cachexia

PF-07258669 is a selective melanocortin 4 receptor (MC4) antagonist used in the study of cachexia and loss of appetite.

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.

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.

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.

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

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.

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].

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

Ponsegromab (PF 06946860) is a selective and effective humanized anti-GDF15 antibody inhibitor with anti-cachexic activity. It binds to GDF15, preventing its interaction with GFRAL and disrupting GDF15 GFRAL mediated signaling. Ponsegromab has potential anticancer activity and can be used to treat cancer patients with cancer anorexia cachexia syndrome.

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.

Megestrol Acetate-d3 is a deuterated compound of Megestrol Acetate. Megestrol Acetate 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.

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.

6-Methoxykaempferol is a flavonoid found in brazilian propolis. 6-Methoxykaempferol has anti-proliferative activity against cancer cells, neuroprotective effects on isolated rat brain synaptosomes and reduces glutathione levels. 6-Methoxykaempferol exhibits some lipase activity and may be used in the treatment of cachexia. 6-Methoxykaempferol exhibits some lipase activity and can be used in the treatment of 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].

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.

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].

Macimorelin Acetate (EP-1572), an orally active growth hormone (GH) secretagogue and a ghrelin receptor (GHSR) agonist, stimulates GH release. It is utilized in research focusing on adult growth hormone deficiency (AGHD) and Cancer Anorexia-Cachexia Syndrome (CACS).

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].