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| 25mg |
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Purity: ≥98%
RP-54745 (RP 54745) is a novel amino-dithiole-one compound that is active at micromolar concentration on the metabolism of stimulated macrophages, for example, the hexose monophosphate pathway (HMP) and the exocytosis of lysosomal enzymes. LPS-induced interleukin-1 (IL-1) production by murine peritoneal macrophages was also diminished by this compound in vitro as well as in vivo. This effect was confirmed at the mRNA level; at the concentration of 3 x 10(-6) M, the IL-1 alpha and beta mRNA signals were inhibited, whereas the TNF alpha mRNA signal was only slightly lessened. These observations were confirmed in vivo, with a dose of RP 54745 of 25 mg kg-1. These results led us to consider that RP 54745 might influence certain cells and cytokines implicated in the regulation of the immune system, the disfunctioning of which can lead to inflammatory disorders or autoimmune pathologies. In all, as an inhibitor of macrophage stimulation and interleukin-1 production, RP-54745 has a potential to be used as an antirheumatic compound.
| ln Vitro |
LPS-induced interleukin 1 (IL-1) production by mouse peritoneal macrophages is inhibited by RP-54745 [1].
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|---|---|
| ln Vivo |
In various mouse models of induced arthritis, as well as in MRL/lpr mice, which are genetically predisposed to develop autoimmune pathologies including arthritis, RP-54745 (5 mg/kg) is effective at oral dosage modulation. Following three months of treatment with RP-54745, the clinical condition of MRL mice as well as some of its disturbed biochemical and immunological parameters were improved [2].
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| References |
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| Molecular Formula |
C13H12NOS2CL
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|---|---|
| Molecular Weight |
297.82348
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| Exact Mass |
297.005
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| Elemental Analysis |
C, 52.43; H, 4.06; Cl, 11.90; N, 4.70; O, 5.37; S, 21.53
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| CAS # |
135330-08-4
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| PubChem CID |
126203
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.46g/cm3
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| Boiling Point |
411.4ºC at 760 mmHg
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| Flash Point |
202.6ºC
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| Vapour Pressure |
5.59E-07mmHg at 25°C
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| Index of Refraction |
1.707
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| LogP |
4.011
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
18
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| Complexity |
399
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C1SSC(N2C(C)C3=C(C=CC=C3)CC2)=C1Cl
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| InChi Key |
BEJJGVDFQORITE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H12ClNOS2/c1-8-10-5-3-2-4-9(10)6-7-15(8)12-11(14)13(16)18-17-12/h2-5,8H,6-7H2,1H3
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| Chemical Name |
4-Chloro-5-(3,4-dihydro-1-methyl-2(1H)-isoquinolinyl)-3H-1,2-dithiol-3-one
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| Synonyms |
RP-54745; RP 54745; RP54745
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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 mg/mL (~209.86 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.98 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 20.8 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: ≥ 2.08 mg/mL (6.98 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 20.8 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 | 3.3577 mL | 16.7887 mL | 33.5773 mL | |
| 5 mM | 0.6715 mL | 3.3577 mL | 6.7155 mL | |
| 10 mM | 0.3358 mL | 1.6789 mL | 3.3577 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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