| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
AA41612 targets OPN4 (melanopsin), a photopigment expressed in intrinsically photosensitive retinal ganglion cells (ipRGCs). Melanopsin is involved in non-image-forming visual responses, including circadian rhythm regulation and pupillary light reflex. AA41612 is a selective and competitive antagonist with an IC50 of 15.8 nM.
|
|---|---|
| ln Vitro |
In vitro, AA41612 has been shown to attenuate melanopsin photocurrent in a dose-dependent manner. The compound inhibits melanopsin photoresponses without affecting rod or cone function, indicating its selectivity for the melanopsin pathway. The IC50 for OPN4 antagonism is 15.8 nM.
|
| ln Vivo |
In vivo, AA41612 has been studied for its effects on melanopsin-mediated phototransduction. The compound is a potent antagonist of melanopsin-mediated phototransduction. Detailed in vivo data regarding dosage, administration routes, and specific efficacy endpoints are limited in the available literature.
|
| Enzyme Assay |
AA41612's receptor-binding activity has been characterized in cell-based systems. The compound is a selective and competitive OPN4 antagonist with an IC50 of 15.8 nM. Binding assays typically involve measuring the inhibition of melanopsin-mediated photocurrents in cells expressing OPN4.
|
| Cell Assay |
In vitro cell experiments with AA41612 typically use cells expressing melanopsin, such as HEK293 cells transfected with OPN4. Cells are treated with the compound at various concentrations, and photocurrents are measured using patch-clamp electrophysiology. The compound's effects on rod and cone function are assessed to confirm selectivity.
|
| Animal Protocol |
In vivo animal studies with AA41612 have been conducted using rodent models to study melanopsin-mediated phototransduction. The compound is typically administered via intravitreal or systemic routes. Detailed protocols regarding dosage, treatment duration, and specific animal models are not extensively reported in the available literature.
|
| ADME/Pharmacokinetics |
Pharmacokinetic data specific to AA41612 are limited in the available literature. The compound is a small molecule with a molecular weight of 324.22 and a formula of C₁₂H₁₅Cl₂NO₃S. Further pharmacokinetic studies are needed to fully characterize its absorption, distribution, metabolism, and excretion properties.
|
| Toxicity/Toxicokinetics |
Toxicological data for AA41612 are limited. As a research compound, it is intended for laboratory use only and not for human consumption. The compound should be handled under standard laboratory safety practices with appropriate precautions.
|
| