1. Immunology/Inflammation
  2. Salt-inducible Kinase (SIK)
  3. Phanginin A

Phanginin A 

Cat. No.: HY-N9539
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Phanginin A is a potent and orally active SIK1 (salt-induced kinase 1) activator. Phanginin A inhibited gluconeogenesis. Phanginin A increases the expression of p-SIK1 and decreases the expression of p-CREB. Phanginin A reduces blood glucose levels and improves glucose tolerance and dyslipidemia. Phanginin A has the potential for the research of type 2 diabetes.

For research use only. We do not sell to patients.

Phanginin A Chemical Structure

Phanginin A Chemical Structure

CAS No. : 1011528-58-7

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Description

Phanginin A is a potent and orally active SIK1 (salt-induced kinase 1) activator. Phanginin A inhibited gluconeogenesis. Phanginin A increases the expression of p-SIK1 and decreases the expression of p-CREB. Phanginin A reduces blood glucose levels and improves glucose tolerance and dyslipidemia. Phanginin A has the potential for the research of type 2 diabetes[1].

IC50 & Target[1]

SIK1

 

In Vitro

Phanginin A (2.5, 5, 10 µM) suppresses gluconeogenesis in primary mouse hepatocytes in a dose-dependent manner[1].
Phanginin A (5, 10 µM) reduces the mRNA expression of G6P and PEPCK, and decreases the intracellular cAMP accumulation[1].
Phanginin A (5, 10 µM; 0-120 min) inhibits the expression of CREB phosphorylation in a time and dose-dependent manner in primary mouse hepatocytes[1].
Phanginin A (2.5, 5, 10 µM; 0-120 min) increases the expression of p-SIK1 in a time and dose-dependent manner in primary mouse hepatocytes[1].
Phanginin A (5, 10 µM) increases PDE4 activity[1].

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

RT-PCR[1]

Cell Line: Primary mouse hepatocytes
Concentration: 5, 10 µM
Incubation Time:
Result: Significantly decreased PEPCK mRNA expression by 25% and 43% under basal conditions and 45% and 67% under forskolin-stimulated conditions, The G6P mRNA expression was also significantly reduced, with 5 and 10 μM of phanginin A resulting in a decrease of 30% and 46% under basal conditions and 38% and 57% under forskolin-stimulated conditions, respectively.

Western Blot Analysis[1]

Cell Line: Primary mouse hepatocytes
Concentration: 0-120 min
Incubation Time:
Result: Inhibited CREB phosphorylation in a time and dose-dependent manner.
In Vivo

Phanginin A (100 mg/kg; p.o.; once) shows anti-gluconeogenesis activity in type 2 diabetic ob/ob mice[1].
Phanginin A (100 mg/kg; p.o.; once daily for 26 days) improves metabolic disorders in ob/ob mice[1].

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

Animal Model: Type 2 diabetic ob/ob mice[1]
Dosage: 100 mg/kg
Administration: P.o.; once
Result: Significantly reduced the blood glucose, increased the phosphorylation of SIK1 in the liver by 119%, PDE4 activity in the liver was elevated by 74%, decreased in the cAMP concentration along with a 46% decrease in the CREB phosphorylation level in the liver, decreased the mRNA levels of PEPCK and G6P.
Animal Model: Male ob/ob mice[1]
Dosage: 100 mg/kg
Administration: P.o.; once daily for 26 days
Result: Showed an average reduction rate of 29% and 32% in random and fast blood glucose, exhibited a marked improvement in glucose tolerance, significantly reduced by 20% in HbA1c level, showed no effect on food intake and body weight.
Molecular Weight

360.44

Formula

C21H28O5

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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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Phanginin A
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HY-N9539
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