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2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶

基本属性 生物活性体外研究体内研究 用途与合成方法 供应商 相关产品
2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶
2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶 性质
  • 密度 1.213
  • 储存条件 Desiccate at +4°C
2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶 用途与合成方法
  • 生物活性RS-127445是一种选择性5-HT2B受体拮抗剂,pKi为9.5,pIC50为10.4,比作用于其他5-HT受体选择性高1000倍以上。
  • 体外研究RS-127445 is a novel high affinity, selective 5-HT2B receptor antagonist devoid of detectable intrinsic activity. RS-127445 is found to have nM affinity and 1000 fold selectivity for the 5-HT2B receptor. RS-127445 is thus among the highest affinity, most selective 5- HT2B receptor ligands. RS-127445 potently blocks the 5-HT evoked increase in inositol phosphate formation and blocks the 5-HT evoked increases in intracellular calcium concentrations with a potency 1000 times greater than that of yohimbine.
  • 体内研究RS-127445 is readily absorbed with no obvious dose or route-dependent limitations and rapidly absorbed following both oral and intraperitoneal administration with peak plasma concentrations being achieved within 15 min of dosing. RS-127445 concentration in the plasma are achieved are proportional to the administered dose. RS-127445 administrated at dose of 5 mg/kg with approximately 60% of an intraperitoneal dose and 14% of the oral dose is bioavailable. RS-127445 concentration in the plasma is predicted to fully saturate accessible 5-HT2B receptors can be readily achieved and maintained in the rat. RS-127445 administered at 1 to 10 mg/kg with oral significantly inhibits visceral hypersensitivity up to 35 to 74% provoked by restraint stress. Oral RS-127445 produces a significant suppression of TNBS-induced visceral hypersensitivity (15 to 62% inhibition at 3 to 30 mg/ kg), although RS-127445 has no significant effect on the visceral nociceptive threshold of native rats. RS-127445 administrated orally with 1 to 30 mg/kg also dose -dependently reduce the restraint stress-induced defecation in native and TNBS-treated rats. . RS-127445 inhibits colonic motility and defecation.
2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶供应商更多
  • 公司名称:上海波以尔化工有限公司
  • 联系电话:
  • 产品介绍: 英文名称:RS-127445
    CAS:199864-87-4
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  • 公司名称:武汉易泰科技有限公司上海分公司
  • 联系电话:86-21-50328103 * 801、802、803、804 Mobile:18930552037
  • 产品介绍: 中文名称:2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶
    英文名称:RS 127445 hydrochloride;4-(4-Fluoro-1-naphthalenyl)-6-(1-Methylethyl)-2-pyriMidinaMinehydrochloride
    CAS:199864-87-4
    纯度:99% HPLC 包装信息:1Mg ; 5Mg;10Mg ;100Mg;250Mg ;500Mg ;1g;2.5g ;5g ;10g
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  • 公司名称:安徽联创生物医药股份有限公司
  • 联系电话:0551-68779238 0551-68596338,15856900656
  • 产品介绍: 英文名称:4-(4-Fluoro-1-naphthalenyl)-6-(1-Methylethyl)-2-pyriMidinaMine hydrochloride;RS-127,445
    CAS:199864-87-4
    纯度:99% HPLC 包装信息:5KG;1KG,500G,250G,100,50G,25G,10G 备注:药用级
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  • 公司名称:中华试剂网(上海思域化工)
  • 联系电话:86-21-34053660;34053661
  • 产品介绍: 英文名称:RS-127445
    CAS:199864-87-4
    纯度:>99% 包装信息:5Mg
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  • 公司名称:Wuhan NCE Biomedical Co.,Ltd.
  • 联系电话:4000-027-021 |24 hour enquiry :+86-13986109188 |English:+86-15623472865 |Japanese:+81-08033611988
  • 产品介绍: 英文名称:RS-127445
    CAS:199864-87-3
    纯度:99% HPLC 包装信息:50Mg,100Mg,500Mg,1g,5g,10g,50g,100g,500g,1kg 备注:XYA0259
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"2-氨基-4-(4-氟萘-1-基)-6-异丙基嘧啶"相关产品信息