| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
|
| ln Vitro |
In vitro, microvascular endothelial cells' PK2-induced branching is efficiently inhibited by PKRA83 (1 µg/mL) [1]. The neuroprotective effect of rPK2 in dopaminergic N27 cells is blocked by PKRA83 (2 μM, 24 hours) [3]. RPK2 shields N27 cell channels from MPP+-induced dopaminergic neuronal cell death.
|
|---|---|
| ln Vivo |
In xenograft tumor models of astroblastoma, PKRA83 (20 mg/kg; i.p.) exhibits anti-activity [1]. 15 mg/kg of PKRA83 administered intraperitoneally once daily for two weeks inhibits
|
| Animal Protocol |
Animal/Disease Models: glioblastoma (D456MG glioma cells) nu/nu mouse xenograft tumor model [1]
Doses: 20 mg/kg Route of Administration: intraperitoneal (ip) injection, daily Experimental Results: diminished tumor growth rate and tumor weight. The relative blood vessel density diminished and the area of tumor necrosis increased. Animal/Disease Models: collagen-induced arthritis in mice [2] Doses: 15 mg/kg Route of Administration: intraperitoneal (ip) injection, one time/day for 2 weeks Experimental Results: demonstrated less infiltration of inflammatory cells in the joints and thickening of the synovium ( histological evaluation). Reduces IL-1β and 1 L-6 gene expression levels in joints. |
| References |
|
| Molecular Formula |
C27H34CLFN2O4
|
|---|---|
| Molecular Weight |
505.02
|
| Exact Mass |
504.219
|
| CAS # |
1233926-87-8
|
| Related CAS # |
PKRA83 hydrochloride hydrate
|
| PubChem CID |
66726148
|
| Appearance |
Colorless to light yellow ointment
|
| LogP |
5
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
8
|
| Heavy Atom Count |
35
|
| Complexity |
686
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
CC(C)CN(CC1=CC2=C(C(=C1)Cl)OCCCO2)C(=O)[C@@H]3CCN(C3)CC4=CC(=C(C=C4)F)OC
|
| InChi Key |
GZHUKRDKTDCKQD-OAQYLSRUSA-N
|
| InChi Code |
InChI=1S/C27H34ClFN2O4/c1-18(2)14-31(16-20-11-22(28)26-25(13-20)34-9-4-10-35-26)27(32)21-7-8-30(17-21)15-19-5-6-23(29)24(12-19)33-3/h5-6,11-13,18,21H,4,7-10,14-17H2,1-3H3/t21-/m1/s1
|
| Chemical Name |
(3R)-N-[(6-chloro-3,4-dihydro-2H-1,5-benzodioxepin-8-yl)methyl]-1-[(4-fluoro-3-methoxyphenyl)methyl]-N-(2-methylpropyl)pyrrolidine-3-carboxamide
|
| 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) |
DMSO : ~25 mg/mL (~49.50 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.95 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9801 mL | 9.9006 mL | 19.8012 mL | |
| 5 mM | 0.3960 mL | 1.9801 mL | 3.9602 mL | |
| 10 mM | 0.1980 mL | 0.9901 mL | 1.9801 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
