1. Signaling Pathways
  2. GPCR/G Protein
  3. Guanylate Cyclase

Guanylate Cyclase

Guanylatecyclase (guanylylcyclase, GC) is a lyase enzyme. Guanylylcyclase is often part of the G protein signaling cascade that is activated by low intracellular calcium levels and inhibited by high intracellular calcium levels. In response to calcium levels, guanylylcyclase synthesizes cGMP from GTP. cGMP keeps cGMP-gated channels open, allowing for the entry of calcium into the cell. The guanylylcyclase activity is modulated by the calcium-binding guanylylcyclase activating proteins (GCAP1 and GCAP2). A key mechanism by which Ca2+ modulates phototransduction in rods involves the synthesis of cGMP by guanylylcyclase (GC), regulated by a pair of Ca2+-binding GuanylylCyclase Activating Proteins (GCAP1 and GCAP2).

The second messenger cyclic guanosine monophosphate (cGMP) is generated by the heterodimeric α/β-heme protein soluble guanylatecyclase (sGC) upon activation by its endogenous ligand nitric oxide (NO). NO binds to the reduced prosthetic heme group bound to the β subunit. cGMP is a key mediator of the cardiovascular system and its effects lead to vasodilation, inhibition of smooth muscle proliferation, blockade of leukocyte infiltration and inhibition of platelet aggregation. Impairment of the cytoprotective NO/sGC/cGMP-signalling pathway is associated with the development of serious cardiovascular diseases such as hypertension or heart failure.

Guanylate Cyclase 相关产品 (15):

Cat. No. Product Name Effect Purity
  • HY-17584
    Linaclotide Agonist 98.18%
    Linaclotide是一种有效和选择性的鸟苷酸环化酶C激动剂;开发用于治疗便秘型肠易激综合症 (IBS-C) 和慢性便秘。
  • HY-14927
    Lificiguat Activator 99.83%
    Lificiguat 结合到 可溶性鸟苷酸环化酶(sGC)的β亚基,在CO存在条件下,Kd 为 0.6-1.1 μM。
  • HY-14779
    Riociguat Activator 99.58%
    Riociguat 是一种可口服的可溶性鸟苷酸环化酶 (sGC) 刺激剂,常用于治疗肺动脉高压症。
  • HY-14181
    Cinaciguat Activator 99.40%
    Cinaciguat hydrochloride是一种不依赖于一氧化氮的鸟苷酸环化酶 (GC) 活化剂,Kd 值为3.2 nM。
  • HY-12376
    BAY 41-2272 Activator 99.88%
    BAY 41-2272是一种可溶性鸟苷酸环化酶 (sGC) 活化剂。
  • HY-12379
    NS-2028 Inhibitor 99.91%
    NS-2028 是一种高选择性可溶性鸟苷酸环化酶 (sGC) 抑制剂, 其 basal 和 NO 刺激的酶活性的 IC50 值分别为 30 nM 和 200 nM。NS-2028 抑制小鼠小脑匀浆和神经元 NO 合酶中的可溶性鸟苷酸环化酶活性, IC50值分别为17 nM和20 nM。NS-2028 抑制 3-吗啉代-sydnonimine (SIN-1) 在人培养的脐静脉内皮细胞中形成环状GMP,IC50 值为30 nM。NS-2028 常用于一氧化氮信号通路的研究,它完全抑制非血管平滑肌中 NO 依赖性松弛反应 (1μM)。NS-2028 可降低血管内皮生长因子诱导的血管生成和通透性。
  • HY-16774
    Vericiguat Activator 99.09%
    Vericiguat (BAY1021189) 是有效的,有口服活性的,可溶的鸟苷酸环化酶 (guanylate cyclase) 刺激物。
  • HY-78237
    Nelociguat Activator 99.73%
    Nelociguat (BAY60-4552)是一种一氧化氮敏感的可溶性的鸟苷酸环化酶激活物。
  • HY-108741A
    Plecanatide acetate Agonist 99.26%
    Plecanatide acetate 是一种鸟苷酸环化酶 C 受体 (guanylate cyclase-C (GC-C) receptor) 激动剂,在 T84 细胞中,EC50 值为 190 nM。在小鼠结肠炎模型中,Plecanatide acetate 具有抗炎活性。
  • HY-14181A
    Cinaciguat hydrochloride Activator 99.64%
    Cinaciguat hydrochloride 是一种有效的可溶性鸟苷酸环化酶 (GC) 活化剂,在血小板中 EC50 值为 15 nM。
  • HY-109066
    Olinciguat Activator
    Olinciguat (IW-1701) 是一种可口服的鸟苷酸环化酶 (guanylate cyclase, sGC) 刺激剂,在纯化的大鼠和人类酶实验和全细胞实验中刺激 sGC,这种作用具有浓度依赖性。
  • HY-109039
    Praliciguat Activator
    Praliciguat (IW-1973) 是一种有效、可口服的可溶性鸟甘酸环化酶 (soluble guanylate cyclase) 促进剂,增强 NO 信号通路,为血管舒张剂。在 HEK-293 细胞中,Praliciguat (IW-1973) 能够刺激 sGC,EC50 值为 197 nM。
  • HY-111516
    sGC activator 1 Activator
    sGC activator 1 (Compound (+)-23) 是一种可溶性鸟苷酸环化酶 (sGC) 活化剂,在 CHO 和 GTM-3E 细胞中 EC50 分别为 <5 nM 和 5 nM。
  • HY-109136
    Runcaciguat Activator
    Runcaciguat 是一种可口服的可溶性鸟甘酸环化酶 soluble guanylate cyclase 促进剂,可结合选择性的部分 adenosine A1 受体激动剂用于研究心血管及肾病。
  • HY-100295
    (4-Acetamidocyclohexyl) nitrate Activator
    (4-Acetamidocyclohexyl) nitrate (BM121307) 是一种鸟苷酸环化酶 (guanylate cyclase) 激活剂,之前其处于临床I期开发用于治疗缺血性心脏病。此项研究已经停止。
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