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抑制剂&激动剂
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  • 抑制剂&激动剂
    33
    TargetMol | Inhibitors_Agonists
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    TargetMol | Recombinant_Protein
  • 多肽产品
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    TargetMol | Peptide_Products
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  • Piribedil
    吡贝地尔, Trivastan, Trivastal, EU-4200, ET-495
    T32783605-01-4
    Piribedil (Trivastan) 是多巴胺 D2受体激动剂,对 hα1A-肾上腺素受体也显示出拮抗作用。
    • ¥ 291
    In stock
    规格
    数量
  • Vamicamide
    戊米胺, FK-176, FK176, FK 176
    T35033132373-81-0In house
    Vamicamide (FK 176)是一种新型抗胆碱能化合物。Vamicamide 在 32 mg kg (p.o.)或更高时增加小鼠的自发运动活动,并在 100 mg kg 时抑制小鼠强直性惊厥。
    • ¥ 2620 TargetMol
    In stock
    规格
    数量
  • (S)-Vamicamide
    (S)-伐米胺, (S)-Vamicamide (Iso-132373-81-0)
    T35033L151851-72-8In house
    (S)-Vamicamide 是一种新型抗抗胆碱能化合物。Vamicamide 在 32 mg kg 或更高 (p.o.) 时增加小鼠的自发运动活动,并在 100 mg kg 时抑制小鼠强直性惊厥。
    • ¥ 1300 TargetMol
    In stock
    规格
    数量
  • L-Allylglycine
    L-烯丙基甘氨酸
    T3719016338-48-0
    L-Allylglycine 是 GABA 合成酶(谷氨酸脱羧酶)的有效抑制剂。
    • ¥ 99
    In stock
    规格
    数量
  • Qingyangshengenin B
    青阳参甙元B, 青阳参苷元B, Otophylloside B
    TMS1461106758-54-7
    Qingyangshengenin B (Otophylloside B) 是一种分离自 Qingyangshen 的 C-21 甾体苷。它能够在 mRNA 水平上抑制 Aβ 的表达来减少 Aβ 的沉积,对 Aβ 的毒性有保护作用。它具有抗癫痫作用。
    • ¥ 495
    In stock
    规格
    数量
  • RDS-127
    RDS127, RDS 127
    T20243782668-32-4
    RDS-127在大鼠自发运动活动中引起双相剂量相关变化,与APO的报告效果相似。与APO相比,RDS-127的运动刺激效果更为强烈,其效力增强3倍,持续时间延长4倍。在选择性上,RDS-127明显优于APO,它更倾向于激活黑质纹状体途径中的DA自身受体,而不是突触后DA受体。
    • 待询
    10-14周
    规格
    数量
  • RTI-51
    RTI51, RTI4229-51, RTI-4229-51
    T202777135367-08-7
    RTI-51可显著提高运动活性,可能作为治疗可卡因使用的化合物。RTI-51具有高效、选择性强且持久的替代作用,可减少寻药行为。
    • 待询
    10-14周
    规格
    数量
  • (R)-AS-1
    T2032602506367-95-7
    (R)-AS-1 是一种选择性激动性氨基酸转运体2 (EAAT2) 的正向异构调节剂,其EC50为11 nM。(R)-AS-1 以60和90 mg kg剂量显著增加小鼠的自发运动活动。在最大电休克 (MES)、戊四氮 (PTZ) 和电流刺激 (32或44 mA) 所引发的小鼠癫痫模型中,(R)-AS-1 显示出抗癫痫活性,ED50分别为66.3、36.3、15.6和41.6 mg kg。此化合物可应用于神经疾病的研究。
    • 待询
    10-14周
    规格
    数量
  • 5-HT2C agonist-4
    T2035702730085-33-1
    5-HT2C agonist-4 (Compound 3i) 是一种5-HT2C receptor激动剂,其EC50值为5.7 nM,并能降低幼年斑马鱼幼虫的运动活性。
    • 待询
    10-14周
    规格
    数量
  • ZCZ011
    ZCZ 011,ZCZ-011
    T292061998197-39-9
    ZCZ011 is a positive allosteric modulator of the cannabinoid CB1 receptor. ZCZ011 is brain penetrant, increased the potency of orthosteric agonists in mouse behavioral assays indicative of cannabimimetic activity, including antinociception, hypothermia, c
    • ¥ 1920
    5日内发货
    规格
    数量
  • ZK-95962
    T29230101071-43-6
    ZK-95962 is an agonist gamma-aminobutyric acid (GABA) receptor. ZK-95962 had selective effects on releasing exploratory locomotor activity suppressed by footshock (punished crossings). ZK-95962 had weak effects on the measures of anxiolytic activity. The
    • ¥ 11700
    6-8周
    规格
    数量
  • SR9009
    Stenabolic, REV-ERB Agonist II
    T36851379686-30-2
    SR9009 (Stenabolic) 是一种REV-ERBα β激动剂,可增加由 REV-ERBα ERBβ 调节的基因的组成性抑制,IC50分别为 670 nM 和 800 nM。
    • ¥ 219
    In stock
    规格
    数量
  • RO 5263397 hydrochloride
    T38172
    Potent trace amine 1 (TA1) receptor agonist (EC50 values are 0.12, 35 and 17-85 nM for mouse, rat and human receptors, respectively). Increases wakefulness and reduces REM and NREM sleep duration in wild type mice. Inhibits spontaneous locomotor activity in dopamine transport (DAT) knockout mice. Espinoza et al (2018) Biochemical and functional characterization of the trace amine-associated receptor 1 (TAAR1) agonist RO5263397. Front.Pharmacol. 9 645 PMID:29977204 |Galley et al (2015) Discovery and characterization of 2-aminooxazolines as highly potent, selective, and orally active TAAR1 agonists. ACS.Med.Chem.Letts. 7 192 PMID:26985297 |Schwartz et al (2017) Trace amine-associated receptor 1 regulates wakefulness and EEG spectral composition. Neuropsychopharmacology. 42 1305 PMID:27658486
    • 待估
    35日内发货
    规格
    数量
