| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
| ln Vitro |
PKRA83 (1 µg/mL) hydrochloride effectively reduced PK2-induced branching of microvascular endothelial cells in vitro [1]. PKRA83 (2 μM, 24 h) hydrochloride blocked the neuroprotective effect of rPK2 in dopaminergic N27 cells (rPK2 protects N27 cells from MPP+-induced dopaminergic neuronal cell death) [3].
|
|---|---|
| ln Vivo |
PKRA83 (20 mg/kg; intraperitoneal injection) hydrochloride showed antitumor activity in a xenograft tumor model of astroblastoma[1]. PKRA83 (15 mg/kg; intraperitoneal injection, once daily for 2 weeks) hydrochloride blocked collagen-induced arthritis[2].
|
| Animal Protocol |
Animal/Disease Models: glioblastoma (D456MG glioma cell) nu/nu mouse xenograft tumor model[1]
Doses: 20 mg/kg Route of Administration: i.p, daily Experimental Results: Decreased tumor growth rate and tumor weight. Decreased relative blood vessel density and Increased areas of necrotic regions in tumors. Animal/Disease Models: Collagen-induced arthritis in mice[2] Doses: 15 mg/kg Route of Administration: i.p, daily for 2 weeks Experimental Results: Showed less extensive inflammatory cell infiltration and synovial thickening in the joints (Histological evaluation). Lowered IL-1β and 1 L-6 gene expression levels in the joints. |
| References |
| Molecular Formula |
C27H35CL2FN2O4
|
|---|---|
| Molecular Weight |
541.48
|
| Related CAS # |
PKRA83; 1233926-87-8
|
| Appearance |
Typically exists as solids at room temperature
|
| Synonyms |
PKRA7 hydrochloride
|
| 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 | 1.8468 mL | 9.2340 mL | 18.4679 mL | |
| 5 mM | 0.3694 mL | 1.8468 mL | 3.6936 mL | |
| 10 mM | 0.1847 mL | 0.9234 mL | 1.8468 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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