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抑制剂&激动剂
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  • 抑制剂&激动剂
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    TargetMol | Inhibitors_Agonists
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    TargetMol | Natural_Products
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    TargetMol | Isotope_Products
  • SB 204741
    T23312152239-46-8
    SB 204741 是一种选择性的5-HT2B 拮抗剂,具有高亲和性,pKi 值为7.1。
    • ¥ 563
    In stock
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  • Bisaramil hydrochloride
    RGH-2957, RGH 2957, NK-1556, NK1556, NK 1556, Bisaramil hcl
    T2682296480-44-3In house
    Bisaramil hydrochloride (Bisaramil) 是一种新型二氮双环壬烷抗心律失常化合物,抑制自由基生成。Bisaramil hydrochloride 可阻断钠电流,抑制异丙肾上腺素在 K(+) 去极化肌上诱导的缓慢 Ca(2+) 动作电位。
    • ¥ 1980 TargetMol
    In stock
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  • Sinapinic Acid
    芥子酸, Synapoic acid, Sinapic acid
    T3753530-59-6
    Sinapinic Acid (Synapoic acid) 是从 Hydnophytum formicarumJack. 根中分离到的酚类,是HDAC 抑制剂,对ACE-I 的活性也有抑制作用。它有抗肿瘤活性,诱导肿瘤细胞凋亡,具有抗氧化、抗糖尿病的作用。
    • ¥ 119
    In stock
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  • O-Desmethylcarvedilol
    O-去甲卡维地洛, Desmethylcarvedilol, BM-14242
    T20308372956-44-6
    O-Desmethylcarvedilol (Desmethylcarvedilol) 是 Carvedilol 的活性代谢物,为一种非选择性 β-肾上腺素受体 (β-AR) 拮抗剂。该化合物能够抑制在表达瑞安诺丁受体 2 (RyR2) R4496C 突变的 HEK293 细胞中由储存超载所引发的钙释放,其 IC50 为 7.62 µM。此外,O-Desmethylcarvedilol 可以在清醒兔子中减缓心率上升,并预防 Isoproterenol 诱导的舒张压下降,ED50 分别为 32 和 5 µg kg。
    • 待询
    10-14周
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  • Esmolol acid hydrochloride
    盐酸艾司洛尔酸, ASL-8123 hydrochloride
    T20311983356-60-9
    Esmolol acid (ASL-8123) hydrochloride 是一种弱效的β-肾上腺素能受体拮抗剂。Esmolol acid hydrochloride 能以剂量依赖的方式抑制 Isoproterenol 诱导的心率及舒张压变化,可用于肾衰竭的相关研究。
    • 待询
    10-14周
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  • AZ 1729
    T378962016864-46-1
    FFA2 allosteric agonist. Inhibits forskolin-induced cAMP increase and stimulates 35SGTPγS binding in biochemical assays (pEC50 values are 6.9 and 7.23, respectively). Binds at allosteric binding site. In functional assays, displays positive allosteric modulation of FFA-induced Gi signaling and negative allosteric modulation of FFA-induced Gq/G11 signaling. Inhibits lipolytic effect of isoproterenol (pEC50 = 5.03) and induces migration of human neutrophils in vitro. Bolognini et al (2016) A novel allosteric activator of free fatty acid 2 receptor displays unique Gi-functional bias. J.Biol.Chem. 291 18915 PMID:27385588 |Sergeev et al (2017) A single extracellular amino acid in free fatty acid receptor 2 defines antagonist species selectivity and G protein selection bias. Sci.Rep. 7 13741 PMID:29061999
    • 待估
    35日内发货
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  • Isoproterenol-d7 HCl
    T695982517584-04-0
    Isoproterenol-d7 is intended for use as an internal standard for the quantification of isoproterenol by GC- or LC-MS. Isoproterenol is an agonist of β1- and β2-adrenergic receptors (β1- and β2-ARs; Kis = 224 and 458 nM, respectively). It is selective for β1- and β2-ARs over β3-ARs (Ki = 1,570 nM). Isoproterenol inhibits contractions in isolated field-stimulated rat vas deferens (EC50 = 45.6 nM). In vivo, isoproterenol (0.33 mg kg) decreases blood pressure and increases water intake in nephrectomized rats. It reduces blood pressure and increases heart rate in renal hypertensive rabbits. Isoproterenol inhibits histamine-induced bronchospasms in anesthetized dogs. Formulations containing isoproterenol have been used in the treatment of bradydysrhythmias and to improve breathing during anesthesia.
    • 待估
    35日内发货
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  • Fenspiride-d5
    T711411246911-67-0
    Fenspiride-d5 is intended for use as an internal standard for the quantification of fenspiride by GC- or LC-MS. Fenspiride is an antagonist of histamine H1 receptors and a non-steroidal anti-inflammatory drug (NSAID). It inhibits histamine-induced contraction of isolated guinea pig trachea but not histamine-induced inotropy of isolated guinea pig heart. It also inhibits phosphodiesterase 4 (PDE4), PDE5, and PDE3 (IC50s = 69, ~158, and 363 µM, respectively, in isolated human bronchi derived from patients with lung cancer). It is selective for these phosphodiesterases over PDE1 and PDE2, where it provides less than 25% inhibition. Fenspiride potentiates the airway relaxant effects of isoproterenol and sodium nitroprusside indicating an effect on cAMP and cGMP phosphodiesterases, respectively. Aerosolized fenspiride (1 mg ml) reverses bronchoconstriction induced by capsaicin and, when used at aerosolized concentrations ranging from 1-10 mg ml, reduces cough induced by citric aci......
    • 待估
    35日内发货
    规格
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  • INF 195
    INF-195, INF195
    T879451211379-56-4
    INF 195 是一种炎性小体 NLRP3 抑制剂,抑制 NLRP3 驱动的巨噬细胞焦亡 和 IL-1β 释放。INF 195 可减轻异丙肾上腺素诱导的 H9c2 大鼠成肌细胞肥大,可用于研究心肌缺血和心肌梗死。
    • ¥ 113
    In stock
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