  • N,N-Dipropyldopamine (hydrobromide)
    T3822165273-66-7
    N,N-Dipropyldopamine is a dopamine receptor agonist.1,2,3 It decreases dihydrophenylalanine (DOPA) levels in the limbic forebrain and striatum of reserpinized rats (ED50s = 25 and 20 μmol kg, respectively), as well as reduces homovanillic acid levels in rat striatum when administered at a dose of 80 μmol kg.1 N,N-Dipropyldopamine (0.5-16 mg kg) reduces spontaneous locomotor activity in mice, an effect that can be reversed by the antipsychotic spiroperidol.2,3
    • 待估
    35日内发货
    规格
    数量
  • (R)-Preclamol
    T6027085976-54-1
    (R)-Preclamol 是一种具有自身受体和突触后受体刺激特性的多巴胺 (DA) 激动剂。(R)-Preclamol 以低剂量抑制小鼠和大鼠的运动活动。
    • ¥ 882
    5日内发货
    规格
    数量
  • SB-334867 free base
    SB334867A free base, SB-334867, SB334867, SB 334867
    T6140792173-99-0
    SB-334867 free base (SB334867A free base) 是一种选择性 orexin-1(OX1) 受体拮抗剂,对 OX2有选择性,pKb 为7.4,对 5-HT2B、5-HT2C 的选择性是 100 倍,pKi 值分别为 5.4 和 5.3。它减少乙醇消耗,还抑制吗啡诱导的体内运动活动敏感性的获得。
    • ¥ 223
    In stock
    规格
    数量
  • RO-5328673
    T710001310817-94-7
    RO-5328673 is a dual NK2 NK3 antagonist. O5328673. [(3)H]RO5328673 bound to a single saturable site on hNK2, hNK3 and gpNK3 with high-affinity. RO5328673 acted as an insurmountable antagonist at both human and guinea-pig NK3 receptors in the [(3)H]IP accumulation assay. In binding kinetic analyses, [(3)H]RO5328673 had fast association and dissociation rates at hNK2 while it had a fast association rate and a remarkably slow dissociation rate at gp and hNK3. In electrophysiological recordings of gp SNpc, RO5328673 inhibited the senktide-induced potentiation of spontaneous activity of dopaminergic neurons with an insurmountable mechanism of action. RO5328673 exhibited in-vivo activity in gerbils, robustly reversing the senktide-induced locomotor activity.
    • ¥ 15000
    8-10周
    规格
    数量
  • Paraxanthine-d6
    T71327117490-41-2
    Paraxanthine-d6 is intended for use as an internal standard for the quantification of paraxanthine by GC- or LC-MS. Paraxanthine is an active metabolite of caffeine. It is formed via N3-demethylation of caffeine by the cytochrome P450 (CYP) isoform CYP1A2. Paraxanthine is an adenosine A1 and A2 receptor antagonist. In vivo, paraxanthine increases striatal cGMP and extracellular striatal dopamine levels and locomotor activity, as well as inhibits motor depression induced by the adenosine A1 agonist CPA or the adenosine A2 receptor agonist CGS 21680 in rats not habituated to caffeine. It also promotes wakefulness and increases locomotor activity and core temperature in narcoleptic transgenic mice without increasing behavioral anxiety.
    • 待估
    35日内发货
    规格
    数量
  • CTOP TFA
    T75915
    CTOP TFA为高效、高选择性μ-阿片受体(μ-opioid receptor)拮抗剂。其能拮抗吗啡引发的急性镇痛效果及运动能力增强,同时升高伏隔核外多巴胺水平,并呈剂量依赖性增强运动能力。
    • 待询
    规格
    数量
  • Neuropeptide S(Mouse) TFA
    T75950
    Neuropeptide S(Mouse) TFA, an endogenous agonist for the neuropeptide S receptor (NPSR) with an EC50 value of 3 nM, plays a significant role in physiological processes by inducing the mobilization of intracellular Ca2+. This compound elevates locomotor activity and wakefulness, and simultaneously decreases anxiety-like behavior in mice.
    • 待询
    规格
    数量
  • Neuropeptide S(Rat) TFA
    T75951
    Neuropeptide S(Rat) TFA, a robust endogenous agonist for the neuropeptide S receptor (NSPR) with an EC50 of 3.2 nM, enhances locomotor activity and promotes wakefulness while concurrently diminishing anxiety-like behavior in mice.
    • 待询
    规格
    数量
  • NocII TFA
    T81659
    NocII TFA 是孤儿神经肽,能刺激小鼠运动。
    • 待询
    规格
    数量
  • Delta (Phospho) Sleep Inducing Peptide
    DSIP-P
    T8258770754-23-3
    Delta (Phospho) Sleep Inducing Peptide (DSIP-P) 是促进睡眠效应持久的多肽,能诱导大鼠昼夜运动行为的改变。
    • 待询
    规格
    数量
  • Adipokinetic hormone (Gryllus bimaculatus)
    Grybi-AKH
    T83166113800-65-0
    Adipokinetic hormone Gryllus bimaculatus (Grybi-AKH) 是调节昆虫能量平衡的脂肪动力激素,主要功能是动员脂肪体内的脂质和碳水化合物。此外,Grybi-AKH也能增强双斑蟋蟀的运动活性,并在人体体重调节、体重减轻及糖原贮积障碍缓解的研究中具有应用潜力。
    • 待询
    规格
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