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Search Results for " ca2+ influx "

30

抑制剂 & 化合物

9

天然产物

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Cat. No.	Product Name	Target	Signaling Pathways
T6777	Bay K 8644 (±)-BAY-K-8644,SQ 28,873	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	Bay K 8644 (SQ 28,873)是一种二氢吡啶化合物，是一种选择性的 L 型 Ca2+ 通道激活剂，IC50 为 17.3 nM。它通过增加通道的开放时间来增加通过肌膜 Ca2+通道的 Ca2+流入。
T0370	Pheniramine maleate Daneral,Inhiston,Trimetose,马来酸非尼拉敏	5-HT Receptor; Histamine Receptor	GPCR/G Protein; Immunology/Inflammation; Neuroscience
	Pheniramine maleate (Trimetose) 是一种具有抗组胺和血管扩张特性的烷基胺衍生物，可与组胺 H1 受体结合，从而抑制磷脂酶 A2 和内皮源性松弛因子一氧化氮的产生。
T12234	NMDA-IN-1	NMDAR	Neuroscience
	NMDA-IN-1是一种 NR2B 选择性 NMDA 拮抗剂，对NMDA 的Ki 值为 0.85 nM，对NR2B Ca2+ influx 的IC50值为 9.7 nM。
T16687	Pyr3	TRP/TRPV Channel	Membrane transporter/Ion channel
	Pyr3 是一种选择性瞬时受体电位经典通道 3 抑制剂。 Pyr3 以剂量依赖性方式抑制 TRPC3 介导的 Ca2+ 内流 (IC50 = 700 nM)。
TNU0864	HUP30	Potassium Channel; Calcium Channel	Membrane transporter/Ion channel; Metabolism
	HUP30是一种强效的血管舒张剂。HUP30可以刺激可溶性鸟苷酸环化酶，激活 K+离子通道，阻断细胞外 Ca2+的内流。
T16688	Pyr6 N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide	TRP/TRPV Channel	Membrane transporter/Ion channel
	Pyr6 (N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide)是选择性的 TRPC3抑制剂，IC50值为0.49uM。
T11102	DS16570511	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	DS16570511 是一种细胞渗透性的线粒体钙单核转运蛋白(mitochondrial calcium uniporter)小分子抑制剂，阻断了依赖于 MCU 或 MICU1 的 Ca2+流入增加。
T16686	Pyr10	TRP/TRPV Channel	Membrane transporter/Ion channel
	Pyr10 是吡唑衍生物，是TRPC3通道的选择性抑制剂。Pyr10抑制卡巴可刺激的TRPC3转染的 HEK293 细胞中的 Ca2+流入。它具有区分受体操纵的TRPC3和天然基质相互作用分子 1 (STIM1)/Orai1 通道的能力。
T10782	CGP52411 DAPH	EGFR; Beta Amyloid	Angiogenesis; JAK/STAT signaling; Neuroscience; Tyrosine Kinase/Adaptors
	CGP52411 是一种具有口服活性的 ATP 竞争性 EGFR 抑制剂（IC50：0.3 μM）。 CGP52411 阻止 Ca2+ 离子有毒流入神经元细胞，并显着抑制和逆转 β-淀粉样蛋白 Aβ42 原纤维聚集体的形成。 CGP52411 可用于阿尔茨海默病的研究。
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。
T4996	Atosiban 阿托西班,RWJ22164,RW22164	Oxytocin Receptor; Vasopressin Receptor	Endocrinology/Hormones; GPCR/G Protein
	Atosiban (RW22164) 是一种脱氨基催产素类似物，是一种九肽，也是竞争性的催产素受体拮抗剂。它是一种宫缩抑制剂，可用于自发早产的研究。
T2711	Chembridge-5861528 TCS 5861528	TRP/TRPV Channel	Membrane transporter/Ion channel
	Chembridge-5861528 (TCS 5861528) 是有效的 TRPA1离子通道阻断剂。
T5148	Atosiban acetate RW22164,Atosiban acetate (90779-69-4 free base),RWJ22164,醋酸阿托西班	Oxytocin Receptor; Vasopressin Receptor	Endocrinology/Hormones; GPCR/G Protein
	Atosiban acetate (RW22164) 是一种脱氨基催产素类似物，是一种九肽，也是竞争性的催产素受体拮抗剂。它是一种宫缩抑制剂，可用于自发早产的研究。
T6530	HC-030031 2-(1,3-二甲基-2,6-二氧代-2,3-二氢-1H-嘌呤-7(6H)-基)-N-(4-异丙基苯基)乙酰胺,HC030031,TOSLAB 829227	TRP/TRPV Channel	Membrane transporter/Ion channel
	HC-030031 (TOSLAB 829227) 是一种有效的TRPA1选择性抑制剂，拮抗福尔马林和AITC 诱发的钙流入，IC50分别为5.3±0.2和6.2±0.2μM。
T27639	ITH-12575
	ITH-12575 is an inhibitor of Mitochondrial Na+/Ca2+ exchange (mNCX). ITH12575 reduces Ca(2+) influx through CALHM1 at low micromolar concentrations.
T11480	GSK205	Others	Others
	GSK205 is a selective TRPV4 antagonist (IC50: 4.19 μM) for inhibiting TRPV4-mediated Ca2+ influx.
T68361	Asocainol hydrochloride
