1. GPCR/G Protein
  2. GLP Receptor
  3. GZR18

GZR18 是胰高血糖素样肽-1 (GLP-1) 的类似物,对 GLP-1 受体具有激动活性,EC50 为 0.677 nM。GZR18 可以减轻 2 型糖尿病。

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Custom Peptide Synthesis

GZR18 Chemical Structure

GZR18 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GZR18 is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes[1].

IC50 & Target

EC50: 0.677 nM (GLP-1 Receptor)

体外研究
(In Vitro)

GZR18 (30-90 nM,0.5-1 h) 剂量依赖性地刺激小鼠胰岛 β 细胞的葡萄糖依赖性胰岛素分泌[1]

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

体内研究
(In Vivo)

GZR18 (0-100 nmol/kg,皮下注射,单剂量或 11 次注射) 在 db/db 小鼠糖尿病模型中降低小鼠的血糖水平,减轻小鼠体重,具有控制血糖的作用[1]
GZR18 (60 μg/kg,静脉注射或皮下注射,单剂量) 在食蟹猴模型中展现出良好的药代动力学特性[1]

GZR18 在食蟹猴模型中的药代动力学特征[1]

route Dose (μg/kg) T1/2 (h) Tmax (h) Cmax (ng/mL) AUC0-t (ng·h/mL)) AUC0-inf (ng·h/mL) MRT (h) Vd/F (kg/mL) CL/F (h/g·mL) F (%)
s.c. 60 61.3 14 527 51800 55700 75.2 96.6 1.1 73.3
i.v. 60 61.6 0.167 1640 70700 74800 59.2 59.4 0.803 -

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

Animal Model: Type 2 diabete in db/db mice[1]
Dosage: 0-100 nmol/kg
Administration: s.c., single dose or once every 3 days for 33 days
Result: Lowered blood glucose levels, suppressed food and water intake and improved glucose homeostasis.
分子量

4141.63

Formula

C189H295N45O59

Sequence

His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys(AEEA-AEEA-gammaGlu-C22 diacid)-Glu-Phe-Ile-Ala-Trp-Leu-Val-Arg-Gly-Arg-Gly

Sequence Shortening

HGEGTFTSDVSSYLEGQAA-K(AEEA-AEEA-gammaGlu-C22 diacid)-EFIAWLVRGRG

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
  • 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.

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Inquiry Information

产品名称:
GZR18
目录号:
HY-P10269
需求量: