1. GPCR/G Protein
  2. 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 (9):

Cat. No. Product Name Effect Purity
  • 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-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-17584
    Linaclotide Agonist 98.46%
    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-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 99.93%
    BAY 41-2272是一种可溶性鸟苷酸环化酶 (sGC) 活化剂。
  • HY-16774
    Vericiguat Activator >98.0%
    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
    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-14181A
    Cinaciguat hydrochloride Activator >98.0%
    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-100295
    (4-Acetamidocyclohexyl) nitrate Activator
    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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