22
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Cat. No. | Product Name | Target | Signaling Pathways |
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T27260 |
Emivirine
MKC442,MKC-442,MKC 442,DRG-0302,DRG 0302,DRG0302 |
HIV Protease | Microbiology/Virology; Proteases/Proteasome |
Emivirine (MKC-442) 是一种有效和选择性的人类免疫缺陷病毒1型(HIV-1)的非核苷逆转录酶抑制剂。 | |||
T7655 |
Fialuridine
DRG-0098,FIAU,非阿尿苷 |
DNA/RNA Synthesis | Cell Cycle/Checkpoint; DNA Damage/DNA Repair |
Fialuridine (DRG-0098) 是一种 DNA 导向的 DNA 聚合酶抑制剂,可能用于治疗 HBV 感染,在体外和体内对乙型肝炎病毒具有有效的活性。 | |||
T27790 |
Labradimil
RMP-7,ALK-01-040,Receptor-mediated permeabiliser-7,DRG0182,DRG 0182,DRG-0182 |
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Labradimil is a bradykinin B2 receptor agonist. Labradimil increases the permeability of human brain microvascular endothelial cell monolayers. Labradimil enhances delivery of hydrophilic chemotherapeutics and increases survival in rats with metastatic tu | |||
T19689 |
Raluridine
FddClUrd,935U-83,FCU,DRG-0215,BW-935U-83 |
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Raluridine is a RNA-directed DNA polymerase inhibitor potentially for the treatment of HIV infection. 935U83 inhibited virus growth with an average 50% inhibitory concentration (IC50: 1.8 microM) corresponding IC50s were 0.10 microM for FLT (3'-deoxy-3'-f | |||
T8538 |
ML382
|
Others | Others |
ML382 是选择性的 Mas 相关 G 蛋白偶联受体 X1MRGPRX1 (MrgX1)正向调节剂,其EC50=190 nM。 | |||
T6702L |
Terbinafine lactate
DRG-0286,Terbinafine hydrochloride,Lamisil Krem,SF 86-327 hydrochloride,Lamisil,Lamisil AT |
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Terbinafine, a synthetic allylamine antifungal, inhibits ergosterol synthesis by inhibiting squalene epoxidase, an enzyme that is part of the fungal cell membrane synthesis pathway. | |||
T23498 |
UNC3230
UNC 3230 |
Others | Others |
UNC3230 是一种 ATP 竞争性的磷脂酰肌醇 4 磷酸 5 激酶 1C 型 (PIP5K1C) 选择性抑制剂,其IC50约为 41 nM。它还可抑制PIP4K2C,但对其他调节磷酸肌醇水平的脂质激酶无抑制作用。它具有缓解疼痛和抗癌特性。 | |||
T7416 |
WS-12
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TRP/TRPV Channel | Membrane transporter/Ion channel |
WS-12 是有效的TRPM8激动剂,EC50为 39 nM。 | |||
T73469 |
SG2057
DRG16 |
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SG2057 (DRG16) 是一种含有戊二氧基键的 PBD 二聚体,该键选择性地结合DNA 小沟中的序列,形成 DNA 链间和链内交联加合物。SG2057 是一种高效抗肿瘤剂。 | |||
T4431 |
Olodanrigan
PD-126055,EMA401 |
RAAS | Endocrinology/Hormones |
Olodanrigan (EMA401) 是具有口服活性、高选择性及外周受限的血管紧张素 Ⅱ 类型 2 受体(AT2R)拮抗剂。它的缓解疼痛的机制可能是:抑制增强的 AngII/AT2R 诱导的 p38 和 p42/p44 MAPK 激活,进而阻碍 DRG 神经元的过度兴奋性及 DRG 神经元的萌发。它可用于研究神经性疼痛。 | |||
