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OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 25 mg | Inquiry | 3-6 months | 3-6 months | |
| 50 mg | Inquiry | 3-6 months | 3-6 months | |
| 100 mg | Inquiry | 3-6 months | 3-6 months |
| Description | OT-R antagonist 1 inhibits oxytocin-evoked intracellular Ca2+ mobilization (IC50 = 8 nM). OT-R antagonist 1 is a new effective and selective nonpeptide low molecular weight OT-R antagonist. |
| In vitro | OT-R antagonist 1 inhibits IP3-Synthesis, rat OT-R (IC50=0.03 uM). OT-R antagonist 1 inhibits phosphodiesterase IV (IC50 = 6.1 μM, a value about 300-fold higher than the affinity for 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. OT-R antagonist 1 displays a very clean selectivity profile with specific interaction with OT-R. Selectivity against vasopressin receptor subtypes is >6-fold for V1a and >350-fold for V2 and V1b[1][4]. |
| In vivo | OT-R antagonist 1 significantly inhibits spontaneous uterine contractions in pregnant rats near term when administered intravenously or orally. Oxytocininduced contraction of isolated rat uterine strips is blocked by OT-R antagonist 1 (pA2 = 7.82). OT-R antagonist 1(single administration; i.v. or oral routes) causes dose-dependent inhibition of contractions elicited by repeated injections of oxytocin (ED50 = 3.5 mg/kg i.v. and 89 mg/kg p.o., respectively), in anesthetized nonpregnant rats [1] |
| Synonyms | Oxytocin receptor antagonist 1 |
| Molecular Weight | 471.55 |
| Formula | C28H29N3O4 |
| Cas No. | 364071-17-0 |
| Smiles | C(=O)(N1[C@H](C(NC[C@@H](O)C2=CC=CC=C2)=O)C\C(=N\OC)\C1)C3=CC=C(C=C3)C4=C(C)C=CC=C4 |
| Relative Density. | no data available |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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