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1mg |
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5mg |
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10mg |
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50mg |
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100mg |
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Other Sizes |
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ln Vivo |
The short-term memory impairments caused by scopolamine were effectively corrected by PHA-543613 (0.3 mg/kg) [2]. PHA-543613 (i.p. once; 4 and 12 mg/kg) decreases brain edema and behavioral abnormalities [3].
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Animal Protocol |
Animal/Disease Models: Male CD-1 mice (cerebral hemorrhage) ICH induction or sham surgery [3]
Doses: 4 and 12 mg/kg Route of Administration: intraperitoneal (ip) injection; 4 and 12 mg/kg; Results 1 hour after surgery: p-Akt increased, p-GSK-3 and CC3 expression diminished in the ipsilateral hemisphere, and neuronal cell death diminished in the area around the hematoma. Behavioral deficits and brain edema were diminished 72 hrs (hrs (hours)) after ICH. |
References |
[1]. Donn G Wishka, et al. Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide, an agonist of the alpha7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: synthesis and structure--activity relationship. J Med Chem. 2006 Jul 13;49(14):4425-36.
[2]. Nóra Bruszt, et al. Potentiation of cognitive enhancer effects of Alzheimer's disease medication memantine by alpha7 nicotinic acetylcholine receptor agonist PHA-543613 in the Morris water maze task. Psychopharmacology (Berl). 2021 Nov;238(11):3273-3281. [3]. Krafft PR, et al. α7 nicotinic acetylcholine receptor agonism confers neuroprotection through GSK-3β inhibition in a mouse model of intracerebral hemorrhage. Stroke. 2012 Mar;43(3):844-50. |
Molecular Formula |
C15H17N3O2
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Molecular Weight |
271.32
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Exact Mass |
271.1321
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CAS # |
478149-53-0
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Related CAS # |
PHA-543613 dihydrochloride;478148-58-2
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O=C(N[C@@H]1C2CCN(CC2)C1)C1=CC2C=COC=2C=N1.Cl
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Synonyms |
PHA543613; PHA 543613; PHA-543613
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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 : ~250 mg/mL (~921.46 mM)
H2O : ~100 mg/mL (~368.58 mM) |
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 3.6857 mL | 18.4284 mL | 36.8568 mL | |
5 mM | 0.7371 mL | 3.6857 mL | 7.3714 mL | |
10 mM | 0.3686 mL | 1.8428 mL | 3.6857 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.