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OT-R antagonist 1

CAS No.
364071-17-0
Chemical Name:
OT-R antagonist 1
Synonyms
OT-R antagonist 1;LS-192629(OT-R antagonist 1);Oxytocin receptor antagonist 1;2-PyrrolidinecarboxaMide, N-[(2S)-2-hydroxy-2-phenylethyl]-4-(MethoxyiMino)-1-[(2'-Methyl[1,1'-biphenyl]-4-yl)carbonyl]-, (2S,4Z)-
CBNumber:
CB62626741
Molecular Formula:
C28H29N3O4
Molecular Weight:
471.55
MDL Number:
MOL File:
364071-17-0.mol
Last updated:2024-07-02 08:55:13

OT-R antagonist 1 Properties

storage temp. Store at -20°C
solubility Soluble in DMSO
form Solid
color White to off-white

OT-R antagonist 1 price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
ChemScene CS-5583 OT-Rantagonist1 >98.0% 364071-17-0 1mg $420 2021-12-16 Buy
ChemScene CS-5583 OT-Rantagonist1 >98.0% 364071-17-0 5mg $1188 2021-12-16 Buy
ChemScene CS-5583 OT-Rantagonist1 >98.0% 364071-17-0 10mg $1980 2021-12-16 Buy
Crysdot CD31002086 OT-Rantagonist1 98+% 364071-17-0 5mg $686 2021-12-16 Buy
Crysdot CD31002086 OT-Rantagonist1 98+% 364071-17-0 10mg $1146 2021-12-16 Buy
Product number Packaging Price Buy
CS-5583 1mg $420 Buy
CS-5583 5mg $1188 Buy
CS-5583 10mg $1980 Buy
CD31002086 5mg $686 Buy
CD31002086 10mg $1146 Buy

OT-R antagonist 1 Chemical Properties,Uses,Production

Biological Activity

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

in vitro

OT-R antagonist 1 inhibitis IP3-Synthesis, rat OT-R (IC50=0.03 uM).  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.

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.

OT-R antagonist 1 Preparation Products And Raw materials

Raw materials

Preparation Products

OT-R antagonist 1 Suppliers

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ATK CHEMICAL COMPANY LIMITED
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ShangHai Biochempartner Co.,Ltd 17754423994 17754423994 2853530910@QQ.com China 8014 62
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Fan De(Beijing) Biotechnology Co., Ltd. 15911056312 liming@bio-fount.com China 9730 58
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DC Chemicals 021-58447131 13564518121 sales@dcchemicals.com China 9412 58
Beijing xinyanhui pharmaceutical research and development co., LTD 13969155946 1461866103@qq.com China 16111 58
2-PyrrolidinecarboxaMide, N-[(2S)-2-hydroxy-2-phenylethyl]-4-(MethoxyiMino)-1-[(2'-Methyl[1,1'-biphenyl]-4-yl)carbonyl]-, (2S,4Z)- OT-R antagonist 1 Oxytocin receptor antagonist 1 LS-192629(OT-R antagonist 1) 364071-17-0