GPCR / G Protein
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SB-334867 free base
Catalog No. A16695 orexin OX1 receptor antagonistSB-334867 free base is a selective non-peptide orexin OX1 receptor antagonist with a pKb value of 7.2. 了解更多 -
MK-4305 (Suvorexant)
Catalog No. A11500 OX receptor 拮抗剂Suvorexant (MK-4305)是OX1R和OX2R的有效,选择性和口服可生物利用的拮抗剂,目前正在临床研究中作为失眠的新疗法。 了解更多 -
Almorexant
Catalog No. A12503 OX 拮抗剂Almorexant (ACT078573)是一种有效的竞争性双重食欲素1受体(OX1)/orexin 2受体(OX2)拮抗剂,对于OX1和OX2的Ki值分别为1.3和0.17 nM。 了解更多 -
MK-3697
Catalog No. A12633 -
JNJ-10397049
Catalog No. A14104 OX2 receptor 拮抗剂JNJ-10397049是orexin-2受体(OX2R)的有效,选择性且可生物利用的拮抗剂(OX2R的KB = 4.5 nM,OX1R的1.1μM)。 了解更多 -
Almorexant HCl
Catalog No. A14286 OX1/OX2 拮抗剂Almorexant HCl是一种活性双重食欲素受体拮抗剂,对OX1和OX2受体3的IC50为6.6 nM和3.4 nM。 了解更多 -
SB-408124 HCl
Catalog No. A15231 OX Receptor 拮抗剂SB408124 Hydrochloride是OX1受体的非肽拮抗剂,全细胞和膜的Ki分别为57 nM和27 nM。表现出比OX2受体高50倍的选择性。 了解更多 -
Orexin 2 Receptor Agonist
Catalog No. A15982 -
MK-1064
Catalog No. A16360 -
MK-6096 (Filorexant)
Catalog No. A13168 Orexin receptor 拮抗剂MK-6096 (Filorexant)是目前正处于失眠临床开发中的口服生物利用型有效且选择性可逆的OX(1)R和OX(2)R拮抗剂。MK-6096表现出对人OX(1)R和OX(2)R的有效结合和拮抗作用(结合时<3 nM,FLIPR中为11 nM),对超过170个受体和 酶。 了解更多 -
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最新产品
TCS-OX2-29 HCl
Catalog No. A17136 -
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GSK1059865
Catalog No. A12401 -
Nemorexant
Catalog No. A12685 Orexin receptor antagonistNemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively. 了解更多 -
Octreotide Acetate
Catalog No. A12782 somatostatin receptor 拮抗剂Octreotide是sst2,sst3和sst5生长抑素受体的肽激动剂。克隆的人类生长抑素受体的IC50/Kd值(nM)为:290-1140(sst1),0.4-2.1(sst2),4.4-34.5(sst3),> 1000(sst4)和5.6-32(sst5)。 了解更多 -
CYN-154806
Catalog No. A13714 -
Senktide
Catalog No. A16945 -
Tradipitant
Catalog No. A16918 -
Befetupitant
Catalog No. A13149 NK1R antagonistBefetupitant is a high-affinity, nonpeptide, competitive tachykinin 1 receptor (NK1R) antagonist. 了解更多 -
Pavinetant
Catalog No. A21174 NK3R antagonistPavinetant (MLE-4901) is a neurokinin-3 receptor (NK3R) antagonist. 了解更多 -
Maropitant
Catalog No. A21473 -
Vofopitant dihydrochloride
Catalog No. A21543 NK1 receptor antagonistVofopitant dihydrochloride (GR 205171A) is a potent, selective and orally available tachykinin neurokinin 1(NK1) receptor antagonist. 了解更多 -
Serlopitant
Catalog No. A21582 Neurokinin-1 (NK-1) receptor antagonistSerlopitant is a selective Neurokinin-1 (NK-1) receptor antagonist. 了解更多 -
Aprepitant (MK-0869)
Catalog No. A10083 neurokinin-1 receptor 拮抗剂Aprepitant (MK-0869)被归类为NK1拮抗剂。已经显示,阿瑞匹坦通过阻止P物质降落在大脑神经元受体上,从而抑制细胞毒性化疗药物引起的急性呕吐和延迟呕吐。还显示出它能增加5-HT3受体拮抗剂恩丹西酮和皮质类固醇地塞米松的活性,它们也可用于预防化学疗法引起的恶心和呕吐。 了解更多 -
MK-0517 (Fosaprepitant)
Catalog No. A11756 neurokinin-1 receptor 拮抗剂MK-0517 (Fosaprepitant,L-758,298)是Aprepitant的水溶性磷酰基前药,它是NK1拮抗剂。 了解更多 -
Vofopitant (GR 205171)
Catalog No. A12793 -
GW679769 (Casopitant)
Catalog No. A13103 -
Ibodutant (MEN 15596)
Catalog No. A13104 tachykinin NK2 receptor 拮抗剂Ibodutant (MEN 15596)是速激肽NK2受体拮抗剂,pKi 值为10.1,用于治疗腹泻型肠易激综合症(IBS-D)。 了解更多 -
Fosaprepitant dimeglumine
Catalog No. A11069 -
Rolapitant
Catalog No. A13680 NK1 receptor 拮抗剂Rolapitant,也称为SCH-619734,是一种选择性的,可生物利用的CNS渗透性神经激肽NK1受体拮抗剂,在呕吐动物模型中显示出行为效应。 了解更多 -
Netupitant
Catalog No. A14428 NK1 receptor 拮抗剂Netupitant是一种选择性的神经激肽1(NK1)受体拮抗剂。它竞争性地结合并阻断中枢神经系统(CNS)中人类物质P/NK1受体的活性,从而抑制内源性速激肽神经肽物质P(SP)的NK1受体结合,这可能导致预防化疗引起的恶心和呕吐(CINV)。 了解更多 -
Talnetant hydrochloride
Catalog No. A15255 NK3 receptor 拮抗剂Talnetant Hydrochloride是一种有效且选择性的NK3受体拮抗剂(ki = 1.4 nM,hNK-3-CHO);对hNK-3受体的选择性是对hNK-2受体的100倍,在浓度高达100 uM时对hNK-1没有亲和力。 了解更多 -
Vorapaxar (SCH 530348)
Catalog No. A12832 PAR-1 拮抗剂Vorapaxar (SCH 530348)是一种有效的口服活性凝血酶受体(PAR-1)拮抗剂,Ki为8.1 nM。 了解更多 -
ML 161
Catalog No. A13495 -
K145
Catalog No. A16288 -
K145 hydrochloride
Catalog No. A16289