L371,257
L371,257 Basic information
- Product Name:
- L371,257
- Synonyms:
-
- L371,257
- 1-[4-[(1-Acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]-4-(2-oxo-2H-3,1-benzoxazin-1(4H)-yl)piperidine
- 1-[1-[4-(1-acetylpiperidin-4-yl)oxy-2-methoxybenzoyl]piperidin-4-yl]-4H-3,1-benzoxazin-2-one
- 2H-3,1-Benzoxazin-2-one, 1-[1-[4-[(1-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]-4-piperidinyl]-1,4-dihydro-
- 257
- L-371
- L371,257,L 371,257
- 1-(1-(4-((1-acetylpiperidin-4-yl)oxy)-2-methoxybenzoyl)piperidin-4-yl)-1,4-dihydro-2H-benzo[d][1,3]oxazin-2-one
- CAS:
- 162042-44-6
- MF:
- C28H33N3O6
- MW:
- 507.58
- Mol File:
- 162042-44-6.mol
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L371,257 Chemical Properties
- Boiling point:
- 728.9±60.0 °C(Predicted)
- Density
- 1.282±0.06 g/cm3(Predicted)
- storage temp.
- Store at RT
- solubility
- Soluble to 10 mM in DMSO with gentle warming
- form
- Powder
- pka
- 0.73±0.20(Predicted)
- color
- White to off-white
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L371,257 Usage And Synthesis
Uses
L-371,257 is a potent antagonist of oxytocin-induced contractions of the rat uterus in vitro and in vivo and has significant oral bioavailability in rats.
Biological Activity
Potent, high affinity human oxytocin (OT) receptor antagonist (K i = 4.6 nM) that displays > 800-fold selectivity over human arginine vasopressin receptors V 1a and V 2 . Antagonizes oxytocin-induced contractions in isolated rat uterine tissue (pA 2 = 8.44) and in anesthetised rats following intravenous and intraduodenal administration. Orally active.
in vivo
Systemic administration of nonpenetrant oxytocin receptor antagonist L-371,257 (0.5 and 1.0 mg/kg; i.p. injection) stimulates weight gain in rats[3].
| Animal Model: | Six-hour fasted rats[3] |
| Dosage: | 0.5 and 1.0 mg/kg |
| Administration: | Intraperitoneal injection (a single) 30-45 minutes prior to the start of the dark cycle and access to food; Intraperitoneal injection (given repeatedly) over 6 days. |
| Result: | A single injection significantly stimulated weight gain at 0.5 and 1.0 mg/kg relative to vehicle treatment. When given repeatedly over 6 days, 0.5 mg/kg significantly stimulated body weight gain (10.5±2.2 g) relative to vehicle treatment (4.7±2.7 g). |
storage
Store at RT
L371,257Supplier
3B Pharmachem (Wuhan) International Co.,Ltd.
- Tel
- 821-50328103-801 18930552037
- 3bsc@sina.com
Shanghai Lollane Biological Technology Co.,Ltd.
- Tel
- 021-52996696，15000506266 15000506266
EMMX Biotechnology LLC
- Tel
- 888-539-0666
- info@emmx.com
Shanghai YuanYe Biotechnology Co., Ltd.
- Tel
- 021-61312847; 18021002903
- 3008007409@qq.com
Shanghai Rechem science Co., Ltd.
- Tel
- 021-31433387 15618786686
- sales@rechemscience.com
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