| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
|
| Targets |
PKC serotonin DGK 2.8 μM (IC50)
|
|---|---|
| ln Vitro |
R59-022 (10 μM, 1 min) hydrochloride increases aggregation of platelets [2]. Norepinephrine release from chromaffin cells is enhanced by R 59-022 (30 μM, 0-60 min) hydrochloride [3]. PKC is activated in HeLa and U87 cells by R 59-022 hydrochloride (40 μM, 30 minutes) [4]. The entry of EBOV GP into Vero cells is blocked by R 59-022 (0-10 μM, 4 hours) hydrochloride [5].
|
| ln Vivo |
SCID mice transplanted with U87 GBM cells had a considerably higher median survival rate when given 59-022 (2 mg/kg, i.p., for 12 days) hydrochloride [6].
|
| Cell Assay |
Western Blot Analysis[4]
Cell Types: HeLa cells Tested Concentrations: 40 uM Incubation Duration: 30 min Experimental Results: Increased the phosphorylation of PKC downstream targets by about 2.5-fold. |
| Animal Protocol |
Animal/Disease Models: SCID (severe combined immunodeficient) mouse implanted with U87 GBM cells[6]
Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection Experimental Results: Increased median survival and diminished tumor volume. |
| References |
|
| Molecular Formula |
C27H27CLFN3OS
|
|---|---|
| Molecular Weight |
496.039187669754
|
| Exact Mass |
495.154
|
| CAS # |
93076-98-3
|
| Related CAS # |
R 59-022;93076-89-2
|
| PubChem CID |
23326062
|
| Appearance |
Off-white to light yellow solid powder
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
5
|
| Heavy Atom Count |
34
|
| Complexity |
868
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C(C1C=CC=CC=1)(C1C=CC(F)=CC=1)=C1CCN(CCC2=C(N=C3SC=CN3C2=O)C)CC1.Cl
|
| InChi Key |
APNKGVNEUKASGR-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C27H26FN3OS.ClH/c1-19-24(26(32)31-17-18-33-27(31)29-19)13-16-30-14-11-22(12-15-30)25(20-5-3-2-4-6-20)21-7-9-23(28)10-8-21;/h2-10,17-18H,11-16H2,1H3;1H
|
| Chemical Name |
6-[2-[4-[(4-fluorophenyl)-phenylmethylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[3,2-a]pyrimidin-5-one;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) |
DMSO : 25 mg/mL (50.40 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.04 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.5 mg/mL (5.04 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0160 mL | 10.0798 mL | 20.1597 mL | |
| 5 mM | 0.4032 mL | 2.0160 mL | 4.0319 mL | |
| 10 mM | 0.2016 mL | 1.0080 mL | 2.0160 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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