	Asocainol hydrochloride ia an antiarrhythmic drug which inhibits slow Ca2+ influx. This is accompanied by alterations in normal Na+-carried action potentials. Therefore, Asocainol not only inhibits Ca2+ inflow but also interferes with the fast inward Na+ current.
T14829	Bromoenol lactone (6E)-Bromoenol lactone	Phospholipase	Metabolism
	Bromoenol lactone is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β; IC50: ~7 μM). It inhibits antigen-stimulated mast cell exocytosis without blocking Ca2+ influx.
T37475	Cyclic ADP-Ribose (ammonium salt) cADP-Ribose,cADPR,Cyclic ADP-Ribose (ammonium salt)
	Cyclic ADP-ribose (cADP-ribose) is an endogenous metabolite of NAD+ that mobilizes the release of stored Ca2+ in the endoplasmic reticulum via ryanodine receptors in various cell types.[1],[2],[3],[4],[5] This second messenger is generated via the cADP-ribose synthases CD38 and CD157.[6],[5],[7] cADP-Ribose may also trigger the cell surface Ca2+ influx channel TRPM2 in a temperature-dependent manner.[8] In vitro, cADP-ribose modulates Ca2+ signaling in rat and mouse cardiomyocytes treated with i...
T80441	FS-2	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	FS-2，一种特异性L型CaV通道抑制剂，能够阻断RIN beta 细胞中，高K+或葡萄糖刺激导致的L型Ca2+内流。
T40101	(±)-1,2-Diolein 1,2-Dioleoyl-rac-glycerol,甘油1,2-二油酸酯	PKC	Chromatin/Epigenetic; Cytoskeletal Signaling
	(±)-1,2-Diolein (1,2-Dioleoyl-rac-glycerol) 是一种PKC 激活剂，可以增加肌小管 Ca2+内流。
T76203	Syringomycin E
	Syringomycin E是一种环状脂肪肽类抗真菌化合物。通过与酿酒酵母的质膜相互作用，Syringomycin E能够抑制其生长，主要机制包括促进K+的外排和Ca2+的内流，引发膜电位的变化，这一过程与通道形成密切相关。
T26452	A 80b A80b,A-80b
	A-80b is a synthesized pyridazino[4,5-b]indole derivate with potent and long-lasting antihypertensive activity. The decrease in diastolic pressure was greater than the decrease in systolic pressure and cardiac frequency was not modified significantly. A-8
TP1910	CALP1
	Cell-permeable calmodulin (CaM) agonist that binds to the EF-hand/Ca2+-binding site; produces CaM-dependent activation of phosphodiesterase. Also binds to cytoplasmic sites on other Ca2+ channels, including NMDA and HIV-1 gp120-activated channels, inhibit
T23102	OBAA	Others	Others
	OBAA 是一种有效的磷脂酶 A2 (PLA2) 抑制剂(IC50= 70 nM)，并且在布氏锥虫中阻断 Melittin 诱导的 Ca2+流入(IC50= 0.4 μM)。
T75793	ω-Agatoxin IVA TFA
	ω-Agatoxin IVA TFA 是一种高效的针对P/Q型Ca2+(Cav2.1)通道的选择性阻滞剂，IC50对P型为2 nM，对Q型为90 nM。此化合物能够抑制高钾条件下的谷氨酸释放和钙流入，IC50在30-225 nM范围。同时，ω-Agatoxin IVA TFA阻断高钾诱发的5-羟色胺及去甲肾上腺素释放，但不影响L型或N型Ca2+通道。
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。
T80930	TRPV2-selective blocker 1
	TRPV2-selective blocker 1 (compound IV2-1) 为选择性TRPV2通道阻断剂，具有6.3 μM IC50，不对TRPV1、TRPV3和TRPV4通道产生影响。该化合物能够抑制巨噬细胞中TRPV2介导的Ca2+流入，进而抑制其吞噬功能。
T73453	MRS4719
	MRS4719 是一种有效的P2X4受体拮抗剂，对人 P2X4 受体的IC50为 0.503 μM。MRS4719 可减少脑梗死体积，减少脑萎缩，在缺血性脑中风模型中具有神经保护和神经康复作用。MRS4719 还能减少 ATP 诱导的人单核细胞源性巨噬细胞 [Ca2+]i 内流。MRS4719 可用于研究缺血性脑中风。
T36805	TPC2-A1-N TPC2-A1-N
	TPC2-A1-N is a novel, lipophilic, membrane permeable isoform-selective small molecule agonist of two-pore channel 2 (TPC2). TPC2-A1-N plays its role by mimicking the physiological actions of NAADP and PI(3,5)P2 through independent binding sites. TPC2-A1-N has inverse effects on key lysosomal activities and increases the pH in the lysosomal lumen in a TPC2-dependent manner[1].

