Ghrelin receptor agonist HM01 (AC01) | Ghrelin receptor agonist

Chemical Structure : Ghrelin agonist HM01

Ghrelin agonist HM01 (AC01)

Catalog No.: PC-35623Not For Human Use, Lab Use Only.

Ghrelin receptor agonist HM01 (AC01) is a potent, orally bioavailable ghrelin receptor agonist with Ki of 1.42 nM for human GHSR1a receptor and EC50 of 1.3 nM.

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Biological Activity

Ghrelin receptor agonist HM01 (AC01) is a potent, orally bioavailable ghrelin receptor agonist with Ki of 1.42 nM for human GHSR1a receptor and EC50 of 1.3 nM.

AC01 (HM01) increased cardiomyocyte contractility without Ca2+ mobilization through GHSR1a-Gαi signaling in primary murine cardiomyocytes from both healthy and HFrEF mice.

AC01 (HM01) (3 and 10 mg/kg) similarly reversed the decreased 4-h fecal weight and water content in 6-OHDA rats.

AC01 (HM01) crosses the blood-brain barrier and alleviates these alterations suggesting a potential benefit for gastrointestinal (GI) symptoms in Parkinson's disease (PD).

AC01 (HM01) improves cardiac function and autonomic balance in nonhuman primates, shows rapid and sustained inotropic effects across species.

HM01 mimics the neuronal effects of ghrelin in the arcuate nucleus and attenuates anorexia-cachexia syndrome in tumor-bearing rats.

HM01 also attenuates cachexia in mice bearing bolon-26 (C26) tumors.

Physicochemical Properties

M.Wt	402.36
Formula	C19H29Cl2N3O2
Appearance	Solid
CAS No.
Storage	Solide Powder -20 °C 12 Months; 4°C 6 Months	In Solvent -80 °C 6 Months; -20°C 6 Months
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	1-[(1S)-1-(2,3-dichloro-4-methoxyphenyl)ethyl]-3-methyl-3-[(4R)-1-Methyl-3,3-dimethyl-4-piperidyl]urea

References

1. Rudd JA, et al. Front Pharmacol. 2018 Aug 6;9:869.

2. Karasawa H, et al. Neurogastroenterol Motil. 2014 Dec;26(12):1771-82.

3. Villars FO, et al. Int J Mol Sci. 2017 May 5;18(5). pii: E986.

Ghrelin agonist HM01 (AC01)

Biological Activity

Physicochemical Properties

References

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