OT-R antagonist 1 (Synonyms: Oxytocin receptor antagonist 1) |
| カタログ番号GC36823 |
OT-R アンタゴニスト 1 は、新しい強力で選択的な非ペプチド低分子量 OT-R アンタゴニストです。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 364071-17-0
Sample solution is provided at 25 µL, 10mM.
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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]
[1]. Serge Halazy, et al. Pharmaceutically active pyrrolidine derivatives as bax inhibitors. WO/2001072705/A1. [2]. Cirillo R, et al. Pharmacology of (2S,4Z)-N-[(2S)-2-hydroxy-2-phenylethyl]-4-(methoxyimino) -1-[(2'-methyl[1,1'-biphenyl]-4-yl)carbonyl]-2-pyrrolidinecarboxamide, a new potent and selective nonpeptide antagonist of the oxytocin receptor. J Pharmacol Exp Ther. 2003 Jul;306(1):253-61. [3]. William Nadler, et al. Method for preparing pyrrolidine oximes. WO/2005082848/A2. [4]. Serge Halazy, et al. Pharmaceutically active pyrrolidine derivatives as bax inhibitors.WO/2001074769/A1.
| Cas No. | 364071-17-0 | SDF | |
| 同義語 | Oxytocin receptor antagonist 1 | ||
| Canonical SMILES | O=C([C@H](C/1)N(C(C2=CC=C(C3=CC=CC=C3C)C=C2)=O)CC1=N/OC)NC[C@@H](O)C4=CC=CC=C4 | ||
| Formula | C28H29N3O4 | M.Wt | 471.55 |
| 溶解度 | DMSO : 100 mg/mL (212.07 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1207 mL | 10.6033 mL | 21.2067 mL |
| 5 mM | 0.4241 mL | 2.1207 mL | 4.2413 mL |
| 10 mM | 0.2121 mL | 1.0603 mL | 2.1207 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 4 reference(s) in Google Scholar.)
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