Size | Price | Stock | Qty |
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5mg |
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10mg |
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Other Sizes |
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ln Vitro |
Comparing SSR180711 hydrochloride to human n-AChR isoforms α4β2, α3β2, α3β4, and α1β1γδ, it is selective for the α7 receptor subtype (IC50>5 μM). SSR180711 hydrochloride (10 μM) does not inhibit neurotransmitters, peptide receptors, or ion channels by less than 50% [1]. With an EC50 value of 4.4 μM (2.5–7.8 μM), SSR180711 hydrochloride (0.01–1000 μM) is a strong partial agonist of human α7 n-AChR produced in Xenopus oocytes or GH4C1 cells, eliciting a characteristic concentration-dependent inward current[1].
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ln Vivo |
When taken orally, SSR180711 hydrochloride enters the brain quickly (ID50=8 mg/kg). In mouse brain, selective [3H]α-BTX binding is dose-dependently inhibited by SSR180711 hydrochloride (ID50 8.3 and 7.5 mg/kg for oral and intraperitoneal injection, respectively) [1]. In the hippocampus and prefrontal cortex of freely moving rats, SSR180711 hydrochloride (1–10 mg/kg intraperitoneally; 10–30 mg/kg orally) increases extracellular acetylcholine (ACh) levels in a dose-dependent manner [1]. Dosage-dependently, SSR180711 hydrochloride (0.1, 0.3, and 1 mg/kg; iv) raises emissivity [1].
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References |
Molecular Formula |
C14H18BRCLN2O2
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Molecular Weight |
361.6619
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Exact Mass |
360.024
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CAS # |
446031-79-4
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PubChem CID |
9928899
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Appearance |
White to off-white solid powder
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Hydrogen Bond Donor Count |
1
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Hydrogen Bond Acceptor Count |
3
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Rotatable Bond Count |
2
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Heavy Atom Count |
20
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Complexity |
323
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Defined Atom Stereocenter Count |
0
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SMILES |
BrC1C([H])=C([H])C(=C([H])C=1[H])OC(N1C([H])([H])C([H])([H])N2C([H])([H])C([H])([H])C1([H])C([H])([H])C2([H])[H])=O.Cl[H]
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InChi Key |
YNBXNVUZXFMNSJ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C14H17BrN2O2.ClH/c15-11-1-3-13(4-2-11)19-14(18)17-10-9-16-7-5-12(17)6-8-16;/h1-4,12H,5-10H2;1H
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Chemical Name |
(4-bromophenyl) 1,4-diazabicyclo[3.2.2]nonane-4-carboxylate;hydrochloride
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Synonyms |
SSR-180711C; SSR-180711A; SSR-180711
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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 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)
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Solubility (In Vitro) |
DMSO : ~50 mg/mL (~138.25 mM)
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.75 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.
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 (5.75 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 20.8 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. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (5.75 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 | 2.7650 mL | 13.8251 mL | 27.6503 mL | |
5 mM | 0.5530 mL | 2.7650 mL | 5.5301 mL | |
10 mM | 0.2765 mL | 1.3825 mL | 2.7650 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.