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45

抑制剂 & 化合物

4

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T8976	PD-089828	EGFR; FGFR; PDGFR; Src	Angiogenesis; JAK/STAT signaling; Tyrosine Kinase/Adaptors
	PD-089828 是受体酪氨酸激酶 FGFR1、PDGFRβ 和 EGFR 的竞争性抑制剂，IC50分别为0.15、1.76 和 5.47 µM。它也是非受体酪氨酸激酶 c-Src 的非竞争性抑制剂，IC50 为 0.18 µM。
T27606	Indantadol HCl CHF-3381,CMP-3381,GT-3381,V-3381,CNP-3381,Indantadol	MAO; NMDAR	Metabolism; Neuroscience
	Indantadol HCl (CHF-3381) 是一种 NMDA 拮抗剂和非选择性 MAO 抑制剂。
T12444	Phentolamine Analogue 1	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Phentolamine Analogue 1 是 phentolamine 类似物。其中Phentolamine 是非选择性alpha-adrenergic 拮抗剂。
T6387	Ampiroxicam CP 65703,Flucam,安吡昔康	COX	Immunology/Inflammation; Neuroscience
	Ampiroxicam (Flucam) 是一种非选择性的环氧化酶抑制剂，有抗炎活性。
T8738	LUN42518 HCl 47142-51-8(free base)	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	LUN42518 HCl 47142-51-8(free base) 是酚妥拉明的类似物。酚妥拉明是一种非选择性的α-肾上腺素能拮抗剂。
T3951	NSC632839 F6,Ubiquitin Isopeptidase Inhibitor II	DUB	Cell Cycle/Checkpoint; DNA Damage/DNA Repair; Ubiquitination
	NSC-632839 (Ubiquitin Isopeptidase Inhibitor II) 是一种非选择性异肽酶抑制剂，可抑制USP2、USP7和SENP2，EC50分别为 45±4 μM、37±1 μM 和 9.8±1.8 μM。
T21389	Enprofylline Enprofilina,3-propylxanthine,3-n-Propylxanthine,Enprofyllinum,恩丙茶碱	Others	Others
	Enprofylline (Enprofilina) 是具有选择性的 A2B 受体竞争性拮抗剂 (Ki:7 μM) ，也是磷酸二酯酶抑制剂。它可用于研究哮喘、慢性阻塞性肺疾病。
T3622	CP-640186 hydrochloride CP 640186 HCl,盐酸CP-640186	Acetyl-CoA Carboxylase	Metabolism
	CP-640186 hydrochloride (CP 640186 HCl) 是膜渗透性的乙酰辅酶A 羧化酶（ACC）抑制剂，抑制大鼠肝脏ACC1和大鼠骨骼肌ACC2的IC50为53 nM 和61 nM。
T64373	CDK1-IN-2 cdk1 inhibitor 2	CDK	Cell Cycle/Checkpoint
	CDK1-IN-2 (cdk1 inhibitor 2)是一种CDK1抑制剂，IC50为5.8μM。CDK1-IN-2的激酶谱显示了多种激酶的非选择性抑制。
T10355	Apyramide	COX	Immunology/Inflammation; Neuroscience
	Apyramide 是一种抗炎试剂 (NSAID)，是吲哚美辛的前药。Indomethacin 是一种强效的、血脑通透的、非选择性的 COX1 和 COX2 抑制剂。
T1889	CP-640186 CP 640186	Acetyl-CoA Carboxylase	Metabolism
	CP-640186 是一种有效的乙酰辅酶 A 羧化酶 (ACC)抑制剂，抑制大鼠肝脏 ACC1 和大鼠骨骼肌 ACC2 的 IC50分别为 53 nM 和 61 nM。
T2137	Ibudilast AV-411,KC-404,MN-166,异丁司特	PDE	Metabolism
	Ibudilast (MN-166) 是一种环腺苷酸磷酸二酯酶 (PDE) 抑制剂，具有抗血小板聚集作用。它能够抑制气管平滑肌收缩性，可用于研究哮喘。它可对抗活化小胶质细胞的神经毒性，可能是一种有效的神经保护和抗痴呆药物。
T1282	Carteolol hydrochloride Arteoptic,Abbott-43326,OPC-1085 hydrochloride,盐酸卡替洛尔,Carteolol HCl,Mikelan	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Carteolol hydrochloride (Abbott-43326) 是一种非选择性的β肾上腺素受体阻断剂。
T1275	Phentolamine mesylate Phentolamine methanesulfonate,甲磺酸酚妥拉明,Phentolamine mesilate	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Phentolamine mesylate (Phentolamine methanesulfonate) 是一种非选择性的、可逆的，具有口服活性的 α1 和 α2 肾上腺素能受体阻滞剂，能够扩张使血管，降低周围血管阻力。它可用于研究嗜铬细胞瘤相关的高血压，心力衰竭和勃起功能障碍。
T20898	(R)-Propranolol hydrochloride Dexpropranolol hydrochloride,(R)-(+)-Propranolol,盐酸普奈洛尔	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	(R)-Propranolol hydrochloride (Dexpropranolol hydrochloride) 是一种抗肾上腺素受体拮抗剂，是一种普萘洛尔的活性较低的对映体。Dexpropranolol 是一种非选择性的β-adrenergic receptor 拮抗剂，对 β1AR 和 β2AR 具有高亲和力。
