Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T8439 |
Clobenpropit dihydrobromide
|
Apoptosis; Histamine Receptor | Apoptosis; GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Clobenpropit dihydrobromide 是一种组胺H3R 拮抗剂/反向激动剂。它与 5-HT3 受体和 α2A/α2C 肾上腺素受体结合,对组胺H4受体起部分激动剂的作用,还能促进凋亡。 | |||
T14087 |
ABT-239
|
TRP/TRPV Channel | Membrane transporter/Ion channel |
ABT-239是一种新型、高效、非咪唑类H3R 拮抗剂,也是一种TRPV1拮抗剂。 | |||
T32191 |
Irdabisant
CEP-26401,CEP 26401,CEP26401 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
Irdabisant (CEP-26401) 是选择性、口服活性和血脑屏障渗透性的组胺 H3 受体 (histamine H3 receptor, H3R) 拮抗剂/逆激动剂。Irdabisant 显示人 H3R 和大鼠 H3R 的 Ki 分别为 2.0 nM 和 7.2 nM。Irdabisant 抑制 hERG 电流的活性相对较低 (IC50= 13.8 μM)。在大鼠社会认知模型中,Irdabisant 具有认知增强和唤醒作用。Irdabisant 可用于研究精神分裂症或认知障碍。 | |||
T8514 |
LML134
LML-134 |
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
LML134 (LML-134) 是一种可口服的高选择性组胺 H3 受体反向激动剂,有用于过度睡眠障碍的潜力,对 hH3R 的 cAMP 和 bdg 的Kis 分别为 0.3 和 12 nM。 | |||
T11531 |
H3R-IN-1 Hydrochloride
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
H3R-IN-1 Hydrochloride 是一种有效的组胺H3受体 (H3R) 的反向激动剂。 | |||
T11532 |
H4R antagonist 1
|
Histamine Receptor | GPCR/G Protein; Immunology/Inflammation; Neuroscience |
H4R antagonist 1 is a highly selective histamine H4 receptor (H4R) antagonist (IC50: 27 nM). H4R antagonist 1 does not show any noticeable binding affinity to other subtypes of histamine receptors, H1R, H2R, and H3R. | |||
T61603 | H3R antagonist 2 | ||
H3R antagonist 2 (Compound 23) is a multitarget histamine H3 receptor antagonist. It exhibits inhibitory effects on acetylcholinesterase, butyrylcholinesterase, and human monoamine oxidase B (hMAO B) with IC50 values of 180 nM, 880 nM, and 775 nM, respectively. With a Ki of 170 nM for hH3R, H3R antagonist 2 demonstrates favorable anti-neuropathic pain and memory-enhancing effects. Additionally, it can cross the blood-brain barrier (BBB) [1]. | |||
T28275 |
OUP-186
OUP186 |
||
OUP-186 is a high affinity and human/rat species-selective antagonist of histamine H3 receptor. OUP-186 suppressed the proliferation of breast cancer cells. The IC50 values at 48 hours for OUP-186 was approximately 50 μM. OUP-186 potently induced cell dea | |||
T61197 |
Irdabisant hydrochloride
|
||
Irdabisant (CEP-26401) hydrochloride 是一种选择性、口服活性的组胺H3受体拮抗剂/逆激动剂,具备良好的血脑屏障渗透性。该化合物对大鼠和人类的H3受体具有高亲和力,其Ki值分别为7.2 nM和2.0 nM。此外,Irdabisant hydrochloride在抑制hERG电流方面表现出较低的活性,IC50为13.8 μM。在大鼠社会认知模型中,它展现了认知增强和唤醒的效果,可作为精神分裂症或认知障碍研究的潜在工具。 |