化合物

Cat.No: T6777

Synonym: (±)-BAY-K-8644,SQ 28,873

Target: Calcium Channel

Pheniramine maleate

Cat.No: T0370

Synonym: Daneral,Inhiston,Trimetose,马来酸非尼拉敏

Target: 5-HT Receptor, Histamine Receptor

Cat.No: T12234

Target: NMDAR

Cat.No: T16687

Target: TRP/TRPV Channel

Cat.No: TNU0864

Target: Potassium Channel, Calcium Channel

Cat.No: T16688

Synonym: N-[4-[3,5-Bis(trifluoromethyl)-1H-pyrazol-1-yl]phenyl]-3-fluoro-4-pyridinecarboxamide

Target: TRP/TRPV Channel

Cat.No: T11102

Target: Calcium Channel

Cat.No: T16686

Target: TRP/TRPV Channel

Cat.No: T10782

Synonym: DAPH

Target: EGFR, Beta Amyloid

Cat.No: TP1910L1

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

Target: CaMK

Cat.No: T4996

Synonym: 阿托西班,RWJ22164,RW22164

Target: Oxytocin Receptor, Vasopressin Receptor

Chembridge-5861528

Cat.No: T2711

Synonym: TCS 5861528

Target: TRP/TRPV Channel

Atosiban acetate

Cat.No: T5148

Synonym: RW22164,Atosiban acetate (90779-69-4 free base),RWJ22164,醋酸阿托西班

Target: Oxytocin Receptor, Vasopressin Receptor

Cat.No: T6530

Synonym: 2-(1,3-二甲基-2,6-二氧代-2,3-二氢-1H-嘌呤-7(6H)-基)-N-(4-异丙基苯基)乙酰胺,HC030031,TOSLAB 829227

Target: TRP/TRPV Channel

Cat.No: T27639

Cat.No: T11480

Target: Others

Asocainol hydrochloride

Cat.No: T68361

Bromoenol lactone

Cat.No: T14829

Synonym: (6E)-Bromoenol lactone

Target: Phospholipase

Cyclic ADP-Ribose (ammonium salt)

Cat.No: T37475

Synonym: cADP-Ribose,cADPR,Cyclic ADP-Ribose (ammonium salt)

