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Search Results for " ca inhibitor 2 "

38

抑制剂 & 化合物

3

天然产物

2

同位素标记化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T79681	CA inhibitor 2	Carbonic Anhydrase	Metabolism
	CA inhibitor 2 (Compound 4H)，作为碳酸酐酶抑制剂，其半抑制浓度（IC50）为0.033 μM。
T10659	Ca2+ channel agonist 1	Calcium Channel; CDK	Cell Cycle/Checkpoint; Membrane transporter/Ion channel; Metabolism
	Ca2+channel agonist 1 是 N-型钙离子通道激动剂和Cdk2的抑制剂，EC50分别为 14.23 μM 和 3.34 μM，可用作运动神经末梢功能障碍的潜在治疗方法。
T4693	2-Aminoethyl diphenylborinate 2-Aminoethoxydiphenyl borate,二苯基酸,2-APB	Calcium Channel; TRP/TRPV Channel	Membrane transporter/Ion channel; Metabolism
	2-Aminoethyl diphenylborinate (2-APB) 是细胞通透性的 IP3R 和 TRP 通道抑制剂，还抑制 store-operated Ca2+(SOC)通道。
T8944	TTA-A2	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	TTA-A2 是一种选择性 T 型钙通道拮抗剂，是一种有效的抗惊厥药，可减少孕烷 X 受体的激活。它对 Cav3.1 (a1G) 和 Cav3.2 (a1H) 通道在 -80 mV 和- 100 mV 保持电位上具有同样的作用，IC50 值分别为 89 和 92 nM。它可用于多种人类神经系统疾病的研究，包括睡眠障碍和癫痫。
T1101	Minocycline hydrochloride Minocycline HCl,盐酸米诺环素,美满霉素	HIF/HIF Prolyl-Hydroxylase; Antibacterial; Antibiotic	Chromatin/Epigenetic; Metabolism; Microbiology/Virology
	Minocycline hydrochloride (Minocycline HCl) 属于四环素类抗生素，具有出色的吸收和组织渗透性。Minocycline hydrochloride 是一种广谱的抗菌剂，可用于多种细菌感染以及痤疮的治疗。
T1606	Fasudil HA-1077,AT877,法舒地尔	ROCK; Serine/threonin kinase; Calcium Channel; PKA; PKC; Autophagy	Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Stem Cells; Tyrosine Kinase/Adaptors
	Fasudil (HA-1077) 是一种非特异性 RhoA/ROCK 抑制剂，也是 Ca2+通道拮抗剂和血管扩张剂。它对蛋白激酶有抑制作用，ROCK1 的 Ki 值为 0.33 μM，ROCK2 和 PKA、PKC、PKG 的 IC50值分别 0.158 μM 和 4.58 μM、12.30 μM、1.650 μM。
T3060	Fasudil hydrochloride Fasudil (HA-1077) HCl,盐酸法舒地尔,HA-1077,Fasudil HCl,HA-1077 hydrochloride,AT-877	ROCK; Serine/threonin kinase; Calcium Channel; HIV Protease; PKA; PKC; Autophagy	Autophagy; Cell Cycle/Checkpoint; Chromatin/Epigenetic; Cytoskeletal Signaling; Membrane transporter/Ion channel; Metabolism; Microbiology/Virology; Proteases/Proteasome; Stem Cells; Tyrosine Kinase/Adaptors
	Fasudil hydrochloride (HA-1077) 是一种非特异性RhoA/ROCK 抑制剂，也抑制蛋白激酶，对 ROCK1、PKA、PKC 和 MLCK 的 Ki 值分别为 0.33 μM、1.0 μM、9.3 μM 和 55 μM。
T36758	CAIX Inhibitor S4 S4	Carbonic Anhydrase	Metabolism
	CAIX Inhibitor S4 (S4) 是一种有效的碳酸酐酶 IX/XII 抑制剂，Ki 分别为 7 nM 和 2 nM。 CA II 和 CA I 的 Ki 分别为 546 和 5600 nM。
T12108	MRS1845	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	MRS1845 是一种 ORAI1 抑制剂和钙进入（SOCE）阻滞剂，可阻断VP 诱导的 SOCE、OS 和 Ca（2+）沉积。
T77631	Enpp/Carbonic anhydrase-IN-2	Apoptosis; PDE; Carbonic Anhydrase	Apoptosis; Metabolism
	Enpp/Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.07, 0.74, 0.33, 0.68, respectively.Enpp/Carbonic anhydrase-IN-2 induced apoptosis.Enpp/Carbonic anhydrase-IN-2 has antiproliferative activity against cancer cells and low cytotoxicity against normal cells.
T21907	PACOCF3 1,1,1-trifluoroheptadecan-2-one,Palmityltrifluoromethylketone	Phospholipase	Metabolism
	PACOCF3 (Palmityltrifluoromethylketone) (Palmityltrifluoromethylketone) 是一种钙非依赖性的磷脂酶 A2 (phospholipase A2) 抑制剂，IC50为 3.8 μM。PACOCF3 改变肾小管细胞中的 Ca2+信号传导。
T21294	Polmacoxib CG-100649,帕马考昔,CG100649,CG 100649	COX; Carbonic Anhydrase	Immunology/Inflammation; Metabolism; Neuroscience
