L-368,899hydrochloride
- Product Name
- L-368,899hydrochloride
- CAS No.
- 148927-60-0
- Chemical Name
- L-368,899hydrochloride
- Synonyms
- L-368899 free base;L-368,899 hydrochlor;(2S)-2-amino-N-[(1R,3S,4S)-7,7-dimethyl-4-[[4-(2-methylphenyl)piperazin-1-yl]sulfonylmethyl]-3-bicyclo[2.2.1]heptanyl]-4-methylsulfonylbutanamide;(2S)-2-Amino-N-[(1S,2S,4R)-7,7-dimethyl-1-[[[4-(2-methylphenyl)-1-piperazinyl]sulfonyl]methyl]bicyclo[2.2.1]hept-2-yl]-4-(methylsulfonyl)butanamide;Butanamide, 2-amino-N-[(1S,2S,4R)-7,7-dimethyl-1-[[[4-(2-methylphenyl)-1-piperazinyl]sulfonyl]methyl]bicyclo[2.2.1]hept-2-yl]-4-(methylsulfonyl)-, (2S)-
- CBNumber
- CB71075242
- Molecular Formula
- C26H42N4O5S2
- Formula Weight
- 554.77
- MOL File
- 148927-60-0.mol
L-368,899hydrochloride Property
- storage temp.
- Store at +4°C
- solubility
- Chloroform (Slightly), Methanol (Slightly), Water (Slightly)
- form
- Solid
- color
- Off-White to Pale Yellow
- Stability:
- Hygroscopic
N-Bromosuccinimide Price
- Product number
- MTB0000022
- Product name
- L-368,899 HYDROCHLORIDE
- Purity
- 95.00%
- Packaging
- 1MG
- Price
- $660.95
- Updated
- 2021/12/16
- Product number
- MTB0000022
- Product name
- L-368,899 HYDROCHLORIDE
- Purity
- 95.00%
- Packaging
- 10MG
- Price
- $823.46
- Updated
- 2021/12/16
L-368,899hydrochloride Chemical Properties,Usage,Production
Uses
L-368,899 Dihydrochloride is an oxytoxin antagonist and may be used in the treatment of early pregnancy failure.
Biological Activity
Potent, non-peptide and orally active oxytocin receptor antagonist (IC 50 = 8.9 nM) that displays > 40-fold selectivity over vasopressin V 1a and V 2 receptors (IC 50 values are 370 and 570 nM respectively). Antagonizes oxytocin-induced uterine contractions in vitro and in vivo .
in vivo
L-368,899 (0.1, 0.3, 1 mg/kg; infused i.v.; single) shows a dose-related antagonism of OT-stimulated uterine contractions with an AD50 value of 0.35 mg/kg in vivo[1].
L-368,899 (3, 10, 30 mg/kg; i.d.; single) inhibits the contractile effects of OT (AD50= 7 mg/kg) with a long (>4 h) duration of action in vivo (AD50: the dose of L-368,899 required to reduce the response to OT by 50%)[1].
L-368,899 (10 mg/kg, p.o.; single) shows bioavailability (AUC 0-6 h) of 35%[1].
L-368,899 (0.54, 1.8, 5.4 mg/kg; i.v.; single) reduces both oxytocin-induced and endogenous increases in plasma PGFM concentration[2].
| Animal Model: | Adult female Sprague-Dawley rats (250-350 g)[1]. |
| Dosage: | 0.1, 0.3, 1 mg/kg |
| Administration: | Infused intravenous injection; single. |
| Result: | Inhibited OT-stimulated uterine contractions with an AD50 value of 0.35 mg/kg. |
| Animal Model: | Adult female Sprague-Dawley rats (250-350 g)[1]. |
| Dosage: | 3, 10, 30 mg/kg |
| Administration: | Intraduodenal; single. |
| Result: | Exhibited a antagonism of OT-stimulated uterine contractions with an AD50 of 7 mg/kg and duration of action more than 4 h. |
| Animal Model: | Adult female Sprague-Dawley rats (250-350 g)[1]. |
| Dosage: | 10 mg/kg |
| Administration: | Oral administration, single. |
| Result: | Showed orally active with bioavailability (AUC 0-6 h) of 35%. |
| Animal Model: | Mature Dorset cross ewes (53-57 kg; Removal of ovaries)[2]. |
| Dosage: | 0.54, 1.8, 5.4 mg/kg (3, 10 and 30 μg/kg/min for 3 h; dissolved in 0.9% saline). |
| Administration: | Intravenous infusion; single. |
| Result: | Led to a significant decrease in both the frequency (from 2.2 to 1.0 episodes/ewe) and amplitude (from 68.8 to 31.8 pg/mL) of episodes of increased plasma concentration of PGFM. |
L-368,899hydrochloride Preparation Products And Raw materials
Raw materials
Preparation Products
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