MK-0354
Modify Date: 2024-01-10 09:15:58
MK-0354 structure
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Common Name | MK-0354 | ||
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| CAS Number | 851776-28-8 | Molecular Weight | 176.179 | |
| Density | 1.6±0.1 g/cm3 | Boiling Point | 535.3±60.0 °C at 760 mmHg | |
| Molecular Formula | C7H8N6 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | 273.9±25.8 °C | |
Use of MK-0354MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.IC50 value: 1.65 μM (EC50, for hGPR109a), 1.08 μM (EC50, for mGPR109a) [1]Target: GPR109ain 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 β-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 μM. 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] |
| Name | 3-(2H-Tetrazol-5-yl)-1,4,5,6-tetrahydrocyclopenta[c]pyrazole |
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| Synonym | More Synonyms |
| Description | MK-0354 is a partial agonist of GPR109a receptor, for hGPR109a/ mGPR109a with EC50 of 1.65/1.08 μM, showed no activation of GPR109b.IC50 value: 1.65 μM (EC50, for hGPR109a), 1.08 μM (EC50, for mGPR109a) [1]Target: GPR109ain 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 β-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 μM. 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] |
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| Related Catalog | |
| References |
| Density | 1.6±0.1 g/cm3 |
|---|---|
| Boiling Point | 535.3±60.0 °C at 760 mmHg |
| Molecular Formula | C7H8N6 |
| Molecular Weight | 176.179 |
| Flash Point | 273.9±25.8 °C |
| Exact Mass | 176.081039 |
| PSA | 83.14000 |
| LogP | 0.67 |
| Vapour Pressure | 0.0±1.4 mmHg at 25°C |
| Index of Refraction | 1.709 |
| Storage condition | 2-8℃ |
| Cyclopenta[c]pyrazole, 1,4,5,6-tetrahydro-3-(2H-tetrazol-5-yl)- |
| 3-(2H-Tetrazol-5-yl)-1,4,5,6-tetrahydrocyclopenta[c]pyrazole |
| MK-0354 |