Size | Price | Stock | Qty |
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1mg |
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5mg |
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10mg |
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Other Sizes |
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Targets |
pIC50: 8.28 ± 0.11 (GTPγS)[1]
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ln Vitro |
When evaluated at 10 μM, compound 42, or GPR84 antagonist 3, is unable to block the activities of the C3 fatty acid propionate at either FFAR2 or FFAR3[1].
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ln Vivo |
Compound 42, also known as GPR84 antagonist 3, exhibits an excellent elimination half-life of 2.51 hours, a moderate rate of clearance, and bioavailability at a single dose of 1 mg/kg (IV) and 10 mg/kg (Orally).
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Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice (n = 3)[1]
Doses: 1 mg/kg (IV), 10 mg/kg (Orally) Route of Administration: IV, po (oral gavage) once (pharmacokinetic/PK Analysis) Experimental Results: pharmacokinetic/PK Parameters of GPR84 antagonist 3 in Male C57BL/6J mice[1]. IV (1 mg/kg) PO (10 mg/kg) half-life (h) 2.51 ± 6.55 CL (mL/min/kg) 38.9 ± 13.9 Vss (L/kg ) 7.24 ± 9.2 C0 (ng/mL) 394 ± 19.1 AUCall (ng/mL·h) 420 ± 12.5 1590 ± 18.7 Tmax (h) 1 Cmax (ng/mL) 402 ± 31.8 F (%) 36.8 ± 18.7 |
References |
[1]. Mahindra A, et al. Investigating the Structure-Activity Relationship of 1,2,4-Triazine G-Protein-Coupled Receptor 84 (GPR84) Antagonists. J Med Chem. 2022 Aug 10.
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Molecular Formula |
C29H27N5O
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Molecular Weight |
461.56
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CAS # |
2815263-05-7
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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: 100 mg/mL (216.66 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.42 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.1666 mL | 10.8328 mL | 21.6657 mL | |
5 mM | 0.4333 mL | 2.1666 mL | 4.3331 mL | |
10 mM | 0.2167 mL | 1.0833 mL | 2.1666 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.