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- 文献和实验
- 技术资料
- 保存条件：
Powder: -20°C, 3 years; 4°C, 2 years.In solvent: -80°C, 6 months; -20°C, 1 month.
- 库存：
货期：1-2天
- 供应商：
MedChemExpress LLC
- CAS号：
1628741-91-2
- 规格：
10 mM * 1 mL/1 mg/5 mg/10 mg
| 规格： | 10 mM * 1 mL | 产品价格： | ￥3939.0 |
|---|---|---|---|
| 规格： | 1 mg | 产品价格： | ￥1590.0 |
| 规格： | 5 mg | 产品价格： | ￥3500.0 |
| 规格： | 10 mg | 产品价格： | ￥5500.0 |
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SSTR5 antagonist 1
CAS No. : 1628741-91-2
MCE 国际站：SSTR5 antagonist 1
产品活性：SSTR5 antagonist 1 (compound 25a) 是一种选择性，口服有效的生长抑素受体亚型 5 (SSTR5) 拮抗剂，对 hSSTR5 和 mSSTR5 的 IC50 分别为 9.6 和 57 nM。
研究领域：GPCR/G Protein | Neuronal Signaling
作用靶点：Somatostatin Receptor
In Vitro: SSTR5 antagonist 1 (compound 25a) (30 μM) inhibits hERG activity by 5.6%.
SSTR5 antagonist 1 (10 μM) shows highly selective inhibitory effect on SSTR5 over SSTR1-4, with inhibition rates of 11%, 8%, 14%, 10%.
SSTR5 antagonist 1 (1 μM; 15 min and 30 min) exhibits good metabolic stability toward both human and mouse microsomes with in vitro CLint value of <10 μL/min/kg (HLM) and 19 μL/min/kg (MLM), respectively.
In Vivo: SSTR5 antagonist 1 (compound 25a) (1 mg/kg; p.o.; single dose) is orally available with acceptable plasma exposure in mice in pharmacokinetic screening and exhibits excellent solubility (260 μg/mL, pH=6.8).
SSTR5 antagonist 1 (100 mg/kg; p.o.; single dose; measured at 0-120 min) augments insulin secretion in a glucose-dependent manner and lowers blood glucose concentration in high-fat diet fed C57BL/6J mice.
SSTR5 antagonist 1 (1, 3, 10, and 30 mg/kg; p.o.; single dose) shows dose-dependent effect on glucose excursion measured during the oral glucose tolerance test in HFD fed C57BL/6J mice.
Pharmacokinetic profiles in male ICR mouse (8-week-old)
| Route | Dose (mg/kg) | CLtotal (mL/h/kg) | Vss (mL/kg) | MRT (h) | |
| iv | 0.1 | 1761 | 3052 | 1.7 | / |
| Route | Dose (mg/kg) | Cmax (ng/mL) | Tmax
|
AUC0-8 h
|
F (%) |
| po | 1 | 74.8 | 2.0 | 332 | 58 |
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文献和实验Characterization of 5‐HT1A,B and 5‐HT2A,C Serotonin Receptor Binding
, which for this experiment were 249 fmol/mg protein, 0.56 nM, and 0.91, respectively. The dashed line without data points represents specific binding calculated using the values of parameters Bmax , KD , and slope factor.
Saturation Assays of Radioligand Binding to Receptors and Their Allosteric Modulatory Sites
. The binding of ligands (e.g., the agonist muscimol and antagonist bicuculline) to the GABA receptor requires both α and β subunits. Similarly, both α and γ subunits are required for optimal binding of the agonist diazepam and the antagonist flumazenil
Practical Aspects of Radioligand Binding
Figure 1.3.3 Competition between a radiolabeled antagonist and an unlabeled agonist for muscarinic receptors on N1E‐115 cells. [3 H]Quinuclidinyl benzilate ([3 H]QNB; 0.2 nM) was incubated with 200,000 intact cells/tube and various concentrations
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