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Etrinabdione (EHP-101; VCE004.8; VCE-004.8) is a semi-synthetic multitarget cannabinoquinoid, acting as a specific PPARγ and CB2 receptor dual agonist with potent anti-inflammatory activity. While activating the HIF pathway, VCE-004.8 inhibits prolyl-hydroxylases (PHDs). Avoiding diet-induced obesity, VCE-004.8 attenuates adipogenesis.
Targets |
PPARγ; CB2
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ln Vivo |
Etrinabdione (i.p.; 20 mg/kg/day; for 3 weeks) causes a notable decrease in body weight gain, total fat mass, adipocyte volume, and plasma triglyceride levels over the course of three weeks in HFD mice. Additionally, etrinabdione has been shown to significantly improve glucose tolerance, lower levels of leptin, an adiposity marker, and raise levels of adiponectin, incretins (GLP-1 and GIP), and adiponectin[1].
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References |
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Molecular Formula |
C28H35NO3
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Molecular Weight |
433.582408189774
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Exact Mass |
433.26
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Elemental Analysis |
C, 77.56; H, 8.14; N, 3.23; O, 11.07
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CAS # |
1818428-24-8
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Related CAS # |
1818428-24-8
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Appearance |
Solid powder
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SMILES |
CCCCCC1=C(C(=C(C(=O)C1=O)[C@@H]2C=C(CC[C@H]2C(=C)C)C)O)NCC3=CC=CC=C3
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InChi Key |
CGGGAXJIRQSRPH-JTHBVZDNSA-N
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InChi Code |
InChI=1S/C28H35NO3/c1-5-6-8-13-22-25(29-17-20-11-9-7-10-12-20)27(31)24(28(32)26(22)30)23-16-19(4)14-15-21(23)18(2)3/h7,9-12,16,21,23,29,31H,2,5-6,8,13-15,17H2,1,3-4H3/t21-,23+/m0/s1
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Chemical Name |
5-(benzylamino)-4-hydroxy-3-[(1R,6R)-3-methyl-6-prop-1-en-2-ylcyclohex-2-en-1-yl]-6-pentylcyclohexa-3,5-diene-1,2-dione
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Synonyms |
etrinabdione; EHP-101; EHP101; VCE-004; EHP 101; VCE004; VCE 004; VCE004.8; VCE 004.8; VCE-004.8
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HS Tariff Code |
2934.99.9001
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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: ~50 mg/mL (~115.3 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.77 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 (5.77 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. 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 (5.77 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 | 2.3064 mL | 11.5319 mL | 23.0638 mL | |
5 mM | 0.4613 mL | 2.3064 mL | 4.6128 mL | |
10 mM | 0.2306 mL | 1.1532 mL | 2.3064 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.
VCE-004.8 mediates HIF-1α stabilization. J Neuroinflammation . 2018 Mar 1;15(1):64. td> |
Effect of VCE-004.8 on PDH activity and HIF-1α hydroxylation and stabilization. J Neuroinflammation . 2018 Mar 1;15(1):64. td> |
VCE-004.8 induces the expression of HIF-dependent genes. J Neuroinflammation . 2018 Mar 1;15(1):64. td> |
Characterization of VCE-004.8 as a selective PPARγ agonist. Sci Rep . 2018 Oct 31;8(1):16092. td> |
Effect of VCE-004.8 on MSCs differentiation. MSCs were differentiated in adipogenic medium (AM) in the presence of RGZ or VCE-004.8. Sci Rep . 2018 Oct 31;8(1):16092. td> |
Effect of VCE-004.8 on body weight gain, food intake and body composition. Sci Rep . 2018 Oct 31;8(1):16092. td> |