Size | Price | Stock | Qty |
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10mg |
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Other Sizes |
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ln Vitro |
In endotoxin-stimulated peritoneal macrophages, U-74389G (12.5, 25 and 50 μM; 24 h) suppresses the formation of nitrite[3].
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ln Vivo |
Significant anti-inflammatory efficacy is demonstrated by U-74389G (intravenous injection; 10 mg/kg; once daily; 6 d) treatment, which can lower colonic TNF-α, improve CMDI score, and enhance weight change[2]. The administration of U-74389G (intravenous injection; 15 or 30 mg/kg) provides substantial protection against lethality induced by lipopolysaccharide, lowers plasma nitrite levels, improves liver function, lowers hypotension, brings aortic ring hyporeactivity back to control levels, and inhibits the activity of inducible NO synthase in the liver and aorta[3].
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Cell Assay |
Cell Viability Assay[3]
Cell Types: Peritoneal macrophages Tested Concentrations: 12.5, 25 and 50 μM Incubation Duration: 24 hrs (hours) Experimental Results: diminished the nitrite concentrations in the supernatants of LPS-primed macrophages in a dose-dependent manner. |
Animal Protocol |
Animal/Disease Models: Rat model of trinitrobenzenesulfonic acid-induced colitis[2]
Doses: 10 mg/kg Route of Administration: intravenous (iv) injection; 10 mg/kg; one time/day; 6 d Experimental Results: decreased TNF -α, the macroscopic index of mucosal damage score (CMDI) and increased body weight. Animal/Disease Models: Male Sprague–Dawley rats injected with Lipopolysaccharide[3] Doses: 15 or 30 mg/kg Route of Administration: intravenous (iv) injection; 15 or 30 mg/ kg Experimental Results: Protected against lipopolysaccharide-induced lethality (90% survival rate 24 h and 80% 72 h after Lipopolysaccharide injection, respectively, following the highest dose). |
References |
[1]. A M Perna, et al. Protection of rat heart from ischaemia-reperfusion injury by the 21-aminosteroid U-74389G. Pharmacol Res. 1996 Jul-Aug;34(1-2):25-31.
[2]. Georgios Antonios Margonis, et al. Effectiveness of sildenafil and U-74389G in a rat model of colitis. J Surg Res. 2015 Feb;193(2):667-74. [3]. D Altavilla, et al. The lazaroid, U-74389G, inhibits inducible nitric oxide synthase activity, reverses vascular failure and protects against endotoxin shock. Eur J Pharmacol. 1999 Mar 12;369(1):49-55. |
Molecular Formula |
C41H54N6O6
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Molecular Weight |
726.90
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CAS # |
153190-29-5
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
C[C@@]12C=CC(=O)C=C2CC[C@H]3[C@@H]4CC[C@H](C(=O)CN5CCN(CC5)C6=NC(=NC(=C6)N7CCCC7)N8CCCC8)[C@@]4(C)CC=C31.C(=C/C(=O)O)/C(=O)O
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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 (137.57 mM)
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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.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.3757 mL | 6.8785 mL | 13.7571 mL | |
5 mM | 0.2751 mL | 1.3757 mL | 2.7514 mL | |
10 mM | 0.1376 mL | 0.6879 mL | 1.3757 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.