2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. GPR119 Dipeptidyl Peptidase
  4. HBK001

HBK001 是一种具有口服活性和选择性的双重 GPR119 激动剂与 DPP-IV 抑制剂。HBK001 可触发 cAMP 生成、PKA 激活、CREB 磷酸化、葡萄糖刺激的胰岛素分泌、肠促胰岛素血浆水平升高、β 细胞增殖及 β 细胞功能基因上调。HBK001 还可降低血糖、改善高血糖状态、提升葡萄糖耐量并改善胰岛形态。HBK001 可用于 2 型糖尿病的相关研究。

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HBK001

HBK001 Chemical Structure

CAS No. : 1942922-78-2

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HBK001 相关抗体

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

HBK001 is an orally active and selective dual GPR119 agonist and DPP-IV inhibitor. HBK001 triggers cAMP production, PKA activation, CREB phosphorylation, glucose-stimulated insulin secretion, plasma incretin elevation, β-cell proliferation, and β-cell function gene up-regulation. HBK001 reduces blood glucose, ameliorates hyperglycemia, improves glucose tolerance, and enhances islet morphology. HBK001 can be used for the research of type 2 diabetes mellitus[1][2].

IC50 & Target[1]

DPP-4

40 nM (IC50)

体外研究
(In Vitro)

HBK001 可强效抑制 DPP-IV，其 IC50 为 0.04 μM[1]。
HBK001 (10 μM) 对 DPP-8/9 无抑制活性，表现出对 DPP-IV 的高选择性[1]。
HBK001 在 HEK293 细胞中作为 GPR119 激动剂，其 EC50 为 1.40 μM，在 1 μM 浓度下的相对活性为 58%[1]。
HBK001 (30 分钟) 在小鼠和大鼠肝细胞中稳定性较低，但在人肝细胞中稳定性良好，孵育 30 分钟后底物剩余率为 101.2%[1]。
HBK001 (48 小时) 对 Vero 细胞表现出低细胞毒性，其 IC50 为 46.6 μg/mL[1]。
HBK001 (3.28 nM-10 μM；24 小时) 在转染的 HEK293 细胞中激活 GPR119，其 EC50 为 0.03 μM[2]。
HBK001 (10 μM；24 小时) 在转染的 HEK293 细胞中，10 μM 浓度下不会激活 GPR40、GLP1R 或 GIPR，表明其对 GPR119 的激活相较于相关 GPCR 具有选择性[2]。
HBK001 (1-10 μM) 在 16.7 mM 葡萄糖条件下，以浓度依赖的方式增强 ICR 小鼠原代胰岛的葡萄糖刺激胰岛素分泌[2]。
HBK001 (10 μM) 可增强健康供者来源的人原代胰岛在葡萄糖刺激下的胰岛素分泌[2]。
HBK001 (0.1-10 μM) 可在体外以浓度依赖的方式促进 NIT-1 小鼠胰腺 β 细胞的细胞内 cAMP 生成[2]。
HBK001 (10 μM) 可在转染 GPR119 的 HEK293 细胞中激活小鼠 Ins1 和 Ins2 基因启动子的反式激活[2]。
HBK001 (10 μM；24 小时) 可上调 ICR 小鼠原代胰岛中 β 细胞功能相关基因 (Nkx6.1、Nkx2.2、Ins1、Ins2) 的表达[2]。
HBK001 (10 μM) 可通过腺苷酸环化酶依赖通路，增强 KKAy 小鼠原代胰岛的葡萄糖刺激胰岛素分泌[2]。

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

HBK001 相关抗体:

Real Time qPCR[2]

Cell Line: ICR mouse primary islets
Concentration: 10 μM
Incubation Time: 24 h
Result: Upregulated expression of β-cell function-related genes (Nkx6.1, Nkx2.2, Ins1, Ins2)
药代动力学
(Parmacokinetics)
Species Dose Route T1/2 Cmax AUC0-t AUC0-∞ MRT0-∞ Tmax F
Mice[1] 20 mg/kg p.o. 1.06 h 213 ng/mL 308 ng·h/mL 318 ng·h/mL 1.22 h 0.42 h 12.2 %
Mice[1] 2 mg/kg i.v. 1.64 h 850 ng/mL 257 ng·h/mL 261 ng·h/mL 0.76 h / /
Rat[1] 30 mg/kg p.o. 1.11 h 192 ng/mL 468 ng·h/mL 502 ng·h/mL 2.11 h 1.17 h 31.8 %
体内研究
(In Vivo)

