2. GPCR/G Protein Neuronal Signaling
  3. GPR119
  4. YH18968

YH18968 是一种口服有效的 GPR119 激活剂，其诱导 cAMP 积累的 EC50 为 2.8 nM。YH18968 可激活 GPR119，升高细胞内环磷酸腺苷水平，刺激肠道 L 细胞分泌胰高血糖素样肽-1，并触发胰腺 β 细胞分泌葡萄糖依赖性胰岛素。YH18968 可改善正常小鼠和饮食诱导肥胖小鼠的葡萄糖耐量。YH18968 可用于 2 型糖尿病的研究。

MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

YH18968

YH18968 Chemical Structure

CAS No. : 1632498-56-6

1.  客户无需承担相应的运输费用。

2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 是否有货
50 mg   询价  
100 mg   询价  
250 mg   询价  

* Please select Quantity before adding items.

Customer Review

YH18968 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

YH18968 is an orally active GPR119 agonist with an EC50 of 2.8 nM for inducing cAMP accumulation. YH18968 activates GPR119, elevates intracellular cyclic adenosine monophosphate levels, stimulates glucagon-like peptide-1 secretion from intestinal L cells, and triggers glucose-dependent insulin secretion from pancreatic β cells. YH18968 improves glucose tolerance in normal mice and diet-induced obese mice. YH18968 can be used for the research of type 2 diabetes[1].

体外研究
(In Vitro)

YH18968 (0.03-1000 nM; 60 min) 可以剂量依赖的方式刺激 HIT-T15 细胞分泌胰岛素，其 EC50 为 3.5 nM[1]。
YH18968 (0.03-1000 nM; 120 min) 可以剂量依赖的方式刺激 GLUTag 细胞分泌 GLP-1，其 EC50 为 0.1 nM[1]。
YH18968 (0.1-100 μM; 48 h) 在 HIT-T15、GLUTag 和 HepG2 细胞中的细胞毒性极低，三种细胞系中的 LC50 均大于 100 μM[1]。

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

YH18968 相关抗体:

ELISA Assay[1]

Cell Line: HIT-T15 hamster insulinoma cells
Concentration: 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1,000 nM nM (15 mM glucose condition); 100 nM (0, 3, or 15 mM glucose conditions)
Incubation Time: 60 min
Result: Elicited dose-dependent increases in insulin release with an EC50 of 3.5 nM.
Enhanced insulin release in a glucose-dependent manner at 100 nM, with a significant increase observed at 15 mM glucose (2.19-fold vs control) and no effect in the absence of glucose.

ELISA Assay[1]

Cell Line: GLUTag murine intestinal L cells
Concentration: 0.03, 0.1, 0.3, 1, 3, 10, 30, 100, 300, and 1,000 nM
Incubation Time: 120 min
Result: Enhanced GLP-1 secretion in a dose-dependent manner with an EC50 of 0.1 nM.
药代动力学
(Parmacokinetics)
Species Dose Route AUClast AUC0-inf CL Vss MRT Cmax Tmax T1/2 F
Mice[1] 1 mg/kg i.v. 1375.1 ng·h/mL 1619.9 ng·h/mL 617.3 mL/h/kg 2112.2 mL/kg 3.4 h / / / /
Mice[1] 1 mg/kg p.o. 549.7 ng·h/mL 719.8 ng·h/mL / / / 168.6 ng/mL 0.5 h 3.1 h 40.0 %
Mice[1] 10 mg/kg p.o. 2471.7 ng·h/mL 2958.2 ng·h/mL / / / 759.7 ng/mL 0.5 h 2.6 h 18.0 %
Mice[1] 100 mg/kg p.o. 6538.0 ng·h/mL 15773.9 ng·h/mL / / / 1472.2 ng/mL 0.5 h 9.2 h 4.8 %
体内研究
(In Vivo)

YH18968 (0.1-10 mg/kg；口服；单次给药) 可呈剂量依赖性改善正常 C57BL/6J 小鼠的葡萄糖耐量[1]。
YH18968 (0.1-10 mg/kg；口服；单次给药) 可显著改善 DIO 小鼠的葡萄糖耐量，其药效在 1 mg/kg 时达到饱和[1]。
YH18968 (1 mg/kg；口服；每日 1 次；连续 28 天) 维持 DIO 小鼠的葡萄糖耐量改善，且无快速减敏现象，与 Linagliptin (HY-10284) 联合使用时具有叠加效应[1]。

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

Animal Model: C57BL/6J (8-week-old, male)[1]
Dosage: 0.1 mg/kg; 1 mg/kg; 10 mg/kg; 10 mg/kg + 1 mg/kg linagliptin
Administration: p.o.; single dose
Result: Significantly lowered the 2-hour area under the curve (AUC) for blood glucose in a dose-dependent manner compared to vehicle control.
Produced a significant additive glucose-lowering effect when co-administered with 1 mg/kg linagliptin.
Increased active plasma GLP-1 levels by 2.7-fold compared to vehicle control at 30 minutes post-administration at 10 mg/kg dose.
Co-administration with linagliptin significantly increased active GLP-1 levels compared to either agent alone.
Animal Model: diet-induced obese (DIO) (17-week-old, male, Type 2 diabetes model)[1]
Dosage: 0.1 mg/kg; 1 mg/kg; 10 mg/kg
Administration: p.o.; single dose
Result: Significantly lowered the 2-hour AUC for blood glucose compared to vehicle control at 1 and 10 mg/kg doses, with a dose-dependent effect observed.
Produced similar levels of glucose lowering at 1 and 10 mg/kg doses, indicating a saturated effect.
Animal Model: diet-induced obese (DIO) (17-week-old, male, Type 2 diabetes model)[1]
Dosage: 1 mg/kg; 1 mg/kg + 1 mg/kg linagliptin
Administration: p.o.; once daily; 28 days
Result: Significantly lowered the 2-hour AUC for blood glucose compared to vehicle control on day 1, with a more potent effect than 10 mg/kg MBX2982 (HY-15291).
Produced an additive glucose-lowering effect when co-administered with 1 mg/kg linagliptin compared to either agent alone on day 1.
Continued to effectively lower the 2-hour AUC for blood glucose on day 29, maintaining glucose tolerance improvement equivalent to day 1 efficacy when used alone or in combination with Linagliptin.
分子量

545.58

Formula

C27H28FN9O3
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

YH18968 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:

YH189681632498-56-6YH 18968YH-18968GPR119G Protein-Coupled Receptor 119pancreatic beta cellsintestinal L cellsdipeptidyl peptidase 4 inhibitorglucagon-like peptide-1type 2 diabetes mellitusCHO-K1 cellsnormal micediet-induced obese miceintracellular cyclic adenosine monophosphateInhibitorinhibitorinhibit

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称：

  

* 需求量：

* 客户姓名：

 

* Email：

* 电话：

 

* 公司或机构名称：

   留言给我们：

Bulk Inquiry

Inquiry Information

产品名称：
YH18968
目录号：
HY-125646
需求量：

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

   产品名称：

  

* Lot #：

* 客户姓名：

 

* Email：

   电话：

 

* 部门：

* 公司或机构名称：

 

   留言给我们：

Request for HNMR Report

We have received your request and will respond to you as soon as possible.

嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z