T4612	NS309	EGFR; Potassium Channel; HER	Angiogenesis; JAK/STAT signaling; Membrane transporter/Ion channel; Tyrosine Kinase/Adaptors
	NS309 是选择性钙依赖性钾离子通道 SK/IK 的激活剂，在 BK 通道上没有激活作用。
TP1910L1	CALP1 acetate CALP1 acetate(145224-99-3 free base)	CaMK	Neuroscience
	CALP1 acetate 是一种钙调蛋白 (CaM) 激动剂（Kd 为 88 µM），可与 CaM EF-hand/Ca2+ 结合位点结合。 CALP1 通过抑制钙通道的开放来阻断钙流入和细胞凋亡（IC50 为 44.78 µM）。 CALP1 阻断谷氨酸受体通道并阻断储存操作的非选择性阳离子通道。 CALP1 激活依赖于 CaM 的磷酸二酯酶活性。
T38240	2,6-Dichlorodiphenylamine	Antibacterial	Microbiology/Virology
	2,6-Dichlorodiphenylamine 是双氯芬酸钠的一种结构类似物，显示出抗白色念珠菌活性。2,6-Dichlorodiphenylamine 是非选择性抗炎剂，为COX 的抑制剂，在 CHO 细胞中，对人 COX-1 和 COX-2 的IC50分别为 4 和 1.3 nM。
T12402L	Penbutolol HOE 893,l-Penbutolol,Levopenbutol,HOE 893D,Betapressin
	Penbutolol is a nonselective beta-blocker utilized as an antihypertensive and an antianginal.
T68488	Indatraline
	Indatraline is a nonselective monoamine transporter inhibitor.
T32699	Levobunolol Levobunololum,Liquifilm,AK-Beta,Betegan
	Levobunolol is a nonselective beta-blocker. It is used topically to treat glaucoma.
T28977	Tilisolol HCl Tilisolol, trade name Selecal,N 696,N-696,N696
	Tilisolol is a nonselective blocker of beta-adrenergic. Tilisolol hydrochloride dilates coronary arteries through an ATP-sensitive K(+)-channel opening mechanism in dogs.
T28024	Metfendrazine NSC 169501,A-17767,A 17767,methphendrazine,A17767
	Metfendrazine is an irreversible and nonselective monoamine oxidase inhibitor (MAOI).
T25144	Benmoxin Neuralex,Nerusil
	Benmoxin is a monoamine oxidase inhibitor (MAOI) that is irreversible and nonselective.
T4560L1	Alprenolol hydrochloride, (S)- L-Alloprenalol hydrochloride
	Alprenolol hydrochloride, (S)- is a nonselective β-blocker. It is also a serotonin 5HT1A receptor antagonist.
T25205	Caroxazone
	Caroxazone is an antidepressant drug, monoamine oxidase inhibitor (MAOI) that is irreversible and nonselective meanwhile.
T24631	Pheniprazine hydrochloride Pheniprazine HCl,NSC 17766,CCRIS 1417,NSC-17766,NSC17766
	Pheniprazine is an irreversible and nonselective monoamine oxidase inhibitor of the hydrazine chemical class. It was also used in the treatment of angina pectoris and schizophrenia.
T37893	3-MPPI
	3-MPPI 是一种高亲和力非选择性 α1 拮抗剂。
T15386	Glisoxepide	Others	Others
	Glisoxepide is a sulphonamide derivative and is an orally available nonselective K(ATP) channel blocker. It has antihyperglycemic activity and cardiovascular regulation effect.
T12550	Propranolol-d7 hydrochloride Propranolol D7 hydrochloride	Others	Others
	Propranolol D7 hydrochloride is a deuterium labeled Propranolol hydrochloride. Propranolol hydrochloride is a nonselective antagonist of β-adrenergic receptor (βAR).
T10371	Arotinolol	5-HT Receptor	GPCR/G Protein; Neuroscience
	Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. It is an antihypertensive agent.
T12701	(rel)-Tranylcypromine D5 hydrochloride 2-Phenylcyclopropylamine D5 hydrochloride	Histone Demethylase	Chromatin/Epigenetic
	(rel)-Tranylcypromine D5 hydrochloride is a deuterium labeled (rel)-Tranylcypromine hydrochloride. (rel)-Tranylcypromine hydrochloride is an irreversible, nonselective inhibitor of monoamine oxidase (MAO) used in the treatment of depression.
