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SB-705498

生物活性 体外研究 体内研究

CAS号: 501951-42-4
英文名称: SB-705498
英文同义词: SB-705498;1-(2-Bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)-2-pyridyl]pyrrolidin-3-yl]urea;(R)-1-(2-bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)urea;N-(2-Bromophenyl)-N'-[(3R)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl]urea
中文名称: SB-705498
中文同义词: CS-279;N-(2-溴苯基)-N'-[(3R)-1-[5-(三氟甲基)-2-吡啶基]-3-吡咯烷基]脲
CBNumber: CB22628383
分子式: C17H16BrF3N4O
分子量: 429.2343496
MOL File: 501951-42-4.mol
SB-705498化学性质
密度 : 1.59
安全信息

SB-705498 性质、用途与生产工艺

生物活性
SB705498是一种hTRPV1拮抗剂,抑制TRPV1的Capsaicin,酸和热激活,IC50分别为3 nM, 0.1 nM和6 nM,该作用具有一定的电压依赖性,作用于TRPV1比作用于TRPM8选择性高100倍以上。Phase 2。
体外研究
SB705498 (0.3 nM-1 μM) potently inhibits capsaicin-induced activation of human TRPV1 expressed in 1321N1 cells or HEK293 cells with apparent pKi of 7.5 or 7.6, respectively. Coapplication of 100 nM SB705498 rapidly, completely and reversibly inhibits hTRPV1 expressed in HEK293 cells. SB705498 has no significant effect on endogenous [Ca2+] responses in HEK293 cells produced by muscarinic acetylcholine receptor activation with carbachol or store-operated channel-mediated Ca2+ entry after depletion of intracellular stores with the Ca2+ pump inhibitor thapsigargin. SB705498 (10 pM-1 μM) also has no significant antagonist effect versus the close TRPV1 receptor paralog TRPV4 transiently expressed in HEK293 cells and activated using the synthetic ligand 4α-phorbol-12,13-didecanoate (10 μM). SB705498 reveals good antagonist potency against both the rat and guinea pig TRPV1. SB705498 antagonizes rat and guinea pig TRPV1 with pKi of 7.5 and 7.3, respectively. Coapplication of 100 nM to 10 μM SB705498 to the steady state of a maintained capsaicin response leads to rapid and complete inhibition of hTRPV1 at -70 mV. SB705498 inhibits capsaicin-mediated activation of hTRPV1 with IC50 of 3 nM and 17 nM at positive and negative holding potentials (-70 mV and + 70 mV), respectively. Coapplication of 1 μM SB705498 to the plateau period of the response produces complete and reversible inhibition of the TRPV1-mediated conductance. SB705498 shows approximately equal activity versus multiple and diverse chemical and physical modes of TRPV1 receptor activation. SB705498 shows little or no activity versus a wide range of ion channels, receptors and enzymes. SB705498 produces full blockade of heat as well as pH activation of hTRPV1.
体内研究
SB705498 exhibits potent and reversible blockade against the multiple modes of TRPV1 activation, namely the vanilloid (capsaicin), heat- and acid-mediated activation of the receptor. SB705498 displays excellent activity at 10 and 30 mg/kg po with good reversal of allodynia. SB705498 is also shown to give 80% reversal of allodynia in the guinea pig FCA model at 10 mg/kg p.o..
SB-705498 上下游产品信息
上游原料
下游产品
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501951-42-4, SB-705498 相关搜索:
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Inhibitors 其他 小分子抑制剂,天然产物 C17H16BrF3N4O CS-279 N-(2-溴苯基)-N'-[(3R)-1-[5-(三氟甲基)-2-吡啶基]-3-吡咯烷基]脲 501951-42-4 N-(2-Bromophenyl)-N'-[(3R)-1-[5-(trifluoromethyl)-2-pyridinyl]-3-pyrrolidinyl]urea SB-705498 1-(2-Bromophenyl)-3-[(3R)-1-[5-(trifluoromethyl)-2-pyridyl]pyrrolidin-3-yl]urea (R)-1-(2-bromophenyl)-3-(1-(5-(trifluoromethyl)pyridin-2-yl)pyrrolidin-3-yl)urea
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