cachexia

Megestrol acetate (BDH1298) is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.

Aliskiren hemifumarate (CGP60536B) is an orally active nonpeptide renin inhibitor with antihypertensive activity.

Ponsegromab (PF 06946860) is a selective and potent humanized anti-GDF15 antibody inhibitor with IC₅₀ values of 0.123 nM, 0.053 nM, and 0.102 nM for human, rhesus macaque, and mouse targets, respectively. Ponsegromab exhibits anti-cachexia activity by binding to GDF15 to prevent its interaction with GFRAL, thereby disrupting GDF15/GFRAL-mediated signaling. Ponsegromab possesses potential anticancer activity and may be used to treat cancer patients with cancer anorexia-cachexia syndrome. Ponsegromab acts as a chemopreparative agent, increasing intracellular reactive oxygen species levels and reducing glutathione levels.

Salidroside is a bioactive phenolic glycoside compound isolated from Rhodiola rosea and is a prolyl endopeptidase inhibitor. Salidroside can alleviate cachexia symptoms in a tumor cachexia mouse model by activating mTOR signaling and protect dopaminergic neurons by enhancing PINK1/Parkin-mediated mitochondrial autophagy. Salidroside can also inhibit the growth of cancer cells by regulating the CDK4-cyclin D1 pathway to block the G1 phase and/or regulating the Cdc2-cyclin B1 pathway to block the G2 phase.

Relamorelin(BIM28131, RM131) is a selective and potent ghrelin/growth hormone secretagogue receptor (GHSR) agonist with high affinity for GHS-1a receptor (Ki value is 0.42 ± 0.063 nM). Relamorelin(BIM28131, RM131) is also a centrally permeable pentapeptide analog that can increase growth hormone levels and accelerate gastric emptying, and has the potential to study cachexia.

PF-07258669 is a small-molecule compound and a melanocortin 4 receptor (MC4R) antagonist (IC50 = 13 nM, Ki = 0.46 nM) with high selectivity, oral bioavailability, and favorable pharmacokinetic properties. This compound can be used for research on diseases such as cachexia and anorexia.

Ostarine (MK-2866) is a non-steroidal agent with anabolic activity. Selective androgen receptor modulator (SARM) GTx-024 is designed to work like testosterone, thus promoting and/or maintaining libido, fertility, prostate growth, and muscle growth and strength. Mimicking testosterone's action, this agent may increase lean body mass, thereby ameliorating muscle wasting in the hypermetabolic state of cancer cachexia.

ZIP14-IN-1 is a selective inhibitor of ZIP14. It can significantly inhibit the activity of ZIP14, but has no significant effect on ZIP8 (SLC39A8). ZIP14-IN-1 can effectively block the uptake of various divalent metal ions including zinc, iron, manganese and cadmium mediated by ZIP14. Its mechanism of action is to bind to the binding pocket formed at the dimer interface of ZIP14, thereby interfering with the metal ion transport pathway. In addition, ZIP14-IN-1 can reduce the levels of reactive oxygen species (ROS) and lipid peroxidation, alleviate metal-induced cytotoxicity, and can be used in related research on cancer cachexia .

MCL0129, a selective and non-peptidergic melanocortin 4 (MC4) receptor antagonist, is a potential treatment for cachexia.

Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for its potential applications in research related to cachexia, gastroparesis, and gastric/intestinal dysmobility disorders [4] [5].

Aliskiren (CGP 60536; CGP60536B; SPP 100) hydrochloride is a selective, orally active renin inhibitor with an IC50 of 1.5 nM, used in the treatment of cachexia.

Macimorelin acetate is an orally active agonist of the GHSR (Growth Hormone Secretagogue Receptor) and functions as a growth hormone (GH) secretagogue. As a ghrelin mimetic, it potently stimulates the release of endogenous growth hormone by binding to GHSR. Macimorelin acetate is clinically utilized as a diagnostic tool for Adult Growth Hormone Deficiency (AGHD) and is being investigated for the treatment of Cancer Anorexia-Cachexia Syndrome (CACS). Additionally, it has shown potential in neurological research for suppressing seizure activity.

