Size | Price | Stock | Qty |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
R1487 HCl is a novel, potent, orally bioavailable, and highly selective inhibitor of p38α mitogen-activated protein kinase. IIt was discovered during the development of a new series of p38α inhibitors and advanced into a phase 2 clinical trial for rheumatoid arthritis. The pharmacokinetic characteristics of R1487 are good.
Targets |
p38α (Kd = 0.2 nM); p38β (Kd = 29 nM)
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ln Vitro |
R1487 Hydrochloride exhibits IC50 values of 200 nM for the inhibition of TNF-induced IL-1β production and 10 nM for the inhibition of p38α[1].
R1487 (Compounds 2a) inhibits LPS-induced production of IL-1β in human whole blood (HWB) and TNFα production by human monocytic cells (THP-1)[1]. |
ln Vivo |
R1487 (Compounds 2a, orally) demonstrably inhibits serum TNFα and IL-1β in a dose-dependent manner[1].
In rat, dog, and monkey, the oral bioavailability of 10 mg/kg R1487 (Compounds 2a) was 51.6%, 29.3%, and 10.3%, respectively[1]. |
References |
Molecular Formula |
C19H19CLF2N4O3
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Molecular Weight |
424.833
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Exact Mass |
424.1113745
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Elemental Analysis |
C, 53.72; H, 4.51; Cl, 8.34; F, 8.94; N, 13.19; O, 11.30
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CAS # |
449808-64-4
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Related CAS # |
449808-64-4
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Appearance |
Solid powder
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SMILES |
CN1C2=NC(=NC=C2C=C(C1=O)OC3=C(C=C(C=C3)F)F)NC4CCOCC4.Cl
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InChi Key |
RQHSAIGGUWVOBG-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H18F2N4O3.ClH/c1-25-17-11(10-22-19(24-17)23-13-4-6-27-7-5-13)8-16(18(25)26)28-15-3-2-12(20)9-14(15)21;/h2-3,8-10,13H,4-7H2,1H3,(H,22,23,24);1H
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Chemical Name |
6-(2,4-difluorophenoxy)-8-methyl-2-(oxan-4-ylamino)pyrido[2,3-d]pyrimidin-7-one;hydrochloride
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Synonyms |
R-1487 HCl; R1487 HCl; R 1487 HCl
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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: ~20.8 mg/mL (~49.0 mM)
H2O: < 0.1 mg/mL |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.90 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 (4.90 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 | 2.3539 mL | 11.7694 mL | 23.5388 mL | |
5 mM | 0.4708 mL | 2.3539 mL | 4.7078 mL | |
10 mM | 0.2354 mL | 1.1769 mL | 2.3539 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.