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抑制剂 & 化合物

1

天然产物

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Cat. No. Product Name Target Signaling Pathways
T14127 Adenosine A1 receptor activator T62

Adenosine Receptor GPCR/G Protein; Neuroscience
Adenosine A1 receptor activator T62 是腺苷 A1 受体的变构增强剂,有镇痛作用。
TP1559L Ziconotide Acetate (107452-89-1 free base)

醋酸齐考诺肽,Prialt,Ziconotide Acetate

Calcium Channel Membrane transporter/Ion channel; Metabolism
Ziconotide Acetate (107452-89-1 free base) (Prialt) 是一种镇痛剂,已用于治疗神经性和非神经性疼痛。 Ziconotide 通过与位于伤害感受通路初级传入神经元末端部分的 N 型钙通道结合起作用,因此通过有效的镇痛作用减少突触传递。
T41005 PA-8

PACAP GPCR/G Protein
PA-8是一种小分子的的 PACAP I 型(PAC1)受体拮抗剂,有 选择性、有效性和口服活性。PA-8抑制PACAP 诱导的CREB 在PAC1-受体上的磷酸化,但对VPAC11或VPAC2受体无抑制作用。PA-8也抑制pacap 诱导的体外cAMP 水平升高(IC50 = 2 nM)和体内鞘内注射后pacap 诱导的厌恶反应和机械异位性痛。
T1787 Levobupivacaine

Sodium Channel Membrane transporter/Ion channel
Levobupivacaine 是一种氨基酰胺类局麻药,属于n-alkylsubstituted pipecoloxylidide 家族。它是bupivacaine 的 S-对映异构体。
T3614 Inosine pranobex

Groprinosin,Isoprinosine,异丙肌苷,Immunovir,Delimmun

IL Receptor; HIV Protease Immunology/Inflammation; Microbiology/Virology; Proteases/Proteasome
Inosine pranobex (Delimmun) 是一种免疫增强剂,它是一种广谱抗病毒剂,用于 HIV 感染。
T71356 Lanperisone HCl

Lanperisone, also known as NK433, is a muscle relaxant. NK433 inhibited the facilitation of the flexor reflex mediated by group II afferent fibers that was induced by intrathecal administration of noradrenaline-HCl. NK433 had effects more than three times stronger and tending to be longer-lasting than those of eperisone-HCl. These results suggest that NK433 exerts a non-selective inhibition on spinal reflexes and that inhibition of the descending noradrenergic tonic facilitation within the spina...
T68592 Mafosfamide sodium

Mafosfamide sodium is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide sodium alkylates DNA, forming DNA cross-links and inhibiting DNA synthesis. Although closely related to cyclophosphamide, Mafosfamide sodium, unlike cyclophosphamide, does not require hepatic activation to generate its active metabolite 4-hydroxy-cyclophosphamide; accordingly, Mafosfamide sodium is potentially useful in the intrathecal treatment of neoplastic meningitis.
T68434 Mafosfamide

Mafosfamide is a synthetic oxazaphosphorine derivative with antineoplastic properties. Mafosfamide alkylates DNA, forming DNA cross-links and inhibiting DNA synthesis. Although closely related to cyclophosphamide, mafosfamide, unlike cyclophosphamide, does not require hepatic activation to generate its active metabolite 4-hydroxy-cyclophosphamide; accordingly, mafosfamide is potentially useful in the intrathecal treatment of neoplastic meningitis.
T37127 L-AP4 monohydrate

L-AP4 monohydrate

L-AP4 (L-APB) monohydrate is a potent and specific agonist for the group III mGluRs, with EC50s of 0.13, 0.29, 1.0, 249 μM for mGlu4, mGlu8, mGlu6 and mGlu7 receptors, respectively[1][2]. L-AP4 (5-30 μg, intrathecal inhection 4-5 days) significantly increases the paw withdrawal threshold in response to application of von Frey filaments in eight nerve-ligated rats in a dose-dependent manner. Intrathecal administration of different doses of L-AP4 is not associated with any evident motor dysfunctio...
T83739 Myr-Tat-CBD3 TFA

Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3

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。
T83674 K 41498 TFA

K 41498 是一种针对皮质酮释放因子受体2α(CRF2α)和CRF2β的肽拮抗剂,其在表达人类受体的HEK293细胞中的Ki值分别为0.66和0.62 nM。它对CRF2α和CRF2β具有选择性,与CRF1相比(在表达人类受体的HEK293细胞中Ki值为425 nM)。K 41498 (1.84 µg/动物, 静脉注射) 能够阻止大鼠由于尿催肾上腺皮质激素引发的低血压。通过脊髓内给药,K 41498 (0.075-0.5 µmol/动物) 能降低完全弗氏佐剂引起的大鼠模型中机械性爪撤回阈值。
T83731 Tat-CBD3 TFA

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。

化合物

Adenosine A1 receptor activator T62
Cat.No: T14127
Synonym:
Target: Adenosine Receptor
Ziconotide Acetate (107452-89-1 free base)
Cat.No: TP1559L
Synonym: 醋酸齐考诺肽,Prialt,Ziconotide Acetate
Target: Calcium Channel
PA-8
Cat.No: T41005
Synonym:
Target: PACAP
Levobupivacaine
Cat.No: T1787
Synonym:
Target: Sodium Channel
Inosine pranobex
Cat.No: T3614
Synonym: Groprinosin,Isoprinosine,异丙肌苷,Immunovir,Delimmun
Target: IL Receptor, HIV Protease
Lanperisone HCl
Cat.No: T71356
Synonym:
Target:
Mafosfamide sodium
Cat.No: T68592
Synonym:
Target:
Mafosfamide
Cat.No: T68434
Synonym:
Target:
L-AP4 monohydrate
Cat.No: T37127
Synonym: L-AP4 monohydrate
Target:
Myr-Tat-CBD3 TFA
Cat.No: T83739
Synonym: Myr-Tat-Calcium Channel-binding Domain 3,N-myristate-Tat-CBD3
Target:
K 41498 TFA
Cat.No: T83674
Synonym:
Target:
Tat-CBD3 TFA
Cat.No: T83731
Synonym:
Target:
Cat. No. Product Name Target Signaling Pathways
T5S0581 Sec-O-Glucosylhamaudol

亥茅酚苷,Hamaudol 3-glucoside

Others; Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience; Others
Sec-O-Glucosylhamaudol (Hamaudol 3-glucoside) 是从滨海前胡中分离得到的一种天然产物,能够降低 μ 阿片受体的蛋白水平,可用于缓解疼痛的研究。它通过调节脂多糖刺激的 RAW264.7 细胞系中的 p38 丝裂原活化蛋白激酶具有抗炎作用。

天然产物

Sec-O-Glucosylhamaudol
Cat.No: T5S0581
Synonym: 亥茅酚苷,Hamaudol 3-glucoside
Target: Others, Opioid Receptor
TargetMol Loading
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