HBK001 (30 mg/kg；口服；单次给药) 在正常血糖 ICR 小鼠中表现出体内降糖活性，给药方式为单次口服 30 mg/kg[1]。
HBK001 (5-30 mg/kg；口服；单次给药) 可选择性抑制血清 DPP4 活性，增加葡萄糖刺激的肠促胰岛素释放，并降低正常血糖 ICR 小鼠的血糖波动，在 30 mg/kg 时降糖效果进入平台期[2]。
HBK001 (30 mg/kg；口服；每日一次；持续 6 周) 可通过 GPR119 依赖的信号通路改善自发性糖尿病 KKAy 小鼠的高血糖症状、提升葡萄糖耐量、增强胰岛素分泌、恢复胰岛形态，并上调 β 细胞功能相关基因，尽管其仅能抑制约 50%的血清 DPP4 活性[2]。
HBK001 (30 mg/kg；口服；每日一次；持续 5 周) 可改善自发性糖尿病 db/db 小鼠的高血糖症状并提升其葡萄糖耐量[2]。

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

Animal Model: ICR mice (male, 26-27 g)[1]
Dosage: 30 mg/kg
Administration: p.o.; single dose
Result: Reduced blood glucose levels after oral glucose loading.
Showed higher area under the oral glucose tolerance test curve (AUCOGTT) than HBK001 hydrochloride (22) group at equivalent molar dose.
Animal Model: ICR mice (male)[2]
Dosage: 5 mg/kg; 10 mg/kg; 20 mg/kg; 30 mg/kg
Administration: p.o.; single dose
Result: Achieved approximately 50% serum DPP4 inhibition compared to baseline for about 4 hours at 30 mg/kg.
Increased glucose-induced total GLP-1 levels by 41.0% and glucose-induced GIP levels by 40.2% compared to vehicle at 30 mg/kg.
Significantly reduced blood glucose levels 30 minutes after oral glucose loading at doses of 5, 10, 20, and 30 mg/kg, with the area under the curve (AUC) decreased by 17.1%, 21.8%, 24.2%, and 22.8%, respectively, compared to vehicle.
Animal Model: KKAy mice (female, spontaneous diabetic, fasting blood glucose >180 mg/dl)[2]
Dosage: 30 mg/kg
Administration: p.o.; daily; 6 weeks
Result: Significantly decreased fasting blood glucose levels over 6 weeks.
Reduced OGTT AUC by 26.5% compared to vehicle.
Inhibited ~50% of serum DPP4 activity.
Increased first-phase insulin secretion by 4.7-fold compared to vehicle.
Increased glucose infusion rate (GIR) during hyperglycemic clamp.
Increased β-cell area percentage by 17.9% compared to vehicle.
Increased pancreatic CREB phosphorylation.
Up-regulated β-cell function-related genes including NeuroD, Nkx6.1, Nkx2.2, MafA, Ins1, and Ins2 compared to vehicle.
Animal Model: db/db (BKS.Cg-m+/+ Leprdb/J) mice (female, spontaneous diabetic, fasting blood glucose >180 mg/dl)[2]
Dosage: 30 mg/kg
Administration: p.o.; daily; 5 weeks
Result: Significantly decreased fasting blood glucose levels over 5 weeks.
Reduced OGTT AUC by 13.0% compared to vehicle, with effects comparable to linagliptin.
分子量

586.69

Formula

C30H38N10O3
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

HBK001 相关分类

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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:

HBK0011942922-78-2HBK 001HBK-001GPR119Dipeptidyl PeptidaseG Protein-Coupled Receptor 119DPPhERGGPR40GLP1RDPP8DPP-IVtype 2 diabetes mellitusGIPRhuman DPP-IVhuman GPR119Inhibitorinhibitorinhibit

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