	Polmacoxib (CG 100649) 是一流的 NSAID 候选药物，是碳酸酐酶 (CA) 和 COX-2 的双重抑制剂。它在小鼠模型中抑制大肠腺瘤和肿瘤生长。
T16564	PPADS tetrasodium	P2X Receptor; Na+/Ca2+ Exchanger	Membrane transporter/Ion channel; Neuroscience
	PPADS tetrasodiuma 是一种有效的 P2X 受体拮抗剂，也是是豚鼠气道平滑肌 Na/Ca²⁺ 交换逆模式的抑制剂，对谷氨酸/NMDA毒性有神经保护作用。PPADS tetrasodiuma 抑制 P2X1、P2X-2、P2X-3 和 P2X-5。
T21509	CA 074	Cysteine Protease	Proteases/Proteasome
	CA 074 是一种高效的组织蛋白酶B (cathepsin B) 抑制剂， Ki 值为2 to 5 nM。CA 074 抑制灵长类动物缺血性海马神经元死亡，可减轻 SJL/J 小鼠诱导的实验性自身免疫性脑脊髓炎的视网膜病变和视神经炎。
T24845	T16A(inh)-B01 T16Ainh-B01,T16A(inh)B01,T16AinhB01,T16Ainh B01	Others	Others
	T16A(inh)-B01 is the Ca(2+)-activated Cl(-) Channel, Ano1 class B inhibitor.
T24846	T16A(inh)-C01 T16A(inh) C01	Others	Others
	T16A(inh)-C01 is the Ca(2+)-activated Cl(-) Channel, Ano1 class C inhibitor.
T24847	T16A(inh)-D01 T16A(inh) D01,T16Ainh-D01,T16AinhD01,T16A(inh)D01,T16Ainh D01	Others	Others
	T16A(inh)-D01 is the Ca(2+)-activated Cl(-) Channel, Ano1 class D inhibitor.
T28268	ORM-3819	Others	Others
	ORM-3819 is a potent and selective PDE III inhibitor. ORM-3819 promotes cardiac contractility through Ca(2+) sensitization.
T27639	ITH-12575	Others	Others
	ITH-12575 is an inhibitor of Mitochondrial Na+/Ca2+ exchange (mNCX). ITH12575 reduces Ca(2+) influx through CALHM1 at low micromolar concentrations.
T40437	Caloxin 2A1
	Caloxin 2A1 is an inhibitor peptide of the plasma membrane Ca 2+-ATPase (PMCA) responsible for extracellular signaling. Importantly, Caloxin 2A1 has no impact on the basal Mg 2+-ATPase or Na+-K+-ATPase activities.
T24481	ML204 hydrochloride ML204,ML204 HCl,ML-204	Others	Others
	ML204 is a potent inhibitor of the TRPC4 channel. ML204 inhibited TRPC4β-mediated intracellular Ca(2+) rise (IC50: 0.96 μM) and exhibited 19-fold selectivity against muscarinic receptor-coupled TRPC6 channel activation.
T61974	CAII-IN-2	Others	Others
	CAII-IN-2 (compound 3g) 是一种硫代氨基脲衍生物。CAII-IN-2是一种有效的选择性碳酸酐酶-II (CA-II) 抑制剂，抑制牛 CA-II 的 IC50为 12.1 μM。CAII-IN-2 在碳酸酐酶相关生物疾病中具有研究价值。
T75727	ω-Conotoxin GVIA TFA
	ω-Conotoxin GVIA TFA 是一种 N 型钙通道 (Ca2+channel) 抑制剂。
T72164	Enpp/Carbonic anhydrase-IN-2	Others	Others
	Enpp/Carbonic anhydrase-IN-2 是一种有效的 Enpp 和 carbonic anhydrase 抑制剂，对 NPP1、NPP2、NPP3、CA-IX, CA-XII 的 IC50值分别 1.13、 1.07、 0.74、 0.33、 0.68。Enpp/Carbonic anhydrase-IN-2 对癌细胞具有抗增殖活性，对正常细胞具有低细胞毒性。Enpp/Carbonic anhydrase-IN-2 诱导细胞凋亡 (Apoptosis)。
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)。
T60515	CaMKIIα-IN-1	Others	Others
	CaMKIIα-IN-1 (Compound 4d) 是一种具有口服活性的 Ca 2+/钙调素依赖性蛋白激酶 II α (CaMKIIα) 抑制剂。CaMKIIα-IN-1对 CaMKIIα WT hub 的 Kd 值为 219 nM。CaMKIIα-IN-1 表现出良好的代谢稳定性。
T61382	Fasudil dihydrochloride	Others	Others
	Fasudil dihydrochloride, also known as HA-1077 and AT877, is a nonspecific inhibitor of RhoA/ROCK. It exhibits inhibitory effects on protein kinases, including ROCK1 with a Ki value of 0.33 μM, as well as ROCK2, PKA, PKC, and PKG with IC 50 values of 0.158 μM, 4.58 μM, 12.30 μM, and 1.650 μM, respectively. Additionally, Fasudil dihydrochloride demonstrates potent Ca 2+ channel blocking activity and acts as a vasodilator [1] [2] [3].
T79540	hCA/VEGFR-2-IN-1	Carbonic Anhydrase	Metabolism
	hCA/VEGFR-2-IN-1 是一种高效的双靶点抑制剂，对 hCA IX 和 hCA XII 两种碳酸酐酶（CA）具有极低的Ki值，分别为8.3 nM和4.7 nM。同时，hCA/VEGFR-2-IN-1 也是一种有效的 VEGFR-2 抑制剂，其 IC50 值仅为26.3 nM，并且显示出抗癌活性。
