| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
ITX5061 (1 μM) free base significantly inhibited SR-BI-mediated HDL uptake in HEK 293 cells overexpressing SR-BI[1].
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|---|---|
| ln Vivo |
ITX5061 (30 mg/kg; once daily; for 7 days) free base increased HDL-C and apoA-I levels in HuAITg mice, promoted the conversion of HDL to larger particles, and reduced the catabolism and liver uptake of HDL-CE. After one week of treatment, HDL-C increased by 50% and apoA-I increased by 15% [1]. ITX5061 (30 mg/kg; once daily; for 7 days) free base increased HDL-C levels in wild-type mice in an SR-BI-dependent manner, but had no effect on HDL-C in SR-BI−/− mice [1]. ITX5061 (0.037% added to diet; daily; for 18 weeks) free base increased HDL-C by 30% in Ldlr+/− mice fed the Paigen diet for 18 weeks and reduced early atherosclerotic lesions of the aortic arch by 40%, without being related to CETP expression [1].
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| Animal Protocol |
Animal/Disease Models:C57Bl/6 Human Apolipoprotein AI Transgenic Mice (HuAITg)[1]
Doses: 30 mg/kg Route of Administration: Once daily for 7 days Experimental Results: High-density lipoprotein cholesterol (HDL-C) levels increased by 50% compared to baseline. Non-HDL-C levels remained unchanged. Apolipoprotein AI (apoA-I) levels increased by 15% compared to the vector control group. HDL was induced to convert to large-particle HDL. HDL-CE catabolism decreased to 1.86 pools/day (compared to 2.47 pools/day in the control group, P<0.05). HDL-CE production was the same as in the control group, at 129 μg/g/day. [3H]CE accumulation in the liver was significantly reduced. Animal/Disease Models:F1 hybrid C57BL/6 × DBA/1 Ldlr+/− (injection of AAV-CETP to induce CETP expression or not; fed a Paigen high-fat/high-cholesterol/high-cholesterol diet for 18 weeks) [1] Doses: 0.037% added to diet Route of Administration: Once daily; 18 weeks Experimental Results: High-density lipoprotein cholesterol (HDL-C) concentration increased by 30%. There was no difference in total cholesterol or triglyceride levels compared with the control group. Early atherosclerotic lesions of the aortic arch decreased by 40% (regardless of CETP expression). The area of aortic valve lesions tended to decrease, but did not reach statistical significance. |
| References |
| Molecular Formula |
C30H37N3O7S
|
|---|---|
| Molecular Weight |
583.70
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| CAS # |
848144-15-0
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| Appearance |
Typically exists as solids at room temperature
|
| SMILES |
O=C(NC=1C=C(C=C(NS(=O)(=O)C)C1OC)C(C)(C)C)C(=O)C2=CC=C(OCCN3CCOCC3)C=4C=CC=CC24
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.7132 mL | 8.5660 mL | 17.1321 mL | |
| 5 mM | 0.3426 mL | 1.7132 mL | 3.4264 mL | |
| 10 mM | 0.1713 mL | 0.8566 mL | 1.7132 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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