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Search Results for " constriction "

17

抑制剂 & 化合物

2

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T23316	SB 218795	Neurokinin receptor	GPCR/G Protein; Neuroscience
	SB 218795 是一种有效的特异性 NK3 拮抗剂，对 hNK3 的 Ki 为 13 nM，比 hNK2 和 hNK1 的特异性高约 90 倍和 7000 倍。
T15781	LP-935509	Serine/threonin kinase; AAK1 (AP2 associated kinase 1)	Cell Cycle/Checkpoint; Metabolism; Neuroscience
	LP-935509 是一种选择性的、具有脑渗透的、小分子的衔接蛋白-2 相关激酶1 (AAK1) ATP 竞争性抑制剂，其 IC50=3.3 nM，Ki=0.9 nM。它是一种 BIKE 的有效抑制剂 (IC50=14 nM) 和中度的 GAK 抑制剂 (IC50=320 nM)。它能够逆转 SNL 手术后的疼痛。
T4369	SCH-23390 hydrochloride R-(+)-SCH23390 hydrochloride	Potassium Channel; Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	SCH-23390 hydrochloride (R-(+)-SCH23390 hydrochloride) 是一种选择性多巴胺 D1样受体拮抗剂，对 D1和 D5受体的Ki 分别为 0.2 和 0.3 nM。它还抑制 G 蛋白偶联的内向整流钾通道，IC50为 268 nM。它与5-HT2和5-HT1C 受体具有高亲和力，是人5-HT2C 受体激动剂，Ki 为 9.3 nM。
T12865	SCH-23390 maleate R-(+)-SCH-23390 maleate	Potassium Channel; Dopamine Receptor; 5-HT Receptor	GPCR/G Protein; Membrane transporter/Ion channel; Neuroscience
	SCH-23390 maleate (R-(+)-SCH-23390 maleate) 是多巴胺D1样受体选择性拮抗剂，与D1和D5受体结合的Ki 分别为 0.2 nM 和 0.3 nM。它也是人5-HT2C 受体激动剂，Ki 为 9.3 nM。它与5-HT2和5-HT1C 受体具有高亲和力。它还抑制 G 蛋白偶联的内向整流钾通道，IC50为 268 nM。
T10101	Calcium channel-modulator-1	Others; Calcium Channel	Membrane transporter/Ion channel; Metabolism; Others
	Calcium channel-modulator-1是钙离子通道调节剂(IC50:0.8 μM)，具有阻塞主动脉收缩的专业化。
T33868	Palmitoyl glutamic acid N-Palmitoyl-L-glutamic acid,Palmitoylglutaminic acid
	Palmitoyl glutamic acid (N-Palmitoyl-L-glutamic acid) 是一种酰基氨基酸，可阻断主动脉收缩,可拮抗由氟哌啶醇诱发的口腔运动障碍。Palmitoyl glutamic acid 常常添加在化妆品中。
T7391	SAR407899	ROCK; Rho	Cell Cycle/Checkpoint; Cytoskeletal Signaling; Stem Cells
	SAR407899 是一种选择性的 ATP 竞争性ROCK 抑制剂，对ROCK-2的IC50值为 135 nM，对人和大鼠ROCK-2的Ki 值分别为 36 和 41 nM。它是 Rho 激酶抑制剂，有效抑制 endothelin-1 诱导的肾阻力动脉收缩。
T68090	Laprafylline	Others	Others
	Laprafylline 是一种黄嘌呤化合物，对体内支气管收缩有抑制作用，且具有抗肿瘤活性。Laprafylline在低浓度时可充当竞争性血清素能拮抗剂，在高难度时抑制由hist引起的收缩。
T0397	Tetrahydrozoline 四氢唑林,四氢唑啉,Tetryzolin,Tetryzoline	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Tetrahydrozoline (Tetryzoline) 是一种咪唑啉的衍生物，是一种 α-肾上腺素能 (α-adrenergic) 激动剂，能引起血管收缩，广泛用于研究鼻充血、结膜充血。
T1092	Zolmitriptan 佐米曲普坦,311C90,BW-311C90	5-HT Receptor	GPCR/G Protein; Neuroscience
	Zolmitriptan (311C90) 是一种5-HT1B/1D 受体部分激动剂，可用于偏头痛的研究，对 5-HT1B、5-HT1D、5-HT1F 受体的Ki 分别为 5.01、0.63 和 63.09 nM。
T68173	ZD-2138 Ici-D2138	Lipoxygenase	Metabolism
	ZD-2138是一种有效且具有选择性的5-脂氧合酶（5-LOX）的特异性抑制剂，抑制了过敏原诱导的肺支气管收缩，可减少豚鼠孤立气道的神经诱发性快速激肽能收缩。ZD-2138可用来治疗哮喘疾病。
T0871	Noradrenaline bitartrate	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Noradrenaline bitartrate 直接作用于 α 和 β 肾上腺素能受体。它是去甲肾上腺素的酒石酸氢盐，去甲肾上腺素是一种合成苯乙胺，可模拟内源性去甲肾上腺素的拟交感神经作用。临床上，去甲肾上腺素用作外周血管收缩剂，通过其α-肾上腺素能作用导致动脉和静脉床收缩。它还被用作通过其 β-1 肾上腺素能作用介导的强效正性肌力和变时性心脏刺激剂。
T30835	Cgp 45715A Cgp45715A,Cgp-45715A
	CGP 45715A (irukostat) is a potent peptide-leukotriene antagonist used to treat respiratory diseases by antagonizing the bronchial constriction, mucus secretion, and inflammatory effects of these leukotrienes.
T15449	GW-406381	COX	Immunology/Inflammation; Neuroscience
	GW406381 is a highly selective inhibitor of cyclooxygenase-2 (COX-2). GW406381 also attenuates spontaneous ectopic discharge in the sural nerves of rats following chronic constriction injury.
T30827	Cgp 33304 Cgp-33304,Cgp33304
	CGP 33304 is a dual leukotriene receptor antagonist and phospholipase A2 inhibitor. It prevents hypoxia secondary to bronchial constriction induced by leukotriene in a shocking state.
T70280	KB-R7785
	KB-R7785 is a novel ADAM12 and MMP inhibitor, ameliorating cardiac function in a transverse aortic constriction (TAC) model by inhibiting the proteolytic activation of HB-EGF signaling, exerting its antidiabetic effect by ameliorating insulin sensitivity through the inhibition of TNF-alpha production.
T3443	Argiprestocin 精氨缩宫素,Arginine vasotocin	Others	Others
	Argiprestocin (Arginine vasotocin) 也称为抗利尿激素，在维持渗透压中起关键作用。它是在大多数哺乳动物中发现的一种神经垂体激素。用于引起血管收缩的药物。

