| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
CLIK-148 (100 nM-10 μM) potently and specifically inhibited tissue catepsin L activity in rat liver at a concentration of 100 nM, while at a concentration of 1 μM it had almost no inhibitory effect on tissue catepsin B and C, and at a concentration of 10 μM it had only a weak inhibitory effect on tissue catepsin S and K [1]. CLIK-148 (50 μM, 24 hours) inhibited tissue catepsin L activity, thereby blocking proCCK from generating CCK9, and ultimately reducing the production of CCK8 in pituitary AtT-20 cells [2]. CLIK-148 (1-10 nM, 72 hours) effectively inhibited bone collagen degradation mediated by TNF-α-activated human and mouse osteoclasts [3]. CLIK-148 (100 μM) can effectively protect HMG-CoA reductase from pathological degradation in the event of necrosis in C100 cells [4].
|
|---|---|
| ln Vivo |
CLIK-148 (1-10 mg/kg, intraperitoneal injection, single dose) significantly inhibited tissue topology L in blood vessels, but had no effect on the activity of tissue topology B [1]. CLIK-148 (50 mg/kg, renal, daily for 7 days) was effective in preventing and alleviating tumor-induced hypercalcemia [3]. CLIK-148 (32-128 mg/kg, non-vascular or intravascular injection, once daily for 7 days). CLIK-148 (32-128 mg/kg, non-vascular or intravascular injection, once daily for 7 days) CLIK-148 (100-200 mg/kg, head, once daily for 14 days) was effective in pivotal movement and local destruction [3].
|
| Animal Protocol |
Animal/Disease Models: LJC-1 cells induced direct bone metastasis and local bone resorption model of cancer established in CDF1 mice[3]
Doses: 5 mg/kg Route of Administration: Oral administration (p.o.), once daily for 7 days Experimental Results: Significantly reduced the serum calcium level in mice. Animal/Disease Models: Colon tumor 26 PMF-15 cells induced hypercalcemia of malignancy model established in CDF1 mice[3] Doses: 32, 64 and 128 mg/kg Route of Administration: Oral administration (p.o.) or intravenous injection (i.v.), once daily for 7 days Experimental Results: Significantly inhibited the decline of calcium content and protect the bones. Animal/Disease Models: Melanoma A375 cells induced distant bone metastasis model established in CDF1 mice[3] Doses: 100 and 200 mg/kg Route of Administration: Oral administration (p.o.), once daily for 14 days Experimental Results: Reduced the area of the metastatic lesion significantly to 1.0 mm². Did not inhibit the metastasis of cancer cells to other organs such as the liver, muscles, and gums. |
| References |
| Molecular Formula |
C22H26N4O4
|
|---|---|
| Molecular Weight |
410.47
|
| CAS # |
215098-90-1
|
| 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
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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 | 2.4362 mL | 12.1812 mL | 24.3623 mL | |
| 5 mM | 0.4872 mL | 2.4362 mL | 4.8725 mL | |
| 10 mM | 0.2436 mL | 1.2181 mL | 2.4362 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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