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Laflunimus (HR-325; HR325), an analogue of the Leflunomide-active metabolite A-771726, is a novel and potent immunosuppressive agent that is orally bioactiveand acting ac an dihydroorotate dehydrogenase (DHODH) inhibitor. Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively.
| ln Vitro |
For five days, lipopolysaccharide (LPS) was used to stimulate the release of immunoglobulin from mice splenocytes. IgM and IgG secretion were both reduced by laflunimus, with IC50 values of 2.5 and 2 µM, respectively. When 50 µ M of uridine was added, these values rose to 70 and 60 µ M, respectively. On 70Z/3 cells, laflunimus inhibits the expression of the kappa light-chain cell surface, a feature that uridine also reverses[1]. When it comes to inhibiting PGHS in guinea pig polymorphonuclear leukocytes (IC50 = 415 and 4400 nM, respectively) and isolated ovine PGHS-1 (IC50 = 64 and 742 µM) and PGHS-2 (IC50 = 100 and 2766 µM), laflunimus (HR325) is more effective than A77 1726[2].
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| ln Vivo |
With ID50 values of 38 mg/kg, HR325 (50 mg/kg; po; days 14–18 after SRBC injection) suppresses the secondary anti-sheep red blood cell (SRBC) antibody response[1].
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| Animal Protocol |
Animal/Disease Models: Male CD -1 mice (20-24 g)[1]
Doses: 50 mg/kg Route of Administration: Oral; days 14-18 after being injected with SRBC Experimental Results: The level of circulating anti-SRBC IgG in this model was inhibited dose relatedly by orally administered HR325. |
| References |
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| Molecular Formula |
C₁₅H₁₃F₃N₂O₂
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|---|---|
| Molecular Weight |
310.27
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| Exact Mass |
310.093
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| CAS # |
147076-36-6
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| PubChem CID |
54684599
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| Appearance |
Yellow to khaki solid powder
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| Density |
1.441g/cm3
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| Boiling Point |
408.7ºC at 760mmHg
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| Flash Point |
201ºC
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| Vapour Pressure |
2.06E-07mmHg at 25°C
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| Index of Refraction |
1.588
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| LogP |
3.77
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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 |
3
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| Heavy Atom Count |
22
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| Complexity |
529
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1=C(C=CC(=C1)NC(=O)/C(=C(/C2CC2)\O)/C#N)C(F)(F)F
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| InChi Key |
GDHFOVCRYCPOTK-QBFSEMIESA-N
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| InChi Code |
InChI=1S/C15H13F3N2O2/c1-8-6-10(4-5-12(8)15(16,17)18)20-14(22)11(7-19)13(21)9-2-3-9/h4-6,9,21H,2-3H2,1H3,(H,20,22)/b13-11-
|
| Chemical Name |
(Z)-2-cyano-3-cyclopropyl-3-hydroxy-N-[3-methyl-4-(trifluoromethyl)phenyl]prop-2-enamide
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| Synonyms |
LaflunimusHR-325HR325
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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 : ~50 mg/mL (~161.15 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.06 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 | 3.2230 mL | 16.1150 mL | 32.2300 mL | |
| 5 mM | 0.6446 mL | 3.2230 mL | 6.4460 mL | |
| 10 mM | 0.3223 mL | 1.6115 mL | 3.2230 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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