| Size | Price | |
|---|---|---|
| 100mg | ||
| 250mg | ||
| 500mg | ||
| Other Sizes |
| Targets |
mTORC1 S6K1
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|---|---|
| ln Vitro |
With rat primary hepatocytes, coronarin A (3-30 μM; 4 or 12 h) suppresses gluconeogenesis by activating the ERK-dependent Wnt/β-catenin/TCF7L2 pathway and increases glycogen synthesis by activating PI3K/Akt/GSK3β signaling[1]. IRS1 tyrosine phosphorylation is increased at 1-30 μM for 4 hours by blocking mTOR/S6K1 signaling[1].
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| ln Vivo |
Mice's hyperglycemia is reduced by coronerin A (30 or 100 mg/kg; ip or po; once daily for 22 days)[1]. In mice with ob/ob livers, coronerin A (100 mg/kg; po; once daily for 22 days) suppresses the mTOR/S6K1 pathway, hence activating PI3K/Akt and ERK/β-catenin signaling[1]. Coronarin A's pharmacokinetic characteristics following a single dosage in ob/ob mice[1]. The data for Coronarin A, including t1/2 (h), tmax (h), Cmax (ng/mL), AUC0-t (ng⋅h/mL) and AUC0-∞ (ng⋅h/mL), as well as MRT (h), are displayed as the average of three mice. a30 mg/kg of coronarin A was given intraperitoneally or orally to ob/ob mice.
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: Primary rat hepatocytes Tested Concentrations: 1, 3, 10 and 30 μM Incubation Duration: 4 h Experimental Results: Increased the Akt and GSK3β phosphorylation dose-dependently. Dose-dependently stimulated the phosphorylation of both ERK1 and ERK2. Increased the phosphorylation of β-catenin and mitogen-activated protein kinase kinase (MEK). Dose-dependently enhanced the tyrosine phosphorylation of IRS1 at Tyr1222, whereas the serine phosphorylation of IRS1 was dose-dependently inhibited. diminished the phosphorylation of mTOR, S6K1 and S6. Cell Viability Assay[1] Cell Types: Primary rat hepatocytes Tested Concentrations: 1, 3, 10, 30, 100 and 300 μM Incubation Duration: 5.5 h or 12 h Experimental Results: demonstrated no toxicity at 1-30 μM, diminished cell viability after 12 h incubation at 100 μM. |
| Animal Protocol |
Animal/Disease Models: Male ob/ob mice[1]
Doses: 30 mg/kg (IP) or 100 mg/kg ( PO) Route of Administration: Oral or intraperitoneal (ip) administration, one time/day for 22 days Experimental Results: Dramatically diminished the non-fasting and fasting blood glucose. Dramatically decreased the serum insulin concentration at 15 min after glucose loading, decreased the average daily food intake while the body weight was unaffected. Increased hepatic glycogen content and the expression levels of gluconeogenic genes Pck1 and G6pc were Dramatically diminished. Animal/Disease Models: Female ob/ob mice[1] Doses: 30 mg/kg Route of Administration: intraperitoneal (ip) or oral administration (pharmacokinetic/PK Analysis) Experimental Results: intraperitoneal (ip) injection demonstrated higher plasma exposure than po (oral gavage) at the same dose of 30 mg/kg, with Cmax value of 1073 and 388 ng/mL, respectively. |
| References |
[1]. Huang SL, et al. Coronarin A modulated hepatic glycogen synthesis and gluconeogenesis via inhibiting mTORC1/S6K1 signaling and ameliorated glucose homeostasis of diabetic mice. Acta Pharmacol Sin. 2022 Sep 9.
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| Molecular Formula |
C20H28O2
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|---|---|
| Molecular Weight |
300.44
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| CAS # |
119188-33-9
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| SMILES |
C1OC=C(/C=C/[C@H]2C(=C)[C@@H](O)C[C@H]3C(CCC[C@]23C)(C)C)C=1
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| 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)
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| 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.) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.3285 mL | 16.6423 mL | 33.2845 mL | |
| 5 mM | 0.6657 mL | 3.3285 mL | 6.6569 mL | |
| 10 mM | 0.3328 mL | 1.6642 mL | 3.3285 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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