| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
In lymphocytes, GNF362 (0–10 mM) inhibits Ins (1,3,4,5) P4 production, increases antigen receptor-driven Ca2+ responses, and triggers activated T cell apoptosis in an Itpkb-dependent manner[1]. After antigen receptor cross-linking, GNF362 increases SOC responses; in primary B or T lymphocytes, its EC50 is 12 nM[1].
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|---|---|
| ln Vivo |
Orally administered GNF362 (6 or 20 mg/kg; twice daily; 21 days) inhibits the formation of antibodies to a modest degree, but at 6 mg/kg, it significantly lowers the infiltration of inflammatory cells into the joint, joint injury, and proteoglycan loss[1].
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| Animal Protocol |
Animal/Disease Models: A Lewis rat antigen-induced arthritis (rAIA) model[1]
Doses: 6 or 20 mg/kg Route of Administration: Orally administration; 6 or 20 mg/kg; twice (two times) daily; 21 days Experimental Results: decreased knee swelling in both the 20mg/kg and 6mg/kg treatment groups of GNF362 by 47% and 34%, respectively. |
| References |
| Molecular Formula |
C22H21F3N6
|
|---|---|
| Molecular Weight |
426.437554121017
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| Exact Mass |
426.177
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| CAS # |
1003019-41-7
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| PubChem CID |
57999583
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| Appearance |
White to off-white solid powder
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| LogP |
3.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
31
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| Complexity |
641
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| Defined Atom Stereocenter Count |
1
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| SMILES |
FC(C1=CN=C(C=C1)N1CCN(CC2C=NNC=2C2C=CC(C#N)=CC=2)C[C@H]1C)(F)F
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| InChi Key |
VNTCGXMLDSKOKN-OAHLLOKOSA-N
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| InChi Code |
InChI=1S/C22H21F3N6/c1-15-13-30(8-9-31(15)20-7-6-19(12-27-20)22(23,24)25)14-18-11-28-29-21(18)17-4-2-16(10-26)3-5-17/h2-7,11-12,15H,8-9,13-14H2,1H3,(H,28,29)/t15-/m1/s1
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| Chemical Name |
4-[4-[[(3R)-3-methyl-4-[5-(trifluoromethyl)pyridin-2-yl]piperazin-1-yl]methyl]-1H-pyrazol-5-yl]benzonitrile
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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)
|
| Solubility (In Vitro) |
DMSO: 100 mg/mL (234.50 mM)
Ethanol: ≥ 50 mg/mL (117.25 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.86 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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.86 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.88 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. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3450 mL | 11.7250 mL | 23.4500 mL | |
| 5 mM | 0.4690 mL | 2.3450 mL | 4.6900 mL | |
| 10 mM | 0.2345 mL | 1.1725 mL | 2.3450 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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