T69267	Naproxen glucuronide
	Naproxen glucuronide is a nonsteroidal anti-inflammatory drug (NSAID) of the propionic acid class (the same class as ibuprofen) that relieves pain, fever, swelling, and stiffness. It is a nonselective COX inhibitor.
T40757	1-Stearoyl-2-arachidonoyl-sn-glycerol
	1-Stearoyl-2-arachidonoyl-sn-glycerol, a diacylglycerol (DAG) encompassing polyunsaturated fatty acids, possesses the ability to activate PKC. Moreover, this compound has the potential to enhance nonselective cation channel (NSCC) activity.
T11655	Indomethacin-D4 Indometacin-D4,吲哚美辛-D4	CDK	Cell Cycle/Checkpoint
	Indomethacin-D4 is a deuterium labeled Indomethacin. Indomethacin is a potent and nonselective inhibitor of COX1 and COX2, with IC50s of 18 nM and 26 nM for human COX-1 and COX-2, respectively, in CHO cells.
T11754	Ketorolac-d5 Ketorolac D5	PPAR	DNA Damage/DNA Repair; Metabolism
	Ketorolac D5, a deuterium-labeled version of Ketorolac, is a non-steroidal anti-inflammatory agent that functions as a nonselective COX inhibitor. It exhibits IC50 values of 20 nM for COX-1 and 120 nM for COX-2.
T69031	Cirazoline (free base)
	Cirazoline (free base) is a full agonist at the α1A adrenergic receptor, a partial agonist at both the α1B and α1D adrenergic receptors, and a nonselective antagonist to the α₂ adrenergic receptor. It is believed that this combination of properties could make cirazoline an effective vasoconstricting agent.
T13069	Talabostat isomer mesylate	Others	Others
	Talabostat isomer mesylate is an isomer of talabostat mesylate. Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available inhibitor of dipeptidyl peptidase IV (DPP-IV)(Ki of 0.18 nM).
T69019	Mecamylamine 美加明
	Mecamylamine 是一种具有口服活性，非选择性，非竞争性的nAChR 拮抗剂。Mecamylamine 也是一种神经节阻滞剂，可穿过血脑屏障。Mecamylamine 可用于神经疾病，高血压，抗抑郁的研究。
T76262	Cagrilintide
	Cagrilintide为一种处于研发阶段的新型长效酰化胰岛素类似物，兼具非选择性胰岛素受体(AMYR)与降钙素G蛋白偶联受体(CTR)的激动剂功能。该化合物能显著降低体重并减少食物摄入，展现出针对肥胖疾病的研究潜力。
T37861	Talabostat
	Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8/9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9,...
T21750	A 784168
	A-784168 是一种有效的、口服活性的香草素受体 1 型 (TRPV1) 抑制剂。香草素受体 1 型 (TRPV1) 是一种配体门控非选择性阳离子通道，被认为是各种疼痛刺激 (如内源性脂质、辣椒素、热和低 pH 值) 的重要整合剂。口服给药时，A-784168 具有良好的 CNS 渗透性。
T60704	Loxoprofen sodium (dihydrate)
	Loxoprofen sodium dihydrate 是一种非甾体类口服抗炎药，具有镇痛和解热作用。Loxoprofen sodium dihydrate 显示出抗肿瘤活性，并且可减少动脉粥样硬化。Loxoprofen sodium dihydrate 是COX 的非选择性抑制剂，对 COX-1 和 COX-2 的IC50值分别为 6.5 和 13.5 μM。
T60496	Ketorolac hemicalcium
	Ketorolac (RS37619) hemicalcium 是一种非选择性的 COX 抑制剂，对 COX-1 的 IC50 为 20 nM，对 COX-2 的 IC50 为 120 nM。 Ketorolac hemicalcium 是一种非甾体类抗炎药 (NSAID)，可用作 0.5% 滴眼液，用于研究过敏性结膜炎、黄斑囊样水肿、术中瞳孔缩小和术后眼部炎症和疼痛等。 Ketorolac hemicalcium 也是一种可用于癌症研究的 DDX3 抑制剂 [1] [4]。
T75791	CALP1 TFA
	CALP1 TFA 是一种钙调蛋白 (CaM) 激动剂 (Kd 为 88 µM)，与 CaMEF-hand/Ca2+结合位点结合。CALP1 TFA 通过抑制钙通道 (calcium channel) 的开放来阻止钙的流入和凋亡 (IC50为 44.78 µM)。CALP1 TFA 阻止谷氨酸受体 (glutamate receptor channels) 通道，并阻止存储操作的非选择性阳离子通道。CALP1 TFA 激活 CaM 依赖性磷酸二酯酶 (phosphodiesterase) 活性。

