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TGR5 Receptor Agonist {[allProObj[0].p_purity_real_show]}

货号:A672110 同义名: CCDC; TGR5

TGR5 Receptor Agonist是一种强效的 TGR5 (GPCR19) 激动剂,在 U2-OS 细胞和黑色素细胞中显示出改进的效力(pEC50 分别为 6.8 和 7.5)。

TGR5 Receptor Agonist 化学结构 CAS号:1197300-24-5
TGR5 Receptor Agonist 化学结构
CAS号:1197300-24-5
TGR5 Receptor Agonist 3D分子结构
CAS号:1197300-24-5
TGR5 Receptor Agonist 化学结构 CAS号:1197300-24-5
TGR5 Receptor Agonist 3D分子结构 CAS号:1197300-24-5
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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: {[allProObj[0].p_purity_real_show]}
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产品名称 Ca2+ channel-like protein Calcium Channel Cav 2.2 其他靶点 纯度
CDC25B-IN-2 Akt 99%+
Clevidipine 97%
Verapamil HCl 99%
Amlodipine 99%
Amlodipine maleate 98%
(+)-cis-Diltiazem HCl 99%
Zegocractin ++

Orai1/STIM1-mediated Ca2+ currents, IC50: 120 nM

99%+
Tanshinone IIA sulfonate sodium 98%
Ulixacaltamide ++

hCaV3.2, IC50: 110 nM

hCaV3.1, IC50: 50 nM

99%+
Dronedarone HCl 95%
Nitrendipine +

Calcium channel, IC50: 95 nM

98%
Efonidipine HCl monoethanolate 98%
Cinnarizine 98%
SEA0400 ++

NCX, IC50: 33 nM

p38 MAPK,ROS,ERK 99%+
Fasudil HCl PKA,Rho 98%
ML-9 MLCK,Akt 99%+
Flunarizine 2HCl +

Calcium channel, Ki: 68 nM

95%
Lomerizine 2HCl 98%
Efonidipine 98%
Levamlodipine 98%
Nisoldipine ++

L-type Cav1.2, IC50: 10 nM

97%
Isradipine 98%
Lacidipine 98%
Lercanidipine 99%
Loureirin B Potassium Channel 99%+
Tetracaine HCl 98%
Manidipine +++

Calcium channel, IC50: 2.6 nM

99%
Manidipine Dihydrochlorid +++

Calcium channel, IC50: 2.6 nM

98%
Nicardipine 99%
Wilforgine 98+%
Econazole 99%+
Ginsenoside Rd NF-κB 98%
Fendiline HCl 98+%
Mesaconitine 98%
Tetrandrine 95%
Nifedipine 98%
Nilvadipine ++++

Calcium channel, IC50: 0.03 nM

95%
Barnidipine ++++

[3H]nitrendipine, Ki: 0.21 nM

95+%
Azelnidipine 97%
Levetiracetam 98%
Nimodipine 95%
Benidipine HCl 98%
Pinaverium bromide 98%
Pranidipine 99%
NP118809 +

L-type calcium channel, IC50: 12.2 μM

N-type Ca2+ channel, IC50: 0.11 μM

98%
Amlodipine Besylate +++

Calcium channel, IC50: 1.9 nM

97%
Cilnidipine 99%
Cinepazide Maleate 99% (HPLC)
Terfenadine 98%
YM-58483 99%+
Amiloride HCl 98%
Ranolazine 98%
Praeruptorin A Akt,p38 MAPK 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 ++++

Cav 2.2, IC50: 0.001 μM

++++

Cav 2.2, IC50: 0.001 μM

99%+
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
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

CAS号1197300-24-5
分子式C18H14Cl2N2O2
分子量 361.22
SMILES Code O=C(C1=C(C)ON=C1C2=CC=CC=C2Cl)N(C3=CC=C(Cl)C=C3)C
MDL No. MFCD17169972
别名 CCDC; TGR5; MDK00245
运输蓝冰
InChI Key IGRCWJPBLWGNPX-UHFFFAOYSA-N
Pubchem ID 44605616
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Sealed in dry, 2-8°C

溶解方案

DMSO: 50 mg/mL(138.42 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
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