T37403	O-desmethyl Brinzolamide (hydrochloride)	Others	Others
	O-desmethyl Brinzolamide is an active metabolite of the carbonic anhydrase (CA) inhibitor brinzolamide .1,2It inhibits CAII and CAIV (IC50s = 0.136 and 165 nM, respectively).1 1.Huang, Q., Rui, E.Y., Cobbs, M., et al.Design, synthesis, and evaluation of NO-donor containing carbonic anhydrase inhibitors to lower intraocular pressureJ. Med. Chem.58(6)2821-2833(2015) 2.Lo Faro, A.F., Tini, A., Gottardi, M., et al.Development and validation of a fast ultra-high-performance liquid chromatography tand...
T9655	NBC 6	Others	Others
	NLRP3-IN-NBC6 是一种有效的选择性 NLRP3炎性小体抑制剂，IC50为574 nM，其作用独立于 Ca2+。NLRP3-IN-NBC6 抑制 Nigericin 诱导的 THP-1 细胞炎症反应和 Imiquimod 诱导的 LPS-primed 的骨髓源性巨噬细胞 (BMDMs) 释放 IL-1β。
T60526	N-Salicyloyltryptamine	Others	Others
	N-Salicyloyltryptamine(STP) 是一种色胺类似物，具有抗惊厥、抗炎、镇痛和血管舒张的作用。N-Salicyloyltryptamine 作为电压依赖性离子通道（包括Na+、Ca2+、K+离子通道）抑制剂，可抑制 K+电流，IC50值为 34.6 μM ( /to)。
T80975	TMDJ-035	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	TMDJ-035为选择性RyR2抑制剂。该化合物能够抑制携带ryr2突变的小鼠心肌细胞中异常的Ca2+波动和瞬态现象。作为研究RyR2通道开闭机制及其动力学的实验工具，TMDJ-035的应用十分关键。
T68547	SNJ-1945	Others	Others
	SNJ-1945 is a calpain inhibitor with more favorable retinal penetration, high oral bioavailability, and long half-life. SNJ1945 rescued defective function in lissencephaly. SNJ-1945 protects SH-SY5Y cells against MPP(+) and rotenone. SNJ-1945 reduces murine retinal cell death in vitro and in vivo. SNJ-1945 has good aqueous solubility, can prevents the heart from KCl arrest-reperfusion injury associated with the impairment of total Ca(2+) handling by inhibiting the proteolysis of alpha-fodrin a...
T63373	S100A2-p53-IN-1	Others	Others
	S100A2-p53-IN-1（化合物 51）是一款针对S100A2-p53相互作用的抑制剂，专用于阻断S100A2与p53的相互作用。作为一种与Ca2+结合并参与细胞信号传递的蛋白，S100A2在胰腺癌中表达上调。S100A2-p53-IN-1特别针对MiaPaCa-2胰腺癌细胞系，显示出良好的生长抑制效果（GI50为1.2-3.4 μM）。
T14553	BHPI	Others	Others
	BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression. Elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
T73527	GK563	Others	Others
	GK563是一种针对Ca2+-independent phospholipase A2(GVIA iPLA2)的选择性抑制剂，具有1 nM的IC50值。相比于GIVA cPLA2，GK563对GVIA iPLA2的抑制活性高出22000倍。它能减少促炎细胞因子诱导的β-cell凋亡，从而增加了其在对抗自身免疫性疾病（例如1型糖尿病）中的潜在应用价值。
T69383	NBI-42902	Others	Others
	NBI-42902 is a potent inhibitor of peptide radioligand binding to the human GnRH receptor (K(i) = 0.56 nm). Tritiated NBI-42902 binds with high affinity (K(d) = 0.19 nm) to a single class of binding sites and can be displaced by a range of peptide and nonpeptide GnRH receptor ligands. In vitro experiments demonstrate that NBI-42902 is a potent functional, competitive antagonist of GnRH stimulated IP accumulation, Ca(2+) flux, and ERK1/2 activation. It did not stimulate histamine release from rat...
T41016	Vercirnon sodium GSK-1605786 sodium,CCX282-Bsodium,维塞诺钠盐,Traficet-ENsodium	Others	Others
	Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9 . Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC 50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC 50 s>10 μM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC 50 values of 2.8 and 2.6 nM, respectivel...

