1. GPCR/G Protein Neuronal Signaling
  2. Somatostatin Receptor
  3. SSTR3 agonist-1 TFA

SSTR3 agonist-1 TFA 是一种强效、口服有效且选择性的 SSTR3 受体激动剂 (EC50 =0.14 nM)。SSTR3 agonist-1 TFA 与 SSTR3 受体结合,抑制 cAMP 活性。SSTR3 agonist-1 TFA 在常染色体显性多囊肾病 (ADPKD) 小鼠模型中降低肾脏重量和肾囊肿指数 (KCI)。SSTR3 agonist-1 TFA 可用于 ADPKD 的相关研究。

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SSTR3 agonist-1 TFA

SSTR3 agonist-1 TFA Chemical Structure

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  • 生物活性

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生物活性

SSTR3 agonist-1 TFA is a potent, orally active, and selective SSTR3 agnoist (EC50 =0.14 nM). SSTR3 agonist-1 TFA binds to SSTR3 receptor to inhibit cAMP activity. SSTR3 agonist-1 TFA decreases kidney weight and kidney cystic index (KCI) in a mouse model of autosomal dominant polycystic kidney disease (ADPKD). SSTR3 agonist-1 TFA can be used for ADPKD research[1].

IC50 & Target[1]

SSTR3

0.14 nM (EC50)

体外研究
(In Vitro)

SSTR3 agonist-1 (compound 38) (20 分钟) TFA 在稳定表达人源 SSTR3 的 CHO-K1 细胞中抑制 Forskolin (HY-15371) 刺激的 cAMP 积累,EC50 为 0.14 nM[1]

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

体内研究
(In Vivo)

SSTR3 agonist-1 (compound 38) (30 和 60 mg/kg,口服,从出生后第 12 天到第 20 天,每天一次,持续 9 天) TFA 可剂量依赖性地降低 ADPKD 小鼠模型中的肾脏囊肿指数 (KCI) 和肾脏大小[1]

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

Animal Model: Pax8 Tet-O-Cre/Pkd1 flox mice treated with Doxycycline (HY-N0565) hyclate (50 mg/kg) to induce ADPKD[1]
Dosage: 30 and 60 mg/kg
Administration: p.o., daily for 9 days from (PND) 12 to 20
Result: Decreased KCI with a 10.7% suppression compared to the vehicle at 30 mg/kg.
Decreased KCI with a 25.2% suppression compared to the vehicle at 60 mg/kg.
Dose dependently decreased the left kidney weight/body weight (LKW/BW) ratio.
分子量

733.67

Formula

C33H38F7N5O6

性状

固体

颜色

Yellow to brown

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

纯度 & 产品资料
参考文献
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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.

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产品名称:
SSTR3 agonist-1 TFA
目录号:
HY-177493A
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