计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
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概述
SSTR5 antagonist 1 (compound 25a) is a selective and orally available somatostatin receptor subtype 5 ( SSTR5 ) antagonist with IC 50 s of 9.6 and 57 nM for hSSTR5 and mSSTR5 , respectively
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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) CL total (mL/h/kg) V ss (mL/kg) MRT (h) iv 0.1 1761 3052 1.7 / Route Dose (mg/kg) C max (ng/mL) T max (h) AUC 0-8 h (ng·h/mL) F (%) po 1 74.8 2.0 332 58 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: High-fat diet fed C57BL/6J mice Dosage: 100 mg/kg Administration: Oral gavage; single dose; monitored over 2 h Result: Showed the maximum efficacy superior to that of 10 mg/kg Glibenclamide and comparable to that of 30 mg/kg Alogliptin . Augmented insulin secretion in a glucose-dependent manner and displayed a blood glucose-lowering effect, indicating its anti-diabetic efficacy in vivo.
IC50& Target:IC50: 9.6 nM (hSSTR5), 57 nM (mSSTR5)
规格
别名
SSTR5 拮抗剂 1
规格或纯度
10mM in DMSO
英文名称
SSTR5 antagonist 1
生化机理
SSTR5 拮抗剂 1（化合物 25a）是一种选择性口服体生长抑素受体亚型 5（SSTR5）拮抗剂，对 hSSTR5 和 mSSTR5 的 IC 50 s 分别为 9.6 和 57 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
CCOC1=CC(=CC(=C1C2=CC=C(C=C2)F)OCC)CN3CC4(C3)CC(=NO4)N5CCC(CC5)C(=O)O
PubChem CID
分子量
511.59
高级数据
关联靶点（人）
SSTR5
Tclin
生长抑素受体 5 型(Somatostatin receptor type 5)
(2 活性数据)
质检证书(CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
溶液计算器
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