化合物

CA inhibitor 2

Cat.No: T79681

Target: Carbonic Anhydrase

Ca2+ channel agonist 1

Cat.No: T10659

Target: Calcium Channel, CDK

2-Aminoethyl diphenylborinate

Cat.No: T4693

Synonym: 2-Aminoethoxydiphenyl borate,二苯基酸,2-APB

Target: Calcium Channel, TRP/TRPV Channel

Cat.No: T8944

Target: Calcium Channel

Minocycline hydrochloride

Cat.No: T1101

Synonym: Minocycline HCl,盐酸米诺环素,美满霉素

Target: HIF/HIF Prolyl-Hydroxylase, Antibacterial, Antibiotic

Cat.No: T1606

Synonym: HA-1077,AT877,法舒地尔

Target: ROCK, Serine/threonin kinase, Calcium Channel, PKA, PKC, Autophagy

Fasudil hydrochloride

Cat.No: T3060

Synonym: Fasudil (HA-1077) HCl,盐酸法舒地尔,HA-1077,Fasudil HCl,HA-1077 hydrochloride,AT-877

Target: ROCK, Serine/threonin kinase, Calcium Channel, HIV Protease, PKA, PKC, Autophagy

CAIX Inhibitor S4

Cat.No: T36758

Synonym: S4

Target: Carbonic Anhydrase

Cat.No: T12108

Target: Calcium Channel

Enpp/Carbonic anhydrase-IN-2

Cat.No: T77631

Target: Apoptosis, PDE, Carbonic Anhydrase

Cat.No: T21907

Synonym: 1,1,1-trifluoroheptadecan-2-one,Palmityltrifluoromethylketone

Target: Phospholipase

Cat.No: T21294

Synonym: CG-100649,帕马考昔,CG100649,CG 100649

Target: COX, Carbonic Anhydrase

PPADS tetrasodium

Cat.No: T16564

Target: P2X Receptor, Na+/Ca2+ Exchanger

Cat.No: T21509

Target: Cysteine Protease

Cat.No: T24845

Synonym: T16Ainh-B01,T16A(inh)B01,T16AinhB01,T16Ainh B01

Target: Others

Cat.No: T24846

Synonym: T16A(inh) C01

Target: Others

Cat.No: T24847

Synonym: T16A(inh) D01,T16Ainh-D01,T16AinhD01,T16A(inh)D01,T16Ainh D01

Target: Others

Cat.No: T28268

Target: Others

Cat.No: T27639

Target: Others

Cat.No: T40437

ML204 hydrochloride

Cat.No: T24481

Synonym: ML204,ML204 HCl,ML-204

Target: Others

Cat.No: T61974

Target: Others

ω-Conotoxin GVIA TFA

Cat.No: T75727

Enpp/Carbonic anhydrase-IN-2

Cat.No: T72164

Target: Others

Cat.No: T23102

Target: Others

Cat.No: T60515

Target: Others

Fasudil dihydrochloride

Cat.No: T61382

Target: Others

hCA/VEGFR-2-IN-1

Cat.No: T79540

Target: Carbonic Anhydrase

O-desmethyl Brinzolamide (hydrochloride)