T67981 |
Copper histidine
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Copper histidine 抑制了Ctr1介导的奥沙利铂在体外的细胞摄取,而不会改变奥沙利铂在体内DRG 组织中的铂或神经毒性的积累。Copper histidine 通过口服治疗 Menkes 疾病。 | |||
T26745 |
BAY 73-1449
BAY-73-1449,BAY73-1449 |
Others | Others |
BAY 73-1449 是前列环素受体选择性拮抗剂,在人 HEL 细胞和大鼠 DRG 的 cAMP 分析中具有很高的效价,IC50小于 0.1 nM。BAY 73-1449在降血压方面有研究的价值。 | |||
T26376 |
11-deoxy-PGF2a
11-deoxyPGF2a,11-deoxy PGF2a |
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11-deoxy-PGF2a, a selective activator of TREK-2 channels, stimulates DRG c-fiber nociceptor K2P currents and limits calcium influx. | |||
T80448 |
ω-Conotoxin CVIF
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Calcium Channel | Membrane transporter/Ion channel; Metabolism |
ω-Conotoxin CVIF作为选择性Cav2.2通道抑制剂,对大鼠离体DRG神经元中Cav2.2通道的IC50为34.3 nM,其阻断作用表现为弱可逆。 | |||
T80455 |
ω-Conotoxin CVIB
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Sodium Channel | Membrane transporter/Ion channel |
ω-Conotoxin CVIB为非选择性N型及P/Q型电压门控钙通道(VGCC)拮抗剂,能够抑制背根神经节(DRG)中神经元去极化后激活全细胞VGCC电流,其pIC50值为7.64。 | |||
T16135 |
MRS 1523
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Others | Others |
MRS 1523 can exert an antihyperalgesic effect through N-type Ca channel block and action potential inhibition in isolated rat dorsal root ganglion (DRG) neurons. MRS 1523 is an effective and selective adenosine A3 receptor antagonist Ki: 18.9 nM and 113 n | |||
T80421 |
CSD-CH2(1,8)-NH2
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Opioid Receptor | Endocrinology/Hormones; GPCR/G Protein; Neuroscience |
CSD-CH2(1,8)-NH2 是一种针对KOR的选择性且竞争性拮抗剂,具有较低的Ki值(6.8 nM),能够抑制DRG神经元内的钙动员,并能拮抗U50,488的抗伤害效应,常用于神经精神疾病研究领域。 | |||
T83739 |
Myr-Tat-CBD3 TFA
Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3 |
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Myr-Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白-蛋白相互作用的抑制剂。在10 µM的浓度下,该化合物能够约81%地抑制Cav2.2-CRMP2相互作用,并在大鼠初级背根神经节(DRG)神经元中抑制钾诱导的钙流入(IC50约为2.8 µM)。在20 µM的浓度下,Myr-Tat-CBD3能抑制钙电流,但不影响钠电流,在初级DRG神经元中表现出这种特性。经过脊髓内给药,myr-Tat-CBD3(20 µg/5 µl)能够防止大鼠脚掌撤回潜伏期因carrageenan注射而减少。此外,Myr-Tat-CBD3减少大鼠因线索引起的寻求可卡因行为的复发。 | |||
T37201 |
CAY10787
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CAY10787 is an oxysterol and a negative allosteric modulator of GABAAreceptors.1,2It reduces GABA-induced currents in HEK cells expressing α1β1γ2or α4β3γ2subunit-containing GABAAreceptors (IC50s = 1.5 and 1 μM, respectively).2CAY10787 (500 nM) reduces GABA-induced depolarization of peptidergic and non-peptidergic nociceptors, C-LTMRs, and cold thermosensors in isolated mouse dorsal root ganglion (DRG) neurons.In vivo, CAY10787 (2, 10, and 50 mg/kg) increases latency to nocifensive behaviors in t... | |||
