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21

抑制剂 & 化合物

3

天然产物

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Cat. No. Product Name Target Signaling Pathways
T40481 IBS008738

IBS008738, a potent TAZ activator, stabilizes TAZ, elevates the unphosphorylated TAZ level, enhances the interaction of MyoD with the myogenin promoter, upregulates gene transcription regulated by MyoD, and competes with myostatin in C2C12 cells. Additionally, IBS008738 promotes myogenesis in C2C12 cells and facilitates muscle repair in a model of muscle injury.
T5491 GSK3179106

c-RET Apoptosis; Tyrosine Kinase/Adaptors
GSK3179106 是选择性的、具有口服活性的RET 激酶抑制剂,对人和大鼠 RET 的 IC50 分别为 0.4 nM 和 0.2 nM。它能够减轻炎症后和应激引起的内脏超敏反应,对肠易激综合征具有潜在的应用价值。
T1460 Dicyclomine hydrochloride

AChR Neuroscience
Dicyclomine hydrochloride 是口服活性毒蕈碱胆碱能受体拮抗剂。它是一种抗痉挛试剂,在体内可缓解胃肠道平滑肌痉挛。它对 M1 受体亚型和 M2 受体亚型,Ki 分别为5.1和54.6nM,在刷状缘膜和基底质膜中均表现出较高的亲和力。
T1006 Propantheline bromide

Neopepulsan,溴丙胺太林,Pro-Banthine,Neometantyl

AChR Neuroscience
Propantheline bromide (Pro-Banthine) 是一种抗毒蕈碱剂,用于研究多汗症,遗尿,胃肠和膀胱痉挛。
T1551 Tegaserod maleate

HTF-919,马来酸替加色罗,SDZ-HTF-919

5-HT Receptor GPCR/G Protein; Neuroscience
Tegaserod maleate (SDZ-HTF-919) 是选择性5-HT4受体的部分激动剂和5-HT2B 受体的拮抗剂,用于治疗肠易激综合征和便秘。
T26802 BIBS-222

BIBS 222

BIBS-222, a nonpeptide angiotensin II (Ang II) receptor antagonist, appears to be an effective antihypertensive in the model of the renal hypertensive rat.
T3178 BIBS 39

RAAS Endocrinology/Hormones
BIBS 39是新型的非肽类血管紧张素II(AII)受体拮抗剂。
T38507 Renzapride

BRL 24924

5-HT Receptor GPCR/G Protein; Neuroscience
Renzapride (BRL 24924) 是一种混合 5-羟色胺 4 型 (5-HT4) 激动剂和 5-HT3 受体拮抗剂。Renzapride 可用于研究以便秘为主的肠易激综合征(C-IBS)。
T60680 Tegaserod

5-HT Receptor GPCR/G Protein; Neuroscience
Tegaserod 是一种可口服的 5-HT4R 激动剂和 5-HT2B 受体拮抗剂,对多种5-羟色胺受体具有抑制作用。 Tegaserod 具有抗肿瘤活性,用于治疗肠易激综合征 (IBS)。
T11852 Linaclotide

Guanylate cyclase GPCR/G Protein
Linaclotide 是一种有效的选择性鸟苷酸环化酶 C 激动剂,可用于治疗便秘型肠易激综合征 (IBS-C) 和慢性便秘的研究。
T0918 Trimebutine

曲美布汀,Mebutin

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Trimebutine (Mebutin) 是阿片受体激动剂,有抗毒蕈碱活性。它是解痉剂,可调节肠道和结肠运动,并通过抗毒蕈碱和弱μ-阿片受体激动剂作用缓解腹痛。
T30936 Cilansetron Hydrochloride

KC-9946,KC9946,KC 9946

Cilansetron Hydrochloride can be used for irritable Bowel Syndrome (IBS) with Diarrhea Predominance.
T21235 Alosetron

Lotronex,GR68755,GR-68755,GR 68755,阿洛司琼

Alosetron, a 5-HT3 antagonist, is used for the management of severe diarrhea-predominant irritable bowel syndrome (IBS) in women only.
T24887 Tiropramide

CR-605

Tiropramide is an antispasmodic drug. It also useful to inhibit the contractile response of the urinary bladder and in managing abdominal pain in IBS.
T13002 SSR-241586

Others Others
SSR-241586 is a neurokinin receptors antagonist,and is shown to be active in the treatment of depression, schizophrenia, urinary trouble, emesis, and irritable bowel syndrome (IBS).
T4633 Asimadoline

EMD-61753,阿西马朵林

Opioid Receptor Endocrinology/Hormones; GPCR/G Protein; Neuroscience
Asimadoline (EMD-61753) 是一种 κ-阿片(κ-opioid)受体激动剂,对豚鼠和人重组 κ-opioid 的IC50值分别为 5.6 和 1.2 nM。它可改善糖尿病大鼠的异常性疼痛,具有外周抗炎作用,并有用于肠易激综合征的研究潜力。
T38482 MM 419447

MM 419447 is a guanylate cyclase-C agonist, and it is a metabolite of linaclotide. This compound, MM 419447, shows promise in the field of irritable bowel syndrome with constipation (IBS-C) research.
T63877 RET-IN-17