Cat.No: T37403

Target: Others

Cat.No: T9655

Target: Others

N-Salicyloyltryptamine

Cat.No: T60526

Target: Others

Cat.No: T80975

Target: Calcium Channel

Cat.No: T68547

Target: Others

S100A2-p53-IN-1

Cat.No: T63373

Target: Others

Cat.No: T14553

Target: Others

Cat.No: T73527

Target: Others

Cat.No: T69383

Target: Others

Vercirnon sodium

Cat.No: T41016

Synonym: GSK-1605786 sodium,CCX282-Bsodium,维塞诺钠盐,Traficet-ENsodium

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
TN7108	Urolithin C	Apoptosis; Calcium Channel; Reactive Oxygen Species; IGF-1R; Endogenous Metabolite	Apoptosis; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism; NF-κB; Tyrosine Kinase/Adaptors
	Urolithin C 属于多酚类，是鞣花酸的肠道微生物代谢产物，具有胰岛素分泌的葡萄糖依赖性激活活性。Urolithin C 是 L 型 Ca2+通道开放剂，可增强 Ca2+的流入。它通过线粒体介导的途径诱导细胞凋亡，并刺激活性氧的形成。
T3377	L-Phenylalanine L-苯丙氨酸,(S)-2-Amino-3-phenylpropionic acid,phenylalanine,3-Phenyl-L-alanine	Calcium Channel; Endogenous Metabolite; iGluR	Membrane transporter/Ion channel; Metabolism; Neuroscience
	L-Phenylalanine (3-Phenyl-L-alanine) 是分离自大肠杆菌的必需氨基酸，是 NMDARs(KB573 μM) 和非 NMDARs 的甘氨酸和谷氨酸结合位点的竞争性拮抗剂，用于食品香料和药品的生产中。它是一种电压依赖性 α2δ 亚基 Ca2+通道拮抗剂，Ki 为 980 nM。
T75333	Quinine hemisulfate hydrate	Others	Others
	Quinine hemisulfate hydrate，一种从金鸡纳树皮提取的生物碱，具有抗疟疾效果。作为钾离子通道 (potassium channel) 抑制剂，它能够抑制由电压脉冲触发的MT mSlo3 (KCa5.1) 通道在+100 mV下的电流活动，其IC50值达169 μM。

天然产物

Cat.No: TN7108

Target: Apoptosis, Calcium Channel, Reactive Oxygen Species, IGF-1R, Endogenous Metabolite

L-Phenylalanine

Cat.No: T3377

Synonym: L-苯丙氨酸,(S)-2-Amino-3-phenylpropionic acid,phenylalanine,3-Phenyl-L-alanine

Target: Calcium Channel, Endogenous Metabolite, iGluR

Quinine hemisulfate hydrate

Cat.No: T75333

Target: Others

Cat. No.	Product Name	Target	Signaling Pathways
T40376	L-Phenylalanine-15N L-苯丙氨酸 15N,(S)-2-Amino-3-phenylpropionic acid-15N,L-Phenylalanine-15N	Calcium Channel	Membrane transporter/Ion channel; Metabolism
	L-Phenylalanine-15N ((S)-2-Amino-3-phenylpropionic acid-15N) 是 15N 标记的 L-Phenylalanine。L-Phenylalanine 是从大肠杆菌中分离出来的一种必需氨基酸。 L-Phenylalanine 广泛用于食品香精和药物的生产。
T37847	Zonisamide-13C2,15N Zonisamide-13C2,15N
	Zonisamide-13C2,15N is intended for use as an internal standard for the quantification of zonisamide by GC- or LC-MS. Zonisamide is an antiepileptic agent.1 It selectively inhibits the repeated firing of sodium channels (IC50 = 2 μg/ml) in mouse embryo spinal cord neurons and inhibits spontaneous channel firing when used at concentrations greater than 10 μg/ml.2 In rat cerebral cortex neurons, zonisamide (1-1,000 μM) inhibits T-type calcium channels with a maximum reduction of 60% of the calcium...

同位素标记化合物

L-Phenylalanine-15N

Cat.No: T40376

Synonym: L-苯丙氨酸 15N,(S)-2-Amino-3-phenylpropionic acid-15N,L-Phenylalanine-15N

Target: Calcium Channel

Zonisamide-13C2,15N

Cat.No: T37847

Synonym: Zonisamide-13C2,15N

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