| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
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| Targets |
Cbl
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|---|---|
| ln Vitro |
Picrotin has an IC50 value of 13.1 μM and is sensitive to α2 GlyR[1].The analgesic hydrocotarnine (CRIN-2) has patent WO2011160016A2[1]. In THP-1 cells, hydrocotarnine (10 μM; 1 hour) raises the secretion of IL-1β and IL-18, while tyrosine-phosphorylated protein levels overall are increased by (0.1–10 μM; 1 hour) [1]. THP-1-derived macrophages' glycolytic and glycolytic reserve capacities are increased by hydrocotarnine (50 μM; 0-100 min) [2]. In THP-1-derived macrophages, hydrocotarnine (50 μM; 16 hours) inhibits Cbl and raises total GLUT1 protein [2]. It is well recognized that hydrocotanine lessens cancer pain and increases the analgesic effects of opioids [3].
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| ln Vivo |
Hydrocotarnine (10 mg/kg/d; ip; 9 d) has an inhibitory effect on Cbl and causes an increase in IL-18 levels, indicating enhanced activation of the NLRP3 inflammasome in mice [1]. Hydrocotarnine (10 mg/kg/d; i.p.; 9 d) protects mice from DSS-induced colitis with lower scores on pathological assessments of inflammation, epithelial defects, and crypt atrophy [1].
|
| Cell Assay |
Western Blot Analysis[1]
Cell Types: THP-1 Cell Tested Concentrations: 0.1, 1, 10 μM Incubation Duration: 1 hour Experimental Results: Induces p-Pyk2 loss and increases the levels of tyrosine phosphorylated proteins in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models: DSS-induced C57BL/6 mouse colitis model (6-9 weeks old) [1]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day; 9 days, 2.5% DSS treatment from day 1 Start on day 7 and end on day 7 Experimental Results: Weight loss in mice with DSS-induced colitis was Dramatically attenuated compared with PBS-treated control mice, suggesting that reducing negative regulation of NLRP3 inflammasome activation can alleviate colitis in animal models middle. |
| References |
[1]. Chung IC, et al. Src-family kinase-Cbl axis negatively regulates NLRP3 inflammasome activation. Cell Death Dis. 2018 Oct 31;9(11):1109.
[2]. Lin HC, et al. Cbl Negatively Regulates NLRP3 Inflammasome Activation through GLUT1-Dependent Glycolysis Inhibition. Int J Mol Sci. 2020 Jul 19;21(14):5104. [3]. Kim KU, et al. DITMD-induced mitotic defects and apoptosis in tumor cells by blocking the polo-box domain-dependent functions of polo-like kinase 1. Eur J Pharmacol. 2019 Mar 15;847:113-122. |
| Molecular Formula |
C12H15NO3
|
|---|---|
| Molecular Weight |
221.25200
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| Exact Mass |
221.10519334
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| CAS # |
550-10-7
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| Appearance |
Light yellow to yellow solid
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| SMILES |
CN1CCC2=CC3=C(C(=C2C1)OC)OCO3
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| InChi Key |
XXANNZJIZQTCBP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H15NO3/c1-13-4-3-8-5-10-12(16-7-15-10)11(14-2)9(8)6-13/h5H,3-4,6-7H2,1-2H3
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| Chemical Name |
4-methoxy-6-methyl-7,8-dihydro-5H-[1,3]dioxolo[4,5-g]isoquinoline
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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 Vitro) |
DMSO : ≥ 100 mg/mL (~451.98 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.30 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.30 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.30 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.5198 mL | 22.5989 mL | 45.1977 mL | |
| 5 mM | 0.9040 mL | 4.5198 mL | 9.0395 mL | |
| 10 mM | 0.4520 mL | 2.2599 mL | 4.5198 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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