| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| Targets |
SIK1
|
|---|---|
| ln Vitro |
Phanginin A deters gluconeogenesis in primary mouse hepatocytes in a dose-dependent manner at 2.5, 5, and 10 µM [1]. Phanginin A (5, 10 µM) decreases intracellular cAMP buildup and the mRNA expression of G6P and PEPCK [1]. In primary mouse hepatocytes, Phanginin A (5, 10 µM; 0-120 min) decreases the expression of CREB phosphorylation in a time- and dose-dependent way [1]. In primary murine hepatocytes, Phanginin A (2.5, 5, 10 µM; 0-120 min) enhances p-SIK1 expression in a dose- and time-dependent manner [1]. PDE4 activity is increased by phanginin A (5, 10 µM) [1].
|
| ln Vivo |
In type 2 diabetes ob/ob mice, phanginin A (100 mg/kg; po; once) shows antigluconone action[1]. For 26 days, ob/ob mice treated with phanginin A (100 mg/kg; po; once daily) show improvements in metabolic abnormalities[1].
|
| Cell Assay |
RT-PCR[1]
Cell Types: Primary mouse hepatocytes Tested Concentrations: 5, 10 µM Incubation Duration: Experimental Results: Dramatically diminished PEPCK mRNA expression by 25% and 43% under basal conditions and 45% and 67% under forskolin-stimulated conditions, The G6P mRNA expression was also Dramatically decreased, 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 Types: Primary mouse hepatocytes Tested Concentrations: 0-120 min Incubation Duration: Experimental Results: Inhibited CREB phosphorylation in a time and dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: Type 2 diabetic ob/ob mice[1]
Doses: 100 mg/kg Route of Administration: Po; once Experimental Results: Dramatically decreased the blood glucose, increased the phosphorylation of SIK1 in the liver by 119%, PDE4 activity in the liver was elevated by 74%, diminished in the cAMP concentration along with a 46% decrease in the CREB phosphorylation level in the liver, diminished the mRNA levels of PEPCK and G6P. Animal/Disease Models: Male ob/ob mice[1] Doses: 100 mg/ kg Route of Administration: Po; one time/day for 26 days Experimental Results: demonstrated an average reduction rate of 29% and 32% in random and fast blood glucose, demonstrated a marked improvement in glucose tolerance, Dramatically decreased by 20% in HbA1c level, demonstrated no effect on food intake and body weight. |
| References |
[1]. Liu S, et al. Activation of SIK1 by phanginin A inhibits hepatic gluconeogenesis by increasing PDE4 activity and suppressing the cAMP signaling pathway. Mol Metab. 2020 Nov;41:101045.
|
| Additional Infomation |
methyl (1S,2S,9R,10S,13R,14R,17R)-17-hydroxy-9-methyl-5,16-dioxapentacyclo[12.3.3.01,13.02,10.04,8]icosa-4(8),6-diene-14-carboxylate has been reported in Biancaea sappan with data available.
|
| Molecular Formula |
C21H28O5
|
|---|---|
| Molecular Weight |
360.444026947021
|
| Exact Mass |
360.193
|
| CAS # |
1011528-58-7
|
| PubChem CID |
24854205
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
3.2
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
26
|
| Complexity |
593
|
| Defined Atom Stereocenter Count |
7
|
| SMILES |
C[C@@H]1[C@@H]2CC[C@H]3[C@@]4(CCC[C@@]3([C@H]2CC5=C1C=CO5)[C@@H](OC4)O)C(=O)OC
|
| InChi Key |
FBOCRPKLWNKMFW-YCBSRJOKSA-N
|
| InChi Code |
InChI=1S/C21H28O5/c1-12-13-4-5-17-20(18(22)24-2)7-3-8-21(17,19(23)26-11-20)15(13)10-16-14(12)6-9-25-16/h6,9,12-13,15,17,19,23H,3-5,7-8,10-11H2,1-2H3/t12-,13+,15+,17+,19-,20+,21+/m1/s1
|
| Chemical Name |
methyl (1S,2S,9R,10S,13R,14R,17R)-17-hydroxy-9-methyl-5,16-dioxapentacyclo[12.3.3.01,13.02,10.04,8]icosa-4(8),6-diene-14-carboxylate
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7744 mL | 13.8719 mL | 27.7439 mL | |
| 5 mM | 0.5549 mL | 2.7744 mL | 5.5488 mL | |
| 10 mM | 0.2774 mL | 1.3872 mL | 2.7744 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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