For research use only. We do not sell to patients.

OT-R antagonist 1

CAS No. : 364071-17-0

Biological Activity：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 nM
Target: oxytocin receptor
in 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]

Research Area：Endocrinology

Targets：Oxytocin Receptor

Related Small Molecules:L-368,899 hydrochloride;L-372662;L-371,257;Epelsiban;OT antagonist 1;OT-R antagonist 2;Carbetocin;WAY-267464;LIT-001;L-368,899;SHR1653;Retosiban;Barusiban;Cargutocin;OT antagonist 3

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides

About Us:

• MedChemExpress (MCE) offers a wide range of high-quality research chemicals and biochemicals (novel life-science reagents, reference compounds and natural compounds) for scientific use；
• Structurally and synthetically diverse biologically active compounds；
•  roduct quality is the key to our success and we take pride in offering only the highest-grade products.；
• We provide HNMR, LC-MS, HPLC, stability testing and activity assays of our products to clients.；
• Product identity, quality, purity and activity are assured by our robust quality control programs and procedures.；

Structurally and synthetically diverse biologically active compounds；

• Customized order volume ranging from milligrams to kilograms scale；

We provide customer-oriented services. To explore more, please contact us at [email protected]. Our team will gladly assist you.