levels of LDL and very low-density lipoprotein cholesterol.

MDL 101146 is an orally active inhibitor of neutrophil elastase.

MD15 is a negative control for MD13.

MD6a is a melatonin derivative with inhibitory activity against poly(ADP-ribose) polymerase (PARP-1). It maintains protein homeostasis and improves mitochondrial function via the TOR/HSF-1 signaling pathway, providing neuroprotective effects.

MIF degrader MD13 is involved in protein-protein interactions that play key roles in inflammation and cancer. Current strategies to develop small molecule modulators of MIF functions are mainly restricted to the MIF tautomerase active siteMIF degrader MD13. MD13 also exhibits antiproliferative effect in a 3D tumor spheroid model. In conclusion, we describe the first MIF-directed PROTAC (MD13) as a research tool, which also demonstrates the potential of PROTACs in cancer therapy.

2MD, an orally active vitamin D analog, both stimulates periosteal bone formation and decreases trabecular bone resorption, effectively restoring trabecular and cortical bone mass and strength. Additionally, 2MD regulates genes related to intraocular pressure (IOP) and reduces IOP in non-human primates [1] [2].

Anti-Mouse DR5/CD262 Antibody (MD5-1) is an inhibitor derived from a hamster in the United States, specifically targeting the mouse DR5/CD262 as an IgG, κ antibody.

MD01-67 is a macrocyclic compound selectively targeting the neurotensin 2 receptor (NTS2), with a Ki of 2.9 nM. It exhibits analgesic activity and reduces tactile hypersensitivity in rat models of acute, sustained, and chronic inflammatory pain.