| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
4L2-P13D (0.5-5 μM; 72 h) reduced the expression of profibrotic factors (FN1, COL1A1) in HK-2 cells in a dose-dependent manner [1]. 4L2-P13D (0-50 μM; 24 h) did not show cytotoxicity to HK-2 cells even at concentrations as high as 50 μM [1].
|
|---|---|
| ln Vivo |
4L2-P13D (0.5-2 mg/kg; subcutaneous injection; daily administration; 7 days) showed strong anti-renal fibrosis activity in the UUO mouse model [1].
|
| Cell Assay |
Western Blot Analysis [1]
Cell Types: TGF-β1 induced human proximal renal tubular epithelial cells (HK-2) Tested Concentrations: 0.5, 2 and 5 μM Incubation Duration: 72 hours Experimental Results: The expression of fibronectin (FN1) and type I collagen (COL1A1) was reduced in a dose-dependent manner. |
| Animal Protocol |
Animal/Disease Models:C57BL/6J (male, 6-8 weeks old, unilateral ureteral obstruction model) [1]
Doses: 0.5 mg/kg; 2 mg/kg Route of Administration: Subcutaneous injection; once daily for 7 consecutive days Experimental Results: The expression levels of fibrosis markers FN1 and α-smooth muscle α-SMA were significantly reduced. The expression levels of pro-inflammatory markers (TNF-α, TGF-β1, IL-6, IL-1β) and renal injury markers (Kim1, Ngal) were significantly reduced. Blood urea nitrogen (BUN) and creatinine levels were reduced. Collagen deposition was significantly improved, and the high-dose group was more effective than the low-dose group. |
| References |
| Molecular Formula |
C89H123N19O23S
|
|---|---|
| Molecular Weight |
1859.11
|
| Sequence |
Ac-Tyr-Leu-Ile-Gln-His-Tyr-Tyr-Thr-Phe-Ile-Ala-Leu-Asp-Cys-Gly-NH2 (sulfide bridge: Tyr1-Cys14)Ac-YLIQHYYTFIALDCG-NH2 (sulfide bridge: Tyr1-Cys14)
|
| SequenceShortening |
Ac-YLIQHYYTFIALDCG-NH2 (sulfide bridge: Tyr1-Cys14)
|
| Appearance |
Typically exists as solids at room temperature
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 0.5379 mL | 2.6895 mL | 5.3789 mL | |
| 5 mM | 0.1076 mL | 0.5379 mL | 1.0758 mL | |
| 10 mM | 0.0538 mL | 0.2689 mL | 0.5379 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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