化合物

Cat.No: T8976

Target: EGFR, FGFR, PDGFR, Src

Cat.No: T27606

Synonym: CHF-3381,CMP-3381,GT-3381,V-3381,CNP-3381,Indantadol

Target: MAO, NMDAR

Phentolamine Analogue 1

Cat.No: T12444

Target: Adrenergic Receptor

Cat.No: T6387

Synonym: CP 65703,Flucam,安吡昔康

Target: COX

LUN42518 HCl 47142-51-8(free base)

Cat.No: T8738

Target: Adrenergic Receptor

Cat.No: T3951

Synonym: F6,Ubiquitin Isopeptidase Inhibitor II

Target: DUB

Cat.No: T21389

Synonym: Enprofilina,3-propylxanthine,3-n-Propylxanthine,Enprofyllinum,恩丙茶碱

Target: Others

CP-640186 hydrochloride

Cat.No: T3622

Synonym: CP 640186 HCl,盐酸CP-640186

Target: Acetyl-CoA Carboxylase

Cat.No: T64373

Synonym: cdk1 inhibitor 2

Target: CDK

Cat.No: T10355

Target: COX

Cat.No: T1889

Synonym: CP 640186

Target: Acetyl-CoA Carboxylase

Cat.No: T2137

Synonym: AV-411,KC-404,MN-166,异丁司特

Target: PDE

Carteolol hydrochloride

Cat.No: T1282

Synonym: Arteoptic,Abbott-43326,OPC-1085 hydrochloride,盐酸卡替洛尔,Carteolol HCl,Mikelan

Target: Adrenergic Receptor

Phentolamine mesylate

Cat.No: T1275

Synonym: Phentolamine methanesulfonate,甲磺酸酚妥拉明,Phentolamine mesilate

Target: Adrenergic Receptor

(R)-Propranolol hydrochloride

Cat.No: T20898

Synonym: Dexpropranolol hydrochloride,(R)-(+)-Propranolol,盐酸普奈洛尔

Target: Adrenergic Receptor

Cat.No: T4612

Target: EGFR, Potassium Channel, HER

Cat.No: TP1910L1

Synonym: CALP1 acetate(145224-99-3 free base)

