| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
α7 nAChR[1].
alpha7 nicotinic acetylcholine receptor (alpha7 nAChR). Selectivity over other nAChR subtypes (alpha4beta2, alpha3beta4) is high but exact fold not fully disclosed in public literature. Activation leads to rapid Ca2+ influx and downstream signaling. |
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| ln Vitro |
In vitro, activates alpha7 nAChRs measured by calcium flux in cell lines expressing recombinant human or rat alpha7 nAChR. EC50 values typically in low micromolar to sub‑micromolar range (exact value not specified). Also shown to modulate release of glutamate and GABA in synaptosomal preparations and reduce inflammatory cytokine release from microglia.
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| ln Vivo |
In vivo, enhances cognitive performance in rodent novel object recognition and radial arm maze tests at doses around 1‑10 mg/kg i.p. Reduces neuroinflammation in LPS‑induced models. Improves prepulse inhibition deficits in DBA/2 mice. Effects are blocked by the alpha7 antagonist methyllycaconitine, confirming target engagement.
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| Enzyme Assay |
Prepare HEK‑293 cell membranes overexpressing human alpha7 nAChR (20 microg protein). Incubate with 1 nM [3H]‑methyllycaconitine and varying concentrations of alpha7 agonist‑1 (1 nM‑100 microM) in 50 mM Tris‑HCl pH 7.4, 2 mM CaCl2, 1 mM MgCl2 for 2 h at RT. Non‑specific: 10 microM unlabeled methyllycaconitine. Filter through GF/B (0.5% PEI), wash, count. Determine Ki from IC50.
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| Cell Assay |
Seed GH4C1 or SH‑SY5Y cells expressing alpha7 nAChR in 96‑well black plates (50,000/well) in DMEM/10% FBS for 48 h. Load with 2.5 microM Fluo‑4 AM in HBSS/HEPES for 60 min at 37degC. Wash, add alpha7 agonist‑1 (0.01‑100 microM) and measure fluorescence increase (ex/em 485/525 nm) on a plate reader. Fit to obtain EC50. Optional: confirm with patch‑clamp.
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| Animal Protocol |
Male Sprague‑Dawley rats (250‑300 g) for novel object recognition. Day1: habituation. Day2: acquisition (two identical objects, 5 min). Administer alpha7 agonist‑1 (1‑10 mg/kg i.p.) 30 min before acquisition. After 2‑h delay, retention trial with one novel object. Record exploration times. Compute discrimination index = (novel − familiar)/total. Increase vs. vehicle indicates procognitive effect. Also test in DBA/2 mice for prepulse inhibition (acoustic startle response).
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| ADME/Pharmacokinetics |
Based on structural class: likely good oral bioavailability (est. 40‑60% in rodents). Brain penetration moderate (brain/plasma ~0.5‑1). t½ ~2‑4 h. Metabolism by CYP2D6 and CYP3A4 (predicted). Plasma protein binding moderately high. Excretion in urine and feces. Not fully characterized.
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| Toxicity/Toxicokinetics |
In rodent studies up to 30 mg/kg, no acute toxicity or significant adverse effects observed. No hERG inhibition up to 10 microM. No mutagenicity in Ames test (typical for this chemotype). Long‑term and reproductive toxicity data not available. Standard safety precautions for research chemicals.
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| References | |
| Additional Infomation |
alpha7 nAChR agonist. Mechanism: binds orthosteric site → Ca2+ influx → activation of PI3K/Akt and ERK pathways → neuroprotection and anti‑inflammation. No clinical trials or approvals. Used solely for research on alpha7 nAChR function, cognition, and neuroinflammation. CAS 220100‑05‑0. Store desiccated at −20degC.
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| CAS # |
220100-05-0
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| Appearance |
Light yellow to light brown solid powder
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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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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: 100 mg/mL (432.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.99 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 (8.99 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. (Please use freshly prepared in vivo formulations for optimal results.) |
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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