364071-17-0
364071-17-0 structure
- Name: OT-R antagonist 1
- Chemical Name: OT-R antagonist 1
- CAS Number: 364071-17-0
- Molecular Formula: C28H29N3O4
- Molecular Weight: 471.548
- Catalog: Signaling Pathways GPCR/G Protein Oxytocin Receptor
- Create Date: 2018-05-16 05:23:50
- Modify Date: 2024-01-08 16:07:09
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OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM).IC50 value: 8 nMTarget: oxytocin receptorin vitro: OT-R antagonist 1 inhibitis IP3-Synthesis, rat OT-R (IC50=0.03 uM). [4] OT-R antagonist 1 inhibits phosphodiesterase IV with IC50 = 6.1 μM, a value about 300-fold higher than the affinity for OT-R. OT-R antagonist 1 shows a very clean selectivity profile with specific interaction with OT-R. OT-R antagonist 1 competitively inhibits binding of [3H]oxytocin and the peptide antagonist 125I-ornithine vasotocin analog to human and rat oxytocin receptor expressed in human embryonic kidney 293-EBNA or Chinese hamster ovary cells with nanomolar potency. Selectivity against vasopressin receptor subtypes is >6-fold for V1a and >350-fold for V2 and V1b. [1]in vivo: Oxytocininduced contraction of isolated rat uterine strips is blocked by OT-R antagonist 1 (pA2 = 7.82). In anesthetized nonpregnant rats, single administration of OT-R antagonist 1 by i.v. or oral routes causes dose-dependent inhibition of contractions elicited by repeated injections of oxytocin with ED50 = 3.5 mg/kg i.v. and 89 mg/kg p.o., respectively. OT-R antagonist 1 significantly inhibits spontaneous uterine contractions in pregnant rats near term when administered intravenously or orally. [1]
| Name | OT-R antagonist 1 |
|---|---|
| Synonyms |
2-Pyrrolidinecarboxamide, N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-, (2S,4Z)-
(4Z)-N-[(2S)-2-Hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methyl-4-biphenylyl)carbonyl]-L-prolinamide (4Z)-N-[(2S)-2-Hydroxy-2-phenylethyl]-4-(methoxyimino)-1-[(2'-methylbiphenyl-4-yl)carbonyl]-L-prolinamide LS-192629 |
| Description | OT-R antagonist 1 is a new potent and selective nonpeptide low molecular weight OT-R antagonist. OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM).IC50 value: 8 nMTarget: oxytocin receptorin vitro: OT-R antagonist 1 inhibitis IP3-Synthesis, rat OT-R (IC50=0.03 uM). [4] OT-R antagonist 1 inhibits phosphodiesterase IV with IC50 = 6.1 μM, a value about 300-fold higher than the affinity for OT-R. OT-R antagonist 1 shows a very clean selectivity profile with specific interaction with OT-R. OT-R antagonist 1 competitively inhibits binding of [3H]oxytocin and the peptide antagonist 125I-ornithine vasotocin analog to human and rat oxytocin receptor expressed in human embryonic kidney 293-EBNA or Chinese hamster ovary cells with nanomolar potency. Selectivity against vasopressin receptor subtypes is >6-fold for V1a and >350-fold for V2 and V1b. [1]in vivo: Oxytocininduced contraction of isolated rat uterine strips is blocked by OT-R antagonist 1 (pA2 = 7.82). In anesthetized nonpregnant rats, single administration of OT-R antagonist 1 by i.v. or oral routes causes dose-dependent inhibition of contractions elicited by repeated injections of oxytocin with ED50 = 3.5 mg/kg i.v. and 89 mg/kg p.o., respectively. OT-R antagonist 1 significantly inhibits spontaneous uterine contractions in pregnant rats near term when administered intravenously or orally. [1] |
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| Related Catalog | |
| References |
[3]. William Nadler, et al. Method for preparing pyrrolidine oximes. WO/2005082848/A2. |
| Density | 1.2±0.1 g/cm3 |
|---|---|
| Molecular Formula | C28H29N3O4 |
| Molecular Weight | 471.548 |
| Exact Mass | 471.215820 |
| LogP | 2.80 |
| Index of Refraction | 1.618 |
| Storage condition | 2-8℃ |