RY764
RY764 is an orally active and selective MC4R agonist. RY764 binds human MC4R with IC50 = 8 nM; it stimulates cAMP accumulation with EC50 = 11 nM. RY764 produces mechanism-dependent feeding inhibition and pro-erectile activity in rodent models. RY764 is used in research on obesity and sexual function.
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- No. CAS: 491845-95-5
- Fòrmula: C34H51FN4O3
- Peso molecular:582.79
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
MC4R 11 nM (EC50) |
MC5R 850 nM (EC50) |
MC1R 750 nM (IC50) |
MC3R 942 nM (IC50) |
MC4R 8 nM (IC50) |
MC5R 945 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
8 nM
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Binding affinity to human MC4R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
Binding affinity to human MC4R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
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15982875 |
| CHO | IC50 |
942 nM
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Binding affinity to human MC3R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
Binding affinity to human MC3R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
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15982875 |
| CHO | IC50 |
945 nM
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Binding affinity to human MC5R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
Binding affinity to human MC5R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
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15982875 |
| CHO | IC50 |
750 nM
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Binding affinity to human MC1R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
Binding affinity to human MC1R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
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15982875 |
| CHO | IC50 |
3 nM
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Binding affinity to rat MC4R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
Binding affinity to rat MC4R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
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15982875 |
| CHO | IC50 |
7 nM
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Binding affinity to dog MC4R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
Binding affinity to dog MC4R expressed in CHO cells assessed by competitive displacement of [125I]-NDP-α-MSH.
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15982875 |
| CHO | EC50 |
11 nM
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Agonist activity at human MC4R expressed in CHO cells assessed by cAMP accumulation.
Agonist activity at human MC4R expressed in CHO cells assessed by cAMP accumulation.
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15982875 |
| CHO | EC50 |
850 nM
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Agonist activity at human MC5R expressed in CHO cells assessed by cAMP accumulation.
Agonist activity at human MC5R expressed in CHO cells assessed by cAMP accumulation.
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15982875 |
| CHO | EC50 |
160 nM
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Agonist activity at human MC1R expressed in CHO cells assessed by cAMP accumulation.
Agonist activity at human MC1R expressed in CHO cells assessed by cAMP accumulation.
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15982875 |
| CHO | EC50 |
5 nM
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Agonist activity at rat MC4R expressed in CHO cells assessed by cAMP accumulation.
Agonist activity at rat MC4R expressed in CHO cells assessed by cAMP accumulation.
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15982875 |
| CHO | EC50 |
6 nM
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Agonist activity at mouse MC4R expressed in CHO cells assessed by cAMP accumulation.
Agonist activity at mouse MC4R expressed in CHO cells assessed by cAMP accumulation.
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15982875 |
In Vitro
RY764 exhibits the highest binding affinity for rat and mouse MC4R (IC50 3 nM) and human MC4R (IC50 8 nM), and is selective for hMC3R and hMC5R[1].
RY764 exhibits low irreversible protein binding in rat and human liver microsomes within 30 min, and the NADPH-dependent increase is attenuated by GSH[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL | Vdss | T1/2 | F | Tmax | Cmax |
|---|---|---|---|---|---|---|---|---|
| Rat[2] | 1 mg/kg | i.v. | 46.9 mL/min/kg | 9.6 L/kg | 3.2 h | / | / | / |
| Rat[2] | 20 mg/kg | p.o. | / | / | / | 32 % | 3 h | 0.87 μM |
| Dog[2] | 0.5 mg/kg | i.v. | 6.6 mL/min/kg | 2.3 L/kg | 4.9 h | / | / | / |
| Dog[2] | 2.0 mg/kg | p.o. | / | / | / | 50 % | 1.1 h | 0.91 μM |
| Monkey[2] | 0.5 mg/kg | i.v. | 3.4 mL/min/kg | 0.8 L/kg | 4.6 h | / | / | / |
| Monkey[2] | 2 mg/kg | p.o. | / | / | / | 16 % | 1.3 h | 0.85 μM |
In Vivo
RY764 (20 mg/kg; oral; single administration) produces a significant reduction in food intake in wild-type mice, and this anorectic effect disappears in MC3/4R double knockout mice[1].
RY764 (1 mg/kg; intravenous injection; single administration) enhances electrical stimulation-induced erectile activity in anesthetized male C57BL/6J mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley (male, 12-week-old)[2]
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Dosage:2 mg/kg, 6 mg/kg, and 20 mg/kg
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Administration:p.o.; single administration
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Result:Produced significant food intake reduction at 8 h (39%) and 18 h (37%).
Chemical Information
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No. CAS 491845-95-5
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Peso molecular 582.79
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Fòrmula C34H51FN4O3
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SMILES
CC(C)(C)NC(C1(C2CCCCC2)CCN(CC1)C([C@H](NC([C@H]3[C@]4([H])N(C[C@](CC4)([H])C3)C)=O)CC5=CC=C(C=C5)F)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Ye Z, et al. Discovery and activity of (1R, 4S, 6R)-N-[(1R)-2-[4-cyclohexyl-4-[[(1, 1-dimethylethyl) amino] carbonyl]-1-piperidinyl]-1-[(4-fluorophenyl) methyl]-2-oxoethyl]-2-methyl-2-azabicyclo [2.2. 2] octane-6-carboxamide (3, RY764), a potent and selective melanocortin subtype-4 receptor agonist. Bioorganic & medicinal chemistry letters. 2005 Aug 1;15(15):3501-5. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
RY764 Related Classifications
HY-111131 Related Classifications
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