2. GPCR/G Protein Neuronal Signaling
  3. Somatostatin Receptor G protein-coupled Bile Acid Receptor 1
  4. SSTR5/TGR5-modulator-1

SSTR5/TGR5-modulator-1 是一种口服有效的双靶点小分子，分别靶向激活胆汁酸受体 TGR5 和拮抗 生长抑素受体 SSTR5。SSTR5/TGR5-modulator-1 通过激活 TGR5 促进 cAMP 积累，又通过阻断 SSTR5 而抑制激动剂诱导的钙动员。SSTR5/TGR5-modulator-1 在改善小鼠葡萄糖耐量的同时，能在药理学相关剂量下缓解胆囊充盈，显示出良好的体内药效。SSTR5/TGR5-modulator-1 可用于 2 型糖尿病的相关研究。

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SSTR5/TGR5-modulator-1

SSTR5/TGR5-modulator-1 Chemical Structure

CAS No. : 3069267-46-2

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SSTR5/TGR5-modulator-1 相关抗体

Top Publications Citing Use of Products

查看 Somatostatin Receptor 亚型特异性产品:

查看所有亚型
SSTR1 SSTR2 SSTR3 SSTR5 SSTR4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

SSTR5/TGR5-modulator-1 is an orally active and dual-target small molecule, balanced in vitro activity at human TGR5 and human SSTR5. SSTR5/TGR5-modulator-1 activates human TGR5 to promote cAMP accumulation. SSTR5/TGR5-modulator-1 blocks human SSTR5 to inhibit agonist-induced calcium mobilization. SSTR5/TGR5-modulator-1 improves glucose tolerance in mice. SSTR5/TGR5-modulator-1 alleviates gallbladder filling in mice at pharmacologically relevant doses. SSTR5/TGR5-modulator-1 has suboptimal physicochemical and metabolic properties.SSTR5/TGR5-modulator-1 can be used for the research of type 2 diabetes mellitus[1].

IC50 & Target

SSTR5

4.37 nM (IC50)

体外研究
(In Vitro)

SSTR5/TGR5-modulator-1 (Compound 19) (cAMP 实验：30 min；钙实验预孵育：10 min) 可在体外强效激活人源 TGR5 (EC50=5.91 nM) 并拮抗人源 SSTR5 (IC50=4.37 nM)[1]。
SSTR5/TGR5-modulator-1 ((cAMP 实验：30 min)；(钙实验预孵育：10 min)) 表现出具有可比性的跨物种效能，可在体外激活小鼠 TGR5 (EC50=3.40-5.30 nM) 并拮抗小鼠 SSTR5 (IC50=2.97-19.6 nM)[1]。
SSTR5/TGR5-modulator-1 (1 μM; 60 min) 在体外表现出快速的代谢周转，在人肝微粒体中的 T1/2 为 2.2 min，在小鼠肝微粒体中的 T1/2 为 2.8 min[1]。
SSTR5/TGR5-modulator-1 (30-100 μM; 24 h) 对原代肝细胞无毒性，但在孵育 24 h 后，100 μM 浓度下会引发显著的细胞毒性[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

SSTR5/TGR5-modulator-1 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: primary hepatocytes
Concentration: 30 μM; 100 μM
Incubation Time: 24 h
Result: Induced significant cytotoxicity at 100 μM.
Showed no significant toxicity observed at 30 μM.
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 AUClast Clearance (CL) Vss_obs Tmax Cmax Bioavailability
Mice[1] 50 mg/kg p.o. 0.99 h 1646 ng·h/mL / / 0.25 h 1387 ng/mL 16 %
Mice[1] 2 mg/kg i.v. 1.16 h 417 ng·h/mL 81.8 mL/min/kg 3.61 L/kg / / /
体内研究
(In Vivo)

SSTR5/TGR5-modulator-1 (Compound 19) (10-100 mg/kg；口服；单次给药) 可使雄性 C57BL/6 小鼠的口服葡萄糖耐量呈剂量依赖性改善，其中 100 mg/kg 剂量的效果优于 50 mg/kg 的阳性对照[1]。
SSTR5/TGR5-modulator-1 (100 mg/kg；口服；单次给药) 相较于 TGR5 激动剂单药治疗对照组，可减弱雄性 C57BL/6 小鼠中 TGR5 介导的胆囊充盈[1]。
SSTR5/TGR5-modulator-1 (100 mg/kg；口服；单次给药) 可增强雄性 C57BL/6 小鼠的 GLP-1-胰岛素轴，为其降糖作用机制提供了支持[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 (8-week-old male, ~25 g)[1]
Dosage: 10 mg/kg; 30 mg/kg; 100 mg/kg
Administration: p.o.; single dose
Result: Demonstrated dose-dependent suppression of blood glucose levels.
Elicited a greater glucose-lowering effect at 100 mg/kg than positive control compound 2 at 50 mg/kg.
Significantly reduced the area under the plasma glucose curve (AUC0-90 min) at all tested doses compared to vehicle control.
Animal Model: C57BL/6 (8-week-old male)[1]
Dosage: 100 mg/kg
Administration: p.o.; single dose
Result: Reduced gallbladder size compared to both vehicle control subgroup without egg yolk stimulation and compound 2 (50 mg/kg)-treated group, indicating a weaker effect on gallbladder filling.
分子量

727.87

Formula

C39H45N5O7S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

SSTR5/TGR5-modulator-1 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SSTR5/TGR5-modulator-13069267-46-2Somatostatin ReceptorG protein-coupled Bile Acid Receptor 1SSTRsSSTRG-protein coupled receptor 19GPCR19TGR5GPBAR1primary hepatocytesmouse TGR5calcium mobilizationhuman liver microsomeshuman SSTR5type 2 diabetes mellituscAMPmicemouse SSTR5human TGR5Inhibitorinhibitorinhibit

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