RET-IN-17 是 RET 的有效抑制剂。RET-IN-17 具有潜力进行与 IBS 和其他胃肠道疾病相关的疼痛以及具有组成性 RET 激酶活性的癌症的研究。
T72809 (S)-Renzapride

(S)-BRL 24924

(S)-Renzapride ((S)-BRL 24924) 是 Renzapride 的异构体。Renzapride 是一种 5-HT4受体激动剂,Ki 值为 115 nM。Renzapride 还是一种5HT2b 和5HT3受体拮抗剂。Renzapride 可用于便秘型肠易激综合征(C-IBS)的研究。
T64234 Alosetron (Hydrochloride(1:X))

Alosetron (GR 68755) Hydrochloride (1:X) 是一种高效的、具有高度选择性的、具有抗炎作用的 5-HT3 受体 (5-HT3 receptor) 拮抗剂。Alosetron Hydrochloride (1:X) 能够阻断 5HT3 介导的豚鼠肌间和粘膜下神经元的快速去极化(IC50:~55 nM)。Alosetron Hydrochloride (1:X) 能够减缓清醒或麻醉犬直肠扩张的内脏伤害性效应。Alosetron Hydrochloride (1:X) 能够用于研究肠易激综合征 (IBS)。
T78084 PSB 0777 ammonium hydrate

Adenosine Receptor GPCR/G Protein; Neuroscience
PSB 0777 ammonium hydrate 是一种选择性腺苷A2A受体激动剂,Ki值对大鼠A2A受体为44.4 nM,对人A2A受体为360 nM。对大鼠A1受体的Ki值≥10000 nM,对人A1受体为541 nM。该化合物大脑渗透性和口服生物利用度较差,但显示在炎性肠病(IBS)研究中的应用潜力。

化合物

IBS008738
Cat.No: T40481
Synonym:
Target:
GSK3179106
Cat.No: T5491
Synonym:
Target: c-RET
Dicyclomine hydrochloride
Cat.No: T1460
Synonym:
Target: AChR
Propantheline bromide
Cat.No: T1006
Synonym: Neopepulsan,溴丙胺太林,Pro-Banthine,Neometantyl
Target: AChR
Tegaserod maleate
Cat.No: T1551
Synonym: HTF-919,马来酸替加色罗,SDZ-HTF-919
Target: 5-HT Receptor
BIBS-222
Cat.No: T26802
Synonym: BIBS 222
Target:
BIBS 39
Cat.No: T3178
Synonym:
Target: RAAS
Renzapride
Cat.No: T38507
Synonym: BRL 24924
Target: 5-HT Receptor
Tegaserod
Cat.No: T60680
Synonym:
Target: 5-HT Receptor
Linaclotide
Cat.No: T11852
Synonym:
Target: Guanylate cyclase
Trimebutine
Cat.No: T0918
Synonym: 曲美布汀,Mebutin
Target: Opioid Receptor
Cilansetron Hydrochloride
Cat.No: T30936
Synonym: KC-9946,KC9946,KC 9946
Target:
Alosetron
Cat.No: T21235
Synonym: Lotronex,GR68755,GR-68755,GR 68755,阿洛司琼
Target:
Tiropramide
Cat.No: T24887
Synonym: CR-605
Target:
SSR-241586
Cat.No: T13002
Synonym:
Target: Others
Asimadoline
Cat.No: T4633
Synonym: EMD-61753,阿西马朵林
Target: Opioid Receptor
MM 419447
Cat.No: T38482
Synonym:
Target:
RET-IN-17
Cat.No: T63877
Synonym:
Target:
(S)-Renzapride
Cat.No: T72809
Synonym: (S)-BRL 24924
Target:
Alosetron (Hydrochloride(1:X))
Cat.No: T64234
Synonym:
Target:
PSB 0777 ammonium hydrate
Cat.No: T78084
Synonym:
Target: Adenosine Receptor
Cat. No. Product Name Target Signaling Pathways
T68802 Vibsanin A

Vibsanin A,作为一种蛋白激酶C (PKC) 激活剂,展现出对人类癌细胞系的抗增殖活性,同时也兼具HSP90抑制剂的功能。
TN5231 Vibsanin C

Others Others
Vibsanin C是一种天然产物,属于忍冬科荚蒾属,其产品编号为 TN5231,CAS号为 74690-89-4。Vibsanin C可用作对照参考。
TN6791 Palvanil

Hexadecanamide

TRP/TRPV Channel Membrane transporter/Ion channel
Palvanil (Hexadecanamide) 是一种快速脱敏的 TRPV1 激动剂。它可能是治疗 IBS 的有前途的药物,因为它可以调节肠道蠕动并减轻内脏疼痛。

天然产物

Vibsanin A
Cat.No: T68802
Synonym:
Target:
Vibsanin C
Cat.No: TN5231
Synonym:
Target: Others
Palvanil
Cat.No: TN6791
Synonym: Hexadecanamide
Target: TRP/TRPV Channel
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