| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
|
| Targets |
α7 nAChR 10.8 nM (Ki, for rat α7 receptors) α7 nAChR 16.7 nM (Ki, for human α7 receptors) 5-HT3 Receptor 150 nM (Ki)
|
|---|---|
| ln Vitro |
In PC12 cells, A-582941 (0.1-100 μM) prevents cell death brought on by NGF withdrawal[2]. The number of inhibitory postsynaptic potentials (IPSCs) increases by 260±70%, the sum of amplitudes by 220±30%, and the total of areas by 210±40% when A-582941 (100 nM) is administered[2]. In PC12 cells, A-582941 raises ERK1/2 phosphorylation with an EC50 of 95 nM[2].
|
| ln Vivo |
In freely moving rats, the medial prefrontal cortex (mPFCx) exhibits a moderate increase in ACh release when administered intraperitoneally (3 μM/kg) once daily for three days[2]. A-582941 (0.01-1.00 μM/kg, ip) enhances cAMP response element-binding protein (CREB) phosphorylation in the cingulate cortex of mice and ERK1/2 phosphorylation in the hippocampus in a dose-dependent manner[2]. In the mouse cingulate cortex, A-582941 (0.1-1.0 μM /kg, ip) causes dose-dependent increases in Ser-9 GSK-3β phosphorylation[2]. Following oral dosing (mouse 1.0, rat 6.2, dog 3.0, monkey 3.0 μM/kg), A-582941 has high oral bioavailability (mouse ~100%, rat 90%, dog 22%, monkey 50%) and Cmax (mouse 18, rat 114, dog 79, monkey 39 ng/mL)[2]. Following intravenous administration (mouse 1.0, rat 6.2, dog 0.5, monkey 0.5 μM/kg), A-582941 displays the terminal elimination half-lives (mouse 1.4, rat 1.5, dog 1.4, monkey 2.0 h), plasma clearance (mouse 7.9, rat 4.7, dog 5.3, monkey 1.6 L/h/kg), and volumes of distribution (mouse 11.4, rat 9.2, dog 7.9, monkey 3.9 L/kg).
|
| Animal Protocol |
Animal/Disease Models: Male SD (Sprague-Dawley) CD rats (250-275 g)[2]
Doses: 3 μM/kg Route of Administration: Ip one time/day for 3 days Experimental Results: Increased the releases of Ach. The effect remained stable after the second and third administration. |
| References |
|
| Molecular Formula |
C17H22CL2N4
|
|---|---|
| Molecular Weight |
353.29
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| Exact Mass |
280.169
|
| CAS # |
848591-90-2
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| PubChem CID |
44190553
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| Appearance |
Light yellow to yellow solid powder
|
| LogP |
2.144
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
21
|
| Complexity |
341
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
CN1C[C@@H]2CN(C[C@@H]2C1)C3=NN=C(C=C3)C4=CC=CC=C4
|
| InChi Key |
GTMRUYCIJSNXGB-GASCZTMLSA-N
|
| InChi Code |
InChI=1S/C17H20N4/c1-20-9-14-11-21(12-15(14)10-20)17-8-7-16(18-19-17)13-5-3-2-4-6-13/h2-8,14-15H,9-12H2,1H3/t14-,15+
|
| Chemical Name |
(3aR,6aS)-2-methyl-5-(6-phenylpyridazin-3-yl)-1,3,3a,4,6,6a-hexahydropyrrolo[3,4-c]pyrrole
|
| HS Tariff Code |
2934.99.9001
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 (283.05 mM)
|
|---|---|
| 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 | 2.8305 mL | 14.1527 mL | 28.3054 mL | |
| 5 mM | 0.5661 mL | 2.8305 mL | 5.6611 mL | |
| 10 mM | 0.2831 mL | 1.4153 mL | 2.8305 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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