Target: CaMK

2,6-Dichlorodiphenylamine

Cat.No: T38240

Target: Antibacterial

Cat.No: T12402L

Synonym: HOE 893,l-Penbutolol,Levopenbutol,HOE 893D,Betapressin

Cat.No: T68488

Cat.No: T32699

Synonym: Levobunololum,Liquifilm,AK-Beta,Betegan

Cat.No: T28977

Synonym: Tilisolol, trade name Selecal,N 696,N-696,N696

Cat.No: T28024

Synonym: NSC 169501,A-17767,A 17767,methphendrazine,A17767

Cat.No: T25144

Synonym: Neuralex,Nerusil

Alprenolol hydrochloride, (S)-

Cat.No: T4560L1

Synonym: L-Alloprenalol hydrochloride

Cat.No: T25205

Pheniprazine hydrochloride

Cat.No: T24631

Synonym: Pheniprazine HCl,NSC 17766,CCRIS 1417,NSC-17766,NSC17766

Cat.No: T37893

Cat.No: T15386

Target: Others

Propranolol-d7 hydrochloride

Cat.No: T12550

Synonym: Propranolol D7 hydrochloride

Target: Others

Cat.No: T10371

Target: 5-HT Receptor

(rel)-Tranylcypromine D5 hydrochloride

Cat.No: T12701

Synonym: 2-Phenylcyclopropylamine D5 hydrochloride

Target: Histone Demethylase

Naproxen glucuronide

Cat.No: T69267

1-Stearoyl-2-arachidonoyl-sn-glycerol

Cat.No: T40757

Indomethacin-D4

Cat.No: T11655

Synonym: Indometacin-D4,吲哚美辛-D4

Target: CDK

Cat.No: T11754

Synonym: Ketorolac D5

Target: PPAR

Cirazoline (free base)

Cat.No: T69031

Talabostat isomer mesylate

Cat.No: T13069

Target: Others

Cat.No: T69019

Synonym: 美加明

Cat.No: T76262

Cat.No: T37861

Cat.No: T21750

Loxoprofen sodium (dihydrate)

Cat.No: T60704

Ketorolac hemicalcium

Cat.No: T60496

Cat.No: T75791

Cat. No.	Product Name	Target	Signaling Pathways
T0804	Pilocarpine Hydrochloride NSC 5746 HCl,盐酸毛果芸香碱,Pilocarpine HCl,(+)-Pilocarpine hydrochloride	AChR	Neuroscience
	Pilocarpine Hydrochloride (NSC 5746 HCl) 是一种 M3 型毒蕈碱乙酰胆碱受体激动剂，用于制作癫痫实验模型
T1681	Aminophylline 氨茶碱,Phyllocontin	PDE; Adenosine Receptor	GPCR/G Protein; Metabolism; Neuroscience
	Aminophylline (Phyllocontin) 是一种竞争性非选择性磷酸二酯酶抑制剂，具有支气管扩张作用。它是竞争性的腺苷受体拮抗剂，有用于哮喘研究的潜力。
TN4051	Fargesone B	cAMP; Calcium Channel	GPCR/G Protein; Membrane transporter/Ion channel; Metabolism
	Fargesone B inhibits the vascular smooth muscle contraction by suppressing the voltage- and receptor-activated calcium influxes in a nonselective manner.
TCS2185	Yohimbine	Adrenergic Receptor	GPCR/G Protein; Neuroscience
	Yohimbine 是一种有效的、相对非选择性的α2 - 肾上腺素能受体拮抗剂，IC50=0.6μM。

天然产物

Pilocarpine Hydrochloride

Cat.No: T0804

Synonym: NSC 5746 HCl,盐酸毛果芸香碱,Pilocarpine HCl,(+)-Pilocarpine hydrochloride

Target: AChR

Cat.No: T1681

Synonym: 氨茶碱,Phyllocontin

Target: PDE, Adenosine Receptor

Cat.No: TN4051

Target: cAMP, Calcium Channel

Cat.No: TCS2185

Target: Adrenergic Receptor

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