T83732 |
Tat-CBD3A6K TFA
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Tat-CBD3A6K是一种肽类化合物,为N型电压门控钙通道Cav2.2以及collapsin response mediator protein 2 (CRMP2) 蛋白-蛋白相互作用抑制剂Tat-CBD3的衍生物。Tat-CBD3A6K (10 mg/kg) 能够阻止由d4T (stavudine)引发的大鼠抗逆转录病毒神经病痛模型中爪撤回阈值的下降,并减少同一大鼠分离的背根神经节(DRG)神经元的动作电位数量。通过硬膜途径给予Tat-CBD3A6K (30 µM/animal) 能够减少由萜类生物碱辣椒素引发的大鼠硬脑膜血流增加。 | |||
T83731 |
Tat-CBD3 TFA
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Tat-CBD3是一种抑制N型电压门控钙通道Cav2.2与collapsin response mediator protein 2 (CRMP2)之间的蛋白质-蛋白质相互作用的抑制剂。它还能抑制CRMP2与NMDA受体NR2B亚单位之间的蛋白质-蛋白质相互作用。在无细胞实验中,Tat-CBD3 (10 µM)能将Cav2.2-CRMP2相互作用抑制43%,并在免疫共沉淀实验中抑制NMDA受体NR2B亚单位-CRMP2相互作用。它能在初级大鼠背根神经节 (DRG) 神经元中减少约60%的电压诱导钙电流,并在初级大鼠海马神经元中减少谷氨酸诱导的胞内钙水平增加。Tat-CBD3 (20 mg/kg)在大鼠中脑动脉闭塞 (MCAO) 引发的脑缺血模型中减少梗死体积。鞘内给药Tat-CBD3 (20 µg/5 µl)可防止大鼠卡拉胶诱导的热敏感性。 | |||
T83728 |
Tat-AKAP79 (326-336) TFA
Tat-A-kinase Anchor Protein 79 (326-336) |
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Tat-AKAP79 (326-336) 是一种肽,由HIV-1 Tat蛋白质转导域与对应于A-kinase anchor protein 79 (AKAP79) 326至336残基的11个氨基酸肽链相连组成。在200 µM浓度下,能抑制蛋白激酶A (PKA) 或PKC激活诱导的瞬时受体电位钒通道1 (TRPV1) 在分离的大鼠背根神经节 (DRG) 神经元中的敏感化。在体内,Tat-AKAP79 (326-336) 抑制小鼠由甲醛或phorbol 12-myristate 13-acetate (PMA014) 引发的伤害性行为。它还延长了小鼠对辐射热刺激爪子撤回的潜伏期,并在卡拉胶诱导的炎症性疼痛小鼠模型中增加了爪子撤回的机械阈力。 |
Cat. No. | Product Name | Target | Signaling Pathways |
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T2173 |
Veratridine
|
Sodium Channel | Membrane transporter/Ion channel |
Veratridine 是一种生物碱,来自百合科植物。Veratridine 是一种钠通道激动剂, 对 Nav1.7 的峰值电流具有抑制作用,IC50为 18.39 µM。 | |||
TN1087 |
Deoxypodophyllotoxin
脱氧鬼臼毒素,去氧鬼臼毒素 |
Apoptosis; Microtubule Associated; Autophagy | Apoptosis; Autophagy; Cytoskeletal Signaling |
Deoxypodophyllotoxin 是从桃儿七根茎分离的一种木酚素,是鬼臼毒素衍生物,具有抗有丝分裂和抗病毒特性。它是血管生成抑制剂,作为靶向微管药物,在肿瘤学中具有重大影响。它引起 DRG 神经元细胞内 Ca2+浓度增加,诱导细胞自噬和凋亡。 | |||
T37219 |
N-Palmitoyl Glycine
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The acyl amides are a family of endogenous lipids that act as potent modulators of pain and inflammation. The best characterized members of this family are the arachidonoyl amides, which includes N-arachidonoyl ethanolamide (AEA; anandamide). N-palmitoyl glycine (PalGly) contains an 18-carbon saturated fatty acid that is amide-linked to glycine and is structurally similar to the phospholipid-derived N-acyl ethanolamines. Endogenously produced in rat skin and spinal cord, PalGly is present in 100... |