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16

抑制剂 & 化合物

9

天然产物

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Cat. No. Product Name Target Signaling Pathways
T4309 CIL56

CA3

Ferroptosis; ROS Apoptosis; Immunology/Inflammation
CIL56 (CA3) 是一种选择性铁死亡诱导剂,可通过产生铁依赖性活性氧来诱导细胞铁死亡。
T9027 CA-4948

Emavusertib

IRAK; FLT Angiogenesis; Immunology/Inflammation; NF-κB; Tyrosine Kinase/Adaptors
CA-4948 (Emavusertib) 是一种IRAK4抑制剂,也是一种FLT3抑制剂,具有抗肿瘤作用。
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。
T1260 Cromolyn sodium

Disodium Cromoglycate,FPL 670 (Cromolyn) Disodium,FPL-670,色甘酸钠,Sodium cromoglycate

Others; Potassium Channel; GSK-3; Calcium Channel Membrane transporter/Ion channel; Metabolism; Others; PI3K/Akt/mTOR signaling; Stem Cells
Cromolyn sodium (FPL-670) 是一种GSK-3β抑制剂,IC50为 2.0 µM,有抗过敏作用。
T7550 Barnidipine

YM-09730-5(Free base),(4S)-2,6-二甲基-4-(间硝基苯基)-1,4-二氢吡啶-3,5-二羧酸 (3S)-1-苄基-3-吡咯烷基-甲基酯,Mepirodipine

Calcium Channel Membrane transporter/Ion channel; Metabolism
Barnidipine (YM-09730-5(Free base)) 是一种二氢吡啶类钙通道阻滞剂,对 CaA 受体具有选择性作用。它是一种抗高血压药物,通过减少其血管扩张作用继发的外周血管阻力起作用。
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。
T67775 Enpp/Carbonic anhydrase-IN-1

PDE; Carbonic Anhydrase Metabolism
Enpp/Carbonic anhydrase-IN-1 (compound 1e) 是有效的 Enpp 和 carbonic anhydrase 抑制剂。Enpp/Carbonic anhydrase-IN-1抑制 NPP1、NPP2、NPP3CA-II、CA-IX 的 IC50 值分别 1.36、1.35、3.00、0.88、1.02 µM。Enpp/Carbonic anhydrase-IN-1 选择性抑制癌细胞的增殖,对正常细胞毒性较低。
T61340 CAII-IN-3

CAII-IN-3 (compound 3h) is a thiosemicarbazone derivative known for its potent inhibition of carbonic anhydrase-II (CA-II). It exhibits an IC50 value of 13.4 μM [1].
T31573 DPX-3778

DPX-3778 is the triethanolamine salt of 3-(p-chlorophenyl)-6-methoxy-s-triazine-2,4(1H,3H) dione, at concentrations of 0.124-2.48 μM enhanced ca. 4-5-fold the proliferation of tobacco (Nicotiana tabacum L. cv. Wisconsin 38) callus cultured in the presence
T63753 hCAIX-IN-3

hCAII-IN-3 (compound 7e) 是选择性的、有效的碳酸酐酶 (CA II/IX) 抑制剂,他们的 Kis 值分别为 124.2 和 30.5 nM。hCAII-IN-1 对癌症疾病表现出研究潜力。
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)。
T61382 Fasudil dihydrochloride

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].
T72701 Cavα2δ1&NET-IN-3

Cavα2δ1&NET-IN-3 (example 216) 是电压门控钙通道 (VGCC) 的亚基 α2δ 和去甲肾上腺素转运蛋白 (NET) 抑制剂。Cavα2δ1&NET-IN-3 对人的 Cav2.2 钙通道 α2δ-1 亚基和 NET 的 Ki 均为 100-500 nM。
T75866 RFRP-3(human) TFA

RFRP-3 (Neuropeptide VF(124-131))(human) TFA,一种人 GnIH 肽同源物,是一种促性腺激素分泌抑制 Ca2+动员的有效抑制剂。RFRP-3(human) TFA 是一种NPFF1受体激动剂,它抑制 forskolin 诱导的 cAMP 生成的 IC50值为 0.7 nM。
T72213 Efonidipine hydrochloride

NZ-105 hydrochloride

Efonidipine(NZ-105)盐酸盐是T 型和L 型钙离子通道双重阻断剂。
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...

化合物

CIL56
Cat.No: T4309
Synonym: CA3
Target: Ferroptosis, ROS
CA-4948
Cat.No: T9027
Synonym: Emavusertib
Target: IRAK, FLT
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
Cromolyn sodium
Cat.No: T1260
Synonym: Disodium Cromoglycate,FPL 670 (Cromolyn) Disodium,FPL-670,色甘酸钠,Sodium cromoglycate
Target: Others, Potassium Channel, GSK-3, Calcium Channel
Barnidipine
Cat.No: T7550
Synonym: YM-09730-5(Free base),(4S)-2,6-二甲基-4-(间硝基苯基)-1,4-二氢吡啶-3,5-二羧酸 (3S)-1-苄基-3-吡咯烷基-甲基酯,Mepirodipine
Target: Calcium Channel
PPADS tetrasodium
Cat.No: T16564
Synonym:
Target: P2X Receptor, Na+/Ca2+ Exchanger
Enpp/Carbonic anhydrase-IN-1
Cat.No: T67775
Synonym:
Target: PDE, Carbonic Anhydrase
CAII-IN-3
Cat.No: T61340
Synonym:
Target:
DPX-3778
Cat.No: T31573
Synonym:
Target:
hCAIX-IN-3
Cat.No: T63753
Synonym:
Target:
OBAA
Cat.No: T23102
Synonym:
Target: Others
Fasudil dihydrochloride
Cat.No: T61382
Synonym:
Target:
Cavα2δ1&NET-IN-3
Cat.No: T72701
Synonym:
Target:
RFRP-3(human) TFA
Cat.No: T75866
Synonym:
Target:
Efonidipine hydrochloride
Cat.No: T72213
Synonym: NZ-105 hydrochloride
Target:
Zonisamide-13C2,15N
Cat.No: T37847
Synonym: Zonisamide-13C2,15N
Target:
Cat. No. Product Name Target Signaling Pathways
T2782 Catharanthine