Cat.No: T80441

Target: Calcium Channel

(±)-1,2-Diolein

Cat.No: T40101

Synonym: 1,2-Dioleoyl-rac-glycerol,甘油1,2-二油酸酯

Target: PKC

Cat.No: T76203

Cat.No: T26452

Synonym: A80b,A-80b

Cat.No: TP1910

Cat.No: T23102

Target: Others

ω-Agatoxin IVA TFA

Cat.No: T75793

Cat.No: T75791

TRPV2-selective blocker 1

Cat.No: T80930

Cat.No: T73453

Cat.No: T36805

Synonym: TPC2-A1-N

Cat. No.	Product Name	Target	Signaling Pathways
TN1121	Evocarpine	Apoptosis; cAMP; Anti-infection; Calcium Channel; Antibacterial	Apoptosis; GPCR/G Protein; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology
	Evocarpine 是从 Evodiae fructus 分离得到的一种喹诺酮类生物碱，有抗细菌活性。它可通过电压依赖性钙通道抑制 Ca2+内流。
TN2322	Yangambin	Calcium Channel; PAFR	GPCR/G Protein; Membrane transporter/Ion channel; Metabolism
	Yangambin 是从诸如番荔枝科植物中分离出来的呋喃木脂素，是选择性PAF 受体拮抗剂，通过调控Ca2+通道抑制 Ca2+流入，导致 [Ca2+]i 在血管平滑肌细胞和随后的外周血管舒张中减少，具有降压作用。
TN1136	Procyanidin A1 原花青素 A1,Proanthocyanidin A1,原花色素A1	LDL; Calcium Channel; PKC	Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism
	Procyanidin A1 (Proanthocyanidin A1) 是一种原花青素二聚体，具有抗过敏作用，可抑制蛋白激酶 C 激活下游脱粒或 RBL-213 细胞内部储存的 Ca2+流入。
TN1065	Hirsutine	Apoptosis	Apoptosis
	Hirsutine 是一种来自钩藤的吲哚生物碱，可诱导细胞凋亡，是一种登革热病毒抑制剂，且毒性低。它具有抗癌、心脏保护、抗高血压、抗心律失常和血管舒张活性。
T5120	Rhamnose 6-Deoxyhexopyranose,L-鼠李糖,6-Deoxy-L-mannose,alpha-L-Rhamnose	Calcium Channel; Endogenous Metabolite	Membrane transporter/Ion channel; Metabolism
	alpha-L-Rhamnose (6-Deoxy-L-mannose) 是存在植物和细菌中的一种单糖。Rhamnose- 免疫原连接物能被用于免疫疗法。Rhamnose 能通过胞外途径穿过上皮细胞，能够作为肠吸收的标志。
T6S2140	β-Anhydroicaritin Anhydroicaritin,Beta-Anhydroicaritin,脱水淫羊藿素	MMP; Others; TNF; Interleukin	Apoptosis; Immunology/Inflammation; Others; Proteases/Proteasome
	β-Anhydroicaritin 是从乳香提取的一种天然产物，具有重要的生物学和药理学作用，如抗骨质疏松症，雌激素调节和抗肿瘤特性。它改善牙周组织的降解，抑制糖尿病大鼠 TNF-α 和 MMP-3 的合成和分泌。它抑制细胞内 Ca2+的升高，并显著降低 iNOS 蛋白的表达。
T82753	Celangulin
	Celangulin是一种从Celastrus angulatus中提取的天然杀虫成分，该化合物通过激活细胞质膜上的钙通道来增加细胞内Ca2+浓度，并能激活内质网钙通道。
TN2511	Britannilactone diacetate 1,6-O,O-Diacetylbritannilactone	IL Receptor; PARP; ROS; MAPK; Caspase; JAK; JNK; STAT	Angiogenesis; Apoptosis; Chromatin/Epigenetic; DNA Damage/DNA Repair; Immunology/Inflammation; JAK/STAT signaling; MAPK; Proteases/Proteasome; Stem Cells
	1,6-O,O-Diacetylbritannilactone(OODBL) has anti-inflammatory activity, it has a potential therapeutic efficacy on inflammatory diseases especially allergic airway disease as a lead compound. OODBL has anti-asthmatic activity, it reduces leukotriene C4 pro
TN4624	Nantenine	Others	Others
	Nantenine is an acetylcholinesterase inhibitor, it functions as an effective antagonist against a wide range of MDMA-induced effects in mice. Nantenine has anticonvulsant effect, which seems attributable to its stimulation and the resultant decrease of Ca

天然产物

Cat.No: TN1121

Target: Apoptosis, cAMP, Anti-infection, Calcium Channel, Antibacterial

Cat.No: TN2322

Target: Calcium Channel, PAFR

Cat.No: TN1136

Synonym: 原花青素 A1,Proanthocyanidin A1,原花色素A1

Target: LDL, Calcium Channel, PKC

Cat.No: TN1065

Target: Apoptosis

Cat.No: T5120

Synonym: 6-Deoxyhexopyranose,L-鼠李糖,6-Deoxy-L-mannose,alpha-L-Rhamnose

Target: Calcium Channel, Endogenous Metabolite

β-Anhydroicaritin

Cat.No: T6S2140

Synonym: Anhydroicaritin,Beta-Anhydroicaritin,脱水淫羊藿素

Target: MMP, Others, TNF, Interleukin

Cat.No: T82753

Britannilactone diacetate

Cat.No: TN2511

Synonym: 1,6-O,O-Diacetylbritannilactone

Target: IL Receptor, PARP, ROS, MAPK, Caspase, JAK, JNK, STAT

Cat.No: TN4624

Target: Others

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