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| 100mg |
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R-10015 is a broad-spectrum antiviral compound that treats HIV infection. It binds to the ATP-binding pocket and inhibits LIM domain kinase (LIMK) with a potent and selective manner, with an IC50 of 38 nM for human LIMK1.
| Targets |
human LIMK1 (IC50 = 38 nM)
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|---|---|
| ln Vitro |
R-10015 (100 μM; 0-4 hours) directly prevents cofilin phosphorylation in CEM-SS T cells by inhibiting LIM kinase[1].
R-10015 prevents nuclear migration, virion release, and HIV-1 DNA synthesis[1].
R-10015 inhibits a number of viruses, such as herpes simplex virus 1 (HSV-1), Venezuelan equine encephalitis virus (VEEV), Rift Valley fever virus (RVFV), and Zaire ebolavirus (EBOV)[1].
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| ln Vivo |
R-10015 (10 mg/kg; i.p.) shows no signs of toxicity. The outcome raises the prospect of using LIMK inhibitors for a brief period of time to prevent viral infections[1].
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| Cell Assay |
Cell Line: CEM-SS T cells
Concentration: 100 μM Incubation Time: 0 hour,0.5 hour,1 hour,2 hours,4 hours Result: Inhibited cofilin phosphorylation directly through blocking LIM kinase in CEM-SS T cells. |
| Animal Protocol |
6-8 weeks female C3H/HeN mice[1]
10 mg/kg Intraperitoneal injection |
| References |
| Molecular Formula |
C20H19CLN6O2
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|---|---|
| Molecular Weight |
410.856862306595
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| Exact Mass |
410.125
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| Elemental Analysis |
C, 58.47; H, 4.66; Cl, 8.63; N, 20.46; O, 7.79
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| CAS # |
2097938-51-5
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| Related CAS # |
2097938-51-5
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| PubChem CID |
129896912
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| Appearance |
Off-white to pink solid powder
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| LogP |
3.4
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
604
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
MGRJCGXCUUCOQG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H19ClN6O2/c1-29-20(28)12-2-3-14-15(8-12)26-17(25-14)11-4-6-27(7-5-11)19-16-13(21)9-22-18(16)23-10-24-19/h2-3,8-11H,4-7H2,1H3,(H,25,26)(H,22,23,24)
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| Chemical Name |
methyl 2-[1-(5-chloro-7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-yl]-3H-benzimidazole-5-carboxylate
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| Synonyms |
R10015; R-10015; R 10015
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO: 62.5~82 mg/mL (199.6~152.1 mM)
Water ˂1 mg/mL Ethanol: ~10 mg/mL (24.3 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (12.17 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 50.0 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: ≥ 5 mg/mL (12.17 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 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (12.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4339 mL | 12.1696 mL | 24.3392 mL | |
| 5 mM | 0.4868 mL | 2.4339 mL | 4.8678 mL | |
| 10 mM | 0.2434 mL | 1.2170 mL | 2.4339 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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