(+)-3, 4-Didehydrocoronaridine,长春质碱,(+)-3,4-Didehydrocoronaridine

Calcium Channel; AChR Membrane transporter/Ion channel; Metabolism; Neuroscience
Catharanthine ((+)-3,4-Didehydrocoronaridine) 是长春花中的一种生物碱,可抑制电压门控 L 型钙离子通道,具有抗肿瘤和降血压活性。
T6212 Combretastatin A4

CA4,康普瑞汀,Z)-3,4,5,4',-四甲氧基-3'-羟基二苯乙烯,CRC 87-09

Microtubule Associated Cytoskeletal Signaling
Combretastatin A4 (CA4) 是一种微管靶向剂,可结合 β-tubulin,Kd 值为 0.4 μM。
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。
T3915 Ginsenoside Ro

人参皂苷Ro,Chikusetsusaponin 5,Polysciasaponin P3,人参皂苷 Ro,Chikusetsusaponin V

Calcium Channel; Reductase; Prostaglandin Receptor Endocrinology/Hormones; GPCR/G Protein; Immunology/Inflammation; Membrane transporter/Ion channel; Metabolism
Ginsenoside Ro (Chikusetsusaponin V) 能降低 TXA2产量,较弱降低 COX-1 和 TXAS 活性,具有 Ca2+拮抗剂的抗血小板作用,IC50为 155 μM。
T4S1419 (±)-Praeruptorin A

Praeruptorin A,(±)-白花前胡甲素,白花前胡甲素,(-)-Praeruptorin A

p38 MAPK; Calcium Channel; Akt Cytoskeletal Signaling; MAPK; Membrane transporter/Ion channel; Metabolism; PI3K/Akt/mTOR signaling
(±)-Praeruptorin A 是来自白花前胡的干燥根中的一种主要成分,用于研究伴有厚痰和呼吸困难的咳嗽,非天生性咳嗽和上呼吸道感染。它是顺式-内酯 (CKL) 的二酯化产物,可作为 Ca2+-反流阻滞剂,用于高血压的研究。
T2S2215 Crebanine

Apoptosis; Others; Akt Apoptosis; Cytoskeletal Signaling; Others; PI3K/Akt/mTOR signaling
Crebanine 是来自于韦诺萨千金藤的一种生物碱,通过抑制 MAPKs 和 Akt 信号通路表现出抗炎活性,还具有抗心律失常的作用。它可诱导人类癌细胞的 G1阻滞和凋亡。
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。
T4S2326 Cornuside

7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside

ERK; p38 MAPK; NF-κB; JNK MAPK; NF-κB
Cornuside (Comuside) 是从山茱萸的果实中分离出的环烯醚萜苷,可用于炎症疾病的研究和促进血液循环。 它通过下调 MAPK 和 NF-κB 信号通路抑制肥大细胞介导的过敏反应,用于炎性过敏性疾病中的潜能。
TN1086 Dehydrotrametenolic acid

Dehydroeburicoic acid,去氢齿孔酸,松苓新酸

Apoptosis; TNF; NOS; Caspase; NO Synthase Apoptosis; Immunology/Inflammation; Proteases/Proteasome
Dehydrotrametenolic acid (Dehydroeburicoic acid) 是从茯苓的菌核中分离的一种甾醇,具有抗肿瘤活性、抗炎和抗糖尿病作用。它通过 caspase-3途径诱导细胞凋亡。

天然产物

Catharanthine
Cat.No: T2782
Synonym: (+)-3, 4-Didehydrocoronaridine,长春质碱,(+)-3,4-Didehydrocoronaridine
Target: Calcium Channel, AChR
Combretastatin A4
Cat.No: T6212
Synonym: CA4,康普瑞汀,Z)-3,4,5,4',-四甲氧基-3'-羟基二苯乙烯,CRC 87-09
Target: Microtubule Associated
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
Ginsenoside Ro
Cat.No: T3915
Synonym: 人参皂苷Ro,Chikusetsusaponin 5,Polysciasaponin P3,人参皂苷 Ro,Chikusetsusaponin V
Target: Calcium Channel, Reductase, Prostaglandin Receptor
(±)-Praeruptorin A
Cat.No: T4S1419
Synonym: Praeruptorin A,(±)-白花前胡甲素,白花前胡甲素,(-)-Praeruptorin A
Target: p38 MAPK, Calcium Channel, Akt
Crebanine
Cat.No: T2S2215
Synonym:
Target: Apoptosis, Others, Akt
β-Anhydroicaritin
Cat.No: T6S2140
Synonym: Anhydroicaritin,Beta-Anhydroicaritin,脱水淫羊藿素
Target: MMP, Others, TNF, Interleukin
Cornuside
Cat.No: T4S2326
Synonym: 7-Galloylsecologanol,7-O-Galloylsecologanol,山茱萸新苷,Comuside
Target: ERK, p38 MAPK, NF-κB, JNK
Dehydrotrametenolic acid
Cat.No: TN1086
Synonym: Dehydroeburicoic acid,去氢齿孔酸,松苓新酸
Target: Apoptosis, TNF, NOS, Caspase, NO Synthase
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