| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
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| Targets |
SSR-180711A targets the α7 nicotinic acetylcholine receptor (α7 n-AChR), a ligand-gated ion channel involved in cognitive function, memory, and neuroprotection. It is a selective and reversible partial agonist. SSR-180711A has Ki values of 22 nM for rat α7 n-AChRs and 14 nM for human α7 n-AChRs.
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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].
SSR-180711A is a selective α7 n-AChR partial agonist. It has Ki values of 22 nM for rat α7 n-AChRs and 14 nM for human α7 n-AChRs. The compound has IC50 values of 30 nM for rat α7 n-AChRs and 18 nM for human α7 n-AChRs. As a partial agonist, it activates α7 n-AChRs to a lesser extent than full agonists. |
| 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].
SSR-180711A is orally bioactive. It has been studied for its potential in treating neurodegenerative and cognitive disorders, including schizophrenia. Specific animal model data and dosing regimens are not extensively detailed in standard reference sources. |
| Enzyme Assay |
The binding affinity of SSR-180711A to α7 n-AChRs can be assessed using radioligand binding assays with membrane preparations from cells expressing recombinant rat or human α7 n-AChRs. Competition binding experiments are performed with increasing concentrations of SSR-180711A against a fixed concentration of a radiolabeled α7 n-AChR ligand. Ki values are calculated from competition curves.
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| Cell Assay |
The functional activity of SSR-180711A at α7 n-AChRs is evaluated in vitro using cells expressing recombinant α7 n-AChRs or in neuronal preparations. Cells are treated with increasing concentrations of SSR-180711A, and α7 n-AChR-mediated calcium influx is measured using calcium-sensitive fluorescent dyes. The EC50 for receptor activation is determined.
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| Animal Protocol |
SSR-180711A is administered orally to animal models of cognitive disorders. In rodent models of cognitive impairment (e.g., scopolamine-induced amnesia, aged rats, or models of schizophrenia), SSR-180711A is given at various doses via oral gavage. Cognitive function is assessed using behavioral tests such as the Morris water maze, novel object recognition, or prepulse inhibition.
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| ADME/Pharmacokinetics |
SSR-180711A HCl has a molecular formula of C14H18BrClN2O2 and a molecular weight of 361.66. It is orally bioactive. Specific pharmacokinetic parameters such as half-life, bioavailability, and plasma protein binding are not extensively detailed in standard reference sources.
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| Toxicity/Toxicokinetics |
The toxicity profile of SSR-180711A is not extensively documented. As an α7 n-AChR partial agonist, potential adverse effects may include those related to nicotinic receptor activation, such as gastrointestinal effects. Specific LD50 values and organ-specific toxicity data are not readily available.
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| References | |
| Additional Infomation |
SSR-180711A HCl (CAS# 446031-79-4) is also known as SSR-180711C HCl. It is a selective α7 nicotinic acetylcholine receptor partial agonist. SSR-180711A is used for the study of neurodegenerative and cognitive disorders. It is orally bioactive and reversible.
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| 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.
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