化合物

Cat.No: T23316

Target: Neurokinin receptor

Cat.No: T15781

Target: Serine/threonin kinase, AAK1 (AP2 associated kinase 1)

SCH-23390 hydrochloride

Cat.No: T4369

Synonym: R-(+)-SCH23390 hydrochloride

Target: Potassium Channel, Dopamine Receptor, 5-HT Receptor

SCH-23390 maleate

Cat.No: T12865

Synonym: R-(+)-SCH-23390 maleate

Target: Potassium Channel, Dopamine Receptor, 5-HT Receptor

Calcium channel-modulator-1

Cat.No: T10101

Target: Others, Calcium Channel

Palmitoyl glutamic acid

Cat.No: T33868

Synonym: N-Palmitoyl-L-glutamic acid,Palmitoylglutaminic acid

Cat.No: T7391

Target: ROCK, Rho

Cat.No: T68090

Target: Others

Tetrahydrozoline

Cat.No: T0397

Synonym: 四氢唑林,四氢唑啉,Tetryzolin,Tetryzoline

Target: Adrenergic Receptor

Cat.No: T1092

Synonym: 佐米曲普坦,311C90,BW-311C90

Target: 5-HT Receptor

Cat.No: T68173

Synonym: Ici-D2138

Target: Lipoxygenase

Noradrenaline bitartrate

Cat.No: T0871

Target: Adrenergic Receptor

Cat.No: T30835

Synonym: Cgp45715A,Cgp-45715A

Cat.No: T15449

Target: COX

Cat.No: T30827

Synonym: Cgp-33304,Cgp33304

Cat.No: T70280

Cat.No: T3443

Synonym: 精氨缩宫素,Arginine vasotocin

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T5014	Prostaglandin E2 地诺前列酮,前列腺素 E2,PGE2,Dinoprostone,Prostaglandin E2 (PGE2)	Endogenous Metabolite; Prostaglandin Receptor	GPCR/G Protein; Immunology/Inflammation; Metabolism
	Prostaglandin E2 (PGE2) 是一种天然激素，参与人体内的各种生理过程，包括平滑肌收缩和放松、调节血管扩张和收缩、调节血压和炎症调节。
T2S0118	Daurinoline	Calcium Channel; 5-HT Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; Neuroscience
	Daurinoline is a non-competitive antagonist, it exerts marked relaxation effect on basilar artery of rabbits through non-competitive antagonism, it would have a protective function on microcirculation of cerebral pia mater, which may be beneficial to relieve cerebral ischemic injury. Daurinoline could significantly reverse noradrenaline induced constriction of pial arterioles and venules, and increase the number of blood vessels which were decreased by noradrenaline.

天然产物

Prostaglandin E2

Cat.No: T5014

Synonym: 地诺前列酮,前列腺素 E2,PGE2,Dinoprostone,Prostaglandin E2 (PGE2)

Target: Endogenous Metabolite, Prostaglandin Receptor

Cat.No: T2S0118

Target: Calcium Channel, 5-HT Receptor, Histamine Receptor

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