| Identification | Back Directory | [Name]
1,4-Dihydro-4-[3-[[[[3-[4-(3-methoxyphenyl)-1-piperidinyl]propyl]amino]carbonyl]amino]phenyl]-2,6-dimethyl-3,5-pyridinedicarboxylicacid3,5-dimethylesterL-Lactate | [CAS]
186185-03-5 | [Synonyms]
BMS 193885
BMS-193885 >=98% (HPLC)
1,4-dihydro-4-[3-[[[[3-[4-(3-methoxyphenyl)-1-piperidinyl]propyl]amino]carbonyl]amino]phenyl]-2,6-dimethyl-3,5-dimethyl ester-3,5-pyridinedicarboxylic acid
3,5-Pyridinedicarboxylic acid, 1,4-dihydro-4-[3-[[[[3-[4-(3-methoxyphenyl)-1-piperidinyl]propyl]amino]carbonyl]amino]phenyl]-2,6-dimethyl-, 3,5-dimethyl ester
1,4-Dihydro-4-[3-[[[[3-[4-(3-methoxyphenyl)-1-piperidinyl]propyl]amino]carbonyl]amino]phenyl]-2,6-dimethyl-3,5-pyridinedicarboxylicacid3,5-dimethylesterL-Lactate | [Molecular Formula]
C33H42N4O6 | [MDL Number]
MFCD16878998 | [MOL File]
186185-03-5.mol | [Molecular Weight]
590.71 |
| Chemical Properties | Back Directory | [Boiling point ]
707.5±60.0 °C(Predicted) | [density ]
1.188±0.06 g/cm3(Predicted) | [storage temp. ]
Desiccate at +4°C | [solubility ]
DMSO: >10mg/mL | [form ]
powder | [pka]
13.94±0.46(Predicted) | [color ]
light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
BMS 193885, is a potent, and competitive neuropeptide (NPY) Y1 antagonist, that has also displayed 160-fold selectivity over σ1, α1, Y2, Y4 and Y5 receptors respectively. BMS 193885, is also brain penetrant, and able to reduce food intake and body weight through central Y1 inhibition. | [Biological Activity]
BMS-193885 is a potentselective Y1 antagonist th at is active in both acute and chronic animal models of food intake. Although it is active in vivoit is not orally bioavailable due to poor intestinal absorptionso it is not being pursued for pharmaceutical development. BMS-193885 has been used as a pre-clinical proof of concept tool for showing efficacy of Y1 antagonism in treating obesity. | [in vivo]
Acute feeding suppression: BMS-193885 (30-50 μg/5 μL; i.c.v.; single dose) blocks NPY (5 μg, 10 μg)-induced feeding in satious Sprague-Dawley rats[1].
Peripheral feeding suppression: BMS-193885 (10 mg/kg; i.p.; single dose) reduces NPY-induced 1-hour food intake and spontaneous nocturnal food intake in male Sprague-Dawley rats[1][2].
Chronic weight loss: BMS-193885 (10 mg/kg; i.p.; once daily for 44 days) reduces cumulative food intake and weight gain in male Sprague-Dawley rats without tolerance[1].
Cardiovascular safety: BMS-193885 (30 mg/kg; i.v.; single dose) had no serious adverse effects on heart rate and blood pressure in conscious rats and anesthetized dogs[1].
BMS-193885 (5 mg/kg; i.p.; single dose) significantly blocked NPY Y1 receptors in Wistar rats and reduced the effects of NPY injection on cardiopulmonary function[3].
| Animal Model: | Male Sprague-Dawley rats (220-280 g), satiated, with i.c.v. cannula implantation[1] | | Dosage: | 30-50 μg (10% DMSO in sterile Ringer) | | Administration: | i.c.v. injection (5 μL), single dose | | Result: | Significantly reduced NPY-induced 1-h food intake by 57% (30 μg) and 63% (50 μg) compared to vehicle controls. No effect was observed on basal food intake1. |
| Animal Model: | Male Sprague-Dawley rats (220-280 g), satiated[1] | | Dosage: | 10 mg/kg (40% PEG 400 + 60% saline) | | Administration: | i.p. injection, single dose 30 min before dark cycle | | Result: | Reduced NPY-induced 1-h food intake by 33-57% and spontaneous overnight food intake by 29-54% compared to vehicle. |
| Animal Model: | Male Sprague-Dawley rats (220-280 g), naive[1] | | Dosage: | 10 mg/kg BMS-193885 (40% PEG 400 + 60% saline) | | Administration: | i.p. injection daily for 44 days, 2 h before dark cycle | | Result: | Reduced cumulative food intake by 12-15% and suppressed body weight gain by 8.5% compared to vehicle. No tolerance developed, but adhesive peritonitis occurred in some animals. |
| Animal Model: | Conscious male Sprague-Dawley rats (220-280 g); anesthetized dogs[1] | | Dosage: | 30 mg/kg (rats), 10 mg/kg (dogs) (in sterile saline) | | Administration: | i.v. injection, single dose | | Result: | No significant changes in heart rate or blood pressure were observed in rats or dogs. Oral bioavailability was <0.1% due to poor absorption[1]1.
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| [IC 50]
NPY Y1 receptor; NPY Y1 receptor: 3.3 nM (Ki) |
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