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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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GPR34 modulator 1 is a novel and potent antagonist of GPR34 (G Protein-Coupled Receptor 34) which is a Protein associated with Congenital Stationary Night Blindness and Alzheimer Disease.
ln Vitro |
GPR34 is a G protein-coupled receptor that has positive effects on mast cells when combined with nerve growth factor. Its endogenous ligand acts on mast cells or glycinin to increase mast cell histamine-releasing activity. Action Histamine is released by a lipid with this property, such as lysophosphatidylserine. GPR34 antagonists are useful in the treatment of edema, hyperacidity, immunological disorders, histamine production, etc. [1].
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References |
[1]. Fumio Ito, et al. Agent for controlling function of gpr34 receptor. WO2006088246 A1.
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Molecular Formula |
C31H26CLNO4
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Molecular Weight |
511.9954
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CAS # |
907952-06-1
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SMILES |
ClC1C([H])=C([H])C(=C([H])C=1[H])C1C([H])=C([H])C(=C([H])C=1[H])/C(/[H])=C(\[H])/C(N([H])C([H])(C(=O)O[H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])OC([H])([H])C1C([H])=C([H])C([H])=C([H])C=1[H])=O
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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 : ~83.33 mg/mL (~162.75 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.06 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
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 (4.06 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 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 | 1.9531 mL | 9.7656 mL | 19.5312 mL | |
5 mM | 0.3906 mL | 1.9531 mL | 3.9062 mL | |
10 mM | 0.1953 mL | 0.9766 mL | 1.9531 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.