MK-0354

Hersteller MedChem Express
Kategorie
Typ Inhibitors
Specific against other
Menge 50mg
ArtNr HY-13008-50mg
eClass 6.1 30220300
eClass 9.0 32160605
Lieferbar
CAS No.
851776-28-8
Purity
>98%
MW
1761786
Formula
C7H8N6
Solubility
DMSO: >= 36 mg/mL
Biological Description
MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 uM, showed no activation of GPR109b.
IC50 value: 1.65 uM (EC50, for hGPR109a), 1.08 uM (EC50, for mGPR109a) [1]
Target: GPR109a
in vitro: MK-0354 demonstrated clear and statistically significant partial agonism in the cAMP assays for both the mouse and human receptors with efficacy approximately 60-70% of that of either nicotinic acid or beta-hydroxy butyrate, a putative physiologically relevant ligand for hGPR109a, in the same assay platform. In addition, MK-0354 showed no activation of GPR109b in the cAMP assay at any concentration up to 100 uM. Following these interesting observations, we then prepared a number of other 5, 5-fused pyrazoles analogous to those that showed receptor activity in our earlier studies. MK-0354 appeared to be somewhat unique among the members of the pyrazole tetrazole series in having reasonable receptor activity.[1]
in vivo: MK-0354 retained the plasma free fatty acid lowering effects in mice associated with GPR109a agonism, but did not induce vasodilation at the maximum feasible dose. Moreover, preadministration of MK-0354 blocked the flushing effect induced by nicotinic acid but not that induced by PGD2. This profile made MK-0354 a suitable candidate for further study for the treatment of dyslipidemia.[1] MK-0354 is a GPR109A partial agonist that activates the antilipolytic pathway in adipocytes. The single-dose and multiple-dose pharmacokinetics and pharmacodynamics, as well as tolerability, of MK-0354 were examined in two Phase I studies conducted in healthy male volunteers. The lipid efficacy of MK-0354 was assessed in a Phase II study conducted in male and female patients with dyslipidemia.[2]
Menge: 50mg
Lieferbar: In stock
Listenpreis: 823,57 €
Rabatt: -10,0%
Preis: 741,21 €
Sie sparen: 82,36 €
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