Carbamic acid, N-[3-chloro-5-[1-[[6-[2-(5-ethyl-4-methyl-2-thiazolyl)ethyl]-4-(4-morpholinyl)-2-pyridinyl]amino]ethyl]phenyl]-, 1-methylethyl ester
- CAS No.
- 329716-61-2
- Chemical Name:
- Carbamic acid, N-[3-chloro-5-[1-[[6-[2-(5-ethyl-4-methyl-2-thiazolyl)ethyl]-4-(4-morpholinyl)-2-pyridinyl]amino]ethyl]phenyl]-, 1-methylethyl ester
- Synonyms
- J115814;J-115814;UNII-81DP93CF8M;J 115814J-115814;Carbamic acid, N-[3-chloro-5-[1-[[6-[2-(5-ethyl-4-methyl-2-thiazolyl)ethyl]-4-(4-morpholinyl)-2-pyridinyl]amino]ethyl]phenyl]-, 1-methylethyl ester
- CBNumber:
- CB110402462
- Molecular Formula:
- C29H38ClN5O3S
- Molecular Weight:
- 572.16
- MDL Number:
- MOL File:
- 329716-61-2.mol
Carbamic acid, N-[3-chloro-5-[1-[[6-[2-(5-ethyl-4-methyl-2-thiazolyl)ethyl]-4-(4-morpholinyl)-2-pyridinyl]amino]ethyl]phenyl]-, 1-methylethyl ester Properties
Boiling point | 692.9±55.0 °C(Predicted) |
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Density | 1.261±0.06 g/cm3(Predicted) |
pka | 12.93±0.70(Predicted) |
FDA UNII | 81DP93CF8M |
Carbamic acid, N-[3-chloro-5-[1-[[6-[2-(5-ethyl-4-methyl-2-thiazolyl)ethyl]-4-(4-morpholinyl)-2-pyridinyl]amino]ethyl]phenyl]-, 1-methylethyl ester Chemical Properties,Uses,Production
Uses
J-115814 is a potent and selective neuropeptide Y1 antagonist with Ki values of 1.4, 1.8, 1.9, >10000, 620, 6000, >10000 nM for hY1, rY1, mY1, hY2, hY4, hY5, mY6, respectively. J-115814 inhibits feeding behaviors[1].
in vivo
J-115814 (0.3, 1, 3, 10 mg/kg; i.v.) inhibits NPY-induced feeding in SD rats[1].
J-115814 (3, 10, 30 mg/kg; i.p.) shows anorexigenic effect in mice[1].
Animal Model: | db/db and lean C57BL6 mice[1] |
Dosage: | 3, 10, 30 mg/kg |
Administration: | I.p. |
Result: | Decreasesd nocturnal food intake in a dose-dependent manner. |
Animal Model: | SD rats[1] |
Dosage: | 0.3, 1, 3, 10 mg/kg |
Administration: | I.v.; 1 h before ICV NPY |
Result: | Inhibited NPY-induced feeding with significant responses at 3 and 10 mg/kg. |
IC 50
hY1 receptor: 1.4 nM (Ki); rNPY Y1 receptor: 1.8 nM (Ki); mY1: 1.9 nM (Ki); hY4 receptor: 620 nM (Ki); hY5 receptor: 6000 nM (Ki); human Y2 receptor: >10000 nM (Ki); mY6: >10000 nM (Ki)
References
[1] Kanatani A, et al. A typical Y1 receptor regulates feeding behaviors: effects of a potent and selective Y1 antagonist, J-115814. Mol Pharmacol. 2001 Mar;59(3):501-5. DOI:10.1124/mol.59.3.501
Carbamic acid, N-[3-chloro-5-[1-[[6-[2-(5-ethyl-4-methyl-2-thiazolyl)ethyl]-4-(4-morpholinyl)-2-pyridinyl]amino]ethyl]phenyl]-, 1-methylethyl ester Preparation Products And Raw materials
Raw materials
Preparation Products
Carbamic acid, N-[3-chloro-5-[1-[[6-[2-(5-ethyl-4-methyl-2-thiazolyl)ethyl]-4-(4-morpholinyl)-2-pyridinyl]amino]ethyl]phenyl]-, 1-methylethyl ester Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
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TargetMol Chemicals Inc. | support@targetmol.com | United States | 38663 | 58 |
Supplier | Advantage |
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TargetMol Chemicals Inc. | 58 |