Aliskiren fumarate, an orally active, highly potent, and selective renin inhibitor with an IC50 of 1.5 nM, is utilized in the research of hypertension, cardiovascular diseases, and cancer cachexia.

Relamorelin (RM-131) TFA, a pentapeptide ghrelin analog, is a potent and selective agonist for the ghrelin/growth hormone secretagogue receptor (GHSR), exhibiting a K_i of 0.42 nM for the GHS-1a receptor. This compound can cross the blood-brain barrier and effectively increases growth hormone levels while promoting faster gastric emptying, showing significant research potential for conditions such as cachexia, gastroparesis, and disorders related to gastric/intestinal motility [1] [2] [3] [4] [5].

TCMCB07, a cyclic nonapeptide, serves as an orally active, brain-penetrant antagonist of the melanocortin receptor 4 (MC4R), with significant implications in the management of cachexia [1].

TCMCB07 acetate(1456699-27-6 Free base), a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 TFA plays an important role in cachexia.

TCMCB07 TFA is a cyclic nonapeptide and an orally active, brain-penetrating antagonist of the melanocortin receptor 4 (MC4R), playing a significant role in managing cachexia [1].

Compound 1, identified as a GPR61 inverse agonist, exhibits an IC50 of 11 nM, rendering it suitable for metabolism and body weight disorder research, including obesity and cachexia [1].

NAT1-IN-1 (compound 350) is a potent inhibitor targeting N-acetyltransferase 1 (NAT1), with an IC50 of 44 nM. It is applicable in the study of diseases characterized by metabolic hyperactivity, such as amyotrophic lateral sclerosis, cancer cachexia, and sepsis.

Anti-ACVR2B Antibody is a highly specific monoclonal antibody targeting the human activin receptor type IIB (ACVR2B). The compound binds to the extracellular domain of ACVR2B to effectively block signaling mediated by ligands such as activin and myostatin, thereby inhibiting downstream Smad2/3 phosphorylation. In experimental research, it serves as a critical tool for modulating muscle mass and metabolic homeostasis to investigate muscle atrophy, osteoporosis, and cancer-associated cachexia.

Anti-INHBB/Activin B Antibody is a monoclonal antibody specifically targeting the inhibin subunit beta B (INHBB). The INHBB subunit homodimerizes to form Activin B, a member of the TGF-β superfamily involved in regulating cell proliferation, differentiation, apoptosis, and various pathological processes. By specifically binding to INHBB, this antibody blocks the interaction of Activin B with its receptors, thereby inhibiting the activation of the Smad2/3 signaling pathway. In experimental research, this antibody is frequently utilized to study liver fibrosis, muscle wasting (cachexia), and the progression mechanisms of various tumors.

Megestrol Acetate-D3 is a deuterated compound of Megestrol Acetate. Megestrol Acetate (T1284) has a CAS number of 595-33-5. Megestrol acetate is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.

Megestrol acetate (Standard) is the standard substance of Megestrol acetate, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Megestrol acetate (BDH1298) is a progestogen with actions and uses similar to those of the progestogens in general. Megestrol acetate also has anti-androgenic properties. It is given by mouth in the palliative treatment or as an adjunct to other therapy in endometrial carcinoma and in breast cancer. Megestrol acetate has been approved to treat anorexia and cachexia.

Salidroside (Standard) is a reference standard for research and analysis in studies involving Salidroside. Salidroside is a bioactive phenolic glycoside compound isolated from Rhodiola rosea and is a prolyl endopeptidase inhibitor. Salidroside can alleviate cachexia symptoms in a tumor cachexia mouse model by activating mTOR signaling and protect dopaminergic neurons by enhancing PINK1/Parkin-mediated mitochondrial autophagy. Salidroside can also inhibit the growth of cancer cells by regulating the CDK4-cyclin D1 pathway to block the G1 phase and/or regulating the Cdc2-cyclin B1 pathway to block the G2 phase.