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TGR5 Receptor Agonist
TGR5受体激动剂 /TGR5 Receptor Agonist
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货号：A672110
同义名：
CCDC;TGR5
TGR5 receptor agonist, a potent TGR5 (GPCR19) agonist, showed improved potency in the U2-OS cell assay (pEC50 = 6.8) and in melanophore cells (pEC50 = 7.5).
TGR5 Receptor Agonist 化学结构
TGR5 Receptor Agonist 3D分子结构
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TGR5 Receptor Agonist 纯度/质量文件 产品仅供科研
货号：A672110
标准纯度：
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产品说明书
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TGR5 Receptor Agonist 质控信息
CDC25B-IN-2
✔
Akt
99%+
Clevidipine
✔
97%
Verapamil HCl
✔
99%
Amlodipine
✔
99%
Amlodipine maleate
✔
98%
(+)-cis-Diltiazem HCl
✔
95%
Zegocractin
++
Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM
99%+
Tanshinone IIA sulfonate sodium
✔
98%
Ulixacaltamide
++
hCaV3.1, IC50: 50 nM
hCaV3.2, IC50: 110 nM
99%+
Dronedarone Hydrochloride
✔
95%
Nitrendipine
+
Calcium channel, IC50: 95 nM
98%
Efonidipine HCl monoethanolate
✔
98%
Cinnarizine
✔
98%
SEA0400
++
ROS,p38 MAPK,ERK
99%+
Fasudil HCl
✔
Rho,PKA
98%
ML-9
✔
MLCK,Akt
99%+
Flunarizine 2HCl
+
Calcium channel, Ki: 68 nM
95%
Lomerizine 2HCl
✔
98%
Efonidipine
✔
98%
Levamlodipine
✔
97%
Nisoldipine
++
L-type Cav1.2, IC50: 10 nM
97%
Isradipine
✔
98%
Lacidipine
✔
98%
Lercanidipine
✔
98%
Loureirin B
✔
Potassium Channel
99%+
Tetracaine HCl
✔
98%
Manidipine
+++
Calcium channel, IC50: 2.6 nM
98%
Manidipine Dihydrochlorid
+++
Calcium channel, IC50: 2.6 nM
98%
Nicardipine
✔
98%
Wilforgine
✔
98+%
Econazole
✔
99%+
Ginsenoside Rd
✔
NF-κB
98%
Fendiline HCl
✔
98+%
Mesaconitine
✔
98%
Tetrandrine
✔
95%
Nifedipine
✔
95%
Nilvadipine
++++
Calcium channel, IC50: 0.03 nM
98%
Barnidipine
++++
[3 H]nitrendipine, Ki: 0.21 nM
95+%
Azelnidipine
✔
97%
Levetiracetam
✔
98%
Nimodipine
✔
95%
Benidipine HCl
✔
98%
Pinaverium bromide
✔
98%
Pranidipine
✔
98%
NP118809
+
N-type Ca2+ channel, IC50: 0.11 μM
L-type calcium channel, IC50: 12.2 μM
98%
Amlodipine Besylate
+++
Calcium channel, IC50: 1.9 nM
97%
Cilnidipine
✔
98%
Cinepazide Maleate
✔
98%
Terfenadine
✔
98%
YM-58483
✔
99%+
Ranolazine
✔
98%
Praeruptorin A
✔
p38 MAPK,Akt
98%
Ranolazine 2HCl
✔
98%
Felodipine
++++
L-type calcium channel, IC50: 0.15 nM
98%
PD173212
+++
N-type Ca2+ channel, IC50: 36 nM
98%
Levamlodipine besylate
✔
97%
Carboxyamidotriazole Orotate
✔
98%
IGS-1.76
✔
98+%
WH-4-023
++++
++++
99%+
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
TGR5 Receptor Agonist 生物活性
描述
TGR5 Receptor Agonist (CCDC), a robust agonist of Takeda G protein-coupled receptor 5 (TGR5; GPCR19), demonstrates enhanced effectiveness in U2-OS and melanophore cells with pEC50s of 6.8 and 7.5, respectively. This agonist triggers peripheral and central sensitivity to bladder distension in mice and elevates intracellular Ca2+ levels. It also reduces food consumption and heightens insulin sensitivity in diet-induced obese mice. The TGR5 Receptor Agonist is applicable in studies on diabetes, bladder hypersensitivity, and obesity control[1] [2] [3] [4]
体内研究
TGR5 Receptor Agonist (CCDC) directly activates a subset of bladder-associated dorsal root ganglia (DRG) neurons and a small number of non-neuronal cells in Trpv1-/- mice[2]
TGR5 Receptor Agonist (CCDC), administered at doses of 2 or 5 μg intracerebroventricularly (ICV), diminishes food intake and body weight in diet-induced obese mice[3]
TGR5 Receptor Agonist 临床研究
NCT号
适应症或疾病
临床期
招募状态
预计完成时间
地点
NCT01674946
Echolocation
Phase 1
Completed
-
Switzerland
... 展开 >> University Hospital Basel, Phase 1 Research Unit
Basel, Switzerland, 4031 收起 <<
TGR5 Receptor Agonist 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.77mL
0.55mL
0.28mL
13.84mL
2.77mL
1.38mL
27.68mL
5.54mL
2.77mL
TGR5 Receptor Agonist 技术信息
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