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| ln Vitro |
On mBMMC and RPMC cells, the allergy receptor RBL-2H3 is inhibited by orientin (1 µM) [1].
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| ln Vivo |
In a PCA mouse model, one intravenous dosage of orientin (0.1–10 mg/kg) decreases allergy responses [1]. Orientin injections, 10–40 mg/kg, intraperitoneally once daily for 12 days) Within SNL
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| Cell Assay |
Cell viability assay [1]
Cell Types: RBL-2H3, mBMMCs, and RPMCs Tested Concentrations: 0.01–100 µM Incubation Duration: 8 h Experimental Results: Significant inhibition of histamine and β-hexosamine in RBL-2H3, mBMMCs, and RPMC cells enzyme levels. Inhibits intracellular calcium levels in RBL-2H3, mBMMC and RPMC cells. Dramatically inhibits the expression and secretion of pro-inflammatory cytokines in RBL-2H3 cells. Inhibits phosphorylation in RBL-2H3 cells. |
| Animal Protocol |
Animal/Disease Models: SNL rat model [2]
Doses: 10, 20, 40 mg/kg Route of Administration: intraperitoneal (ip) injection; one time/day for 12 days Experimental Results: Alleviates the down-regulation of PWL and promotes behavior in the SNL rat model recover. Reduces levels of IL-6, IL-1β and TNF-α. Increases levels of anti-inflammatory IL-10. Reduce MDA levels. |
| References |
[1]. Dhakal H, et al. Inhibitory effects of orientin in mast cell-mediated allergic inflammation. Pharmacol Rep. 2020 Jan 24.
[2]. Guo D, et al. Orientin and neuropathic pain in rats with spinal nerve ligation. 61Int Immunopharmacol. 2018 May;58:72-79. |
| Molecular Formula |
C21H20O11
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|---|---|
| Molecular Weight |
448.3769
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| Exact Mass |
448.10
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| Elemental Analysis |
C, 56.25; H, 4.50; O, 39.25
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| CAS # |
28608-75-5
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| Appearance |
Solid powder
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| SMILES |
C1=CC(=C(C=C1C2=CC(=O)C3=C(O2)C(=C(C=C3O)O)[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)O)O
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| InChi Key |
PLAPMLGJVGLZOV-VPRICQMDSA-N
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| InChi Code |
InChI=1S/C21H20O11/c22-6-14-17(28)18(29)19(30)21(32-14)16-11(26)4-10(25)15-12(27)5-13(31-20(15)16)7-1-2-8(23)9(24)3-7/h1-5,14,17-19,21-26,28-30H,6H2/t14-,17-,18+,19-,21+/m1/s1
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| Chemical Name |
2-(3,4-dihydroxyphenyl)-5,7-dihydroxy-8-[(2S,3R,4R,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]chromen-4-one
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| Synonyms |
Lutexin; Orientin
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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 : ~31.25 mg/mL (~69.70 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.64 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 20.8 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: ≥ 2.08 mg/mL (4.64 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 20.8 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2303 mL | 11.1513 mL | 22.3025 mL | |
| 5 mM | 0.4461 mL | 2.2303 mL | 4.4605 mL | |
| 10 mM | 0.2230 mL | 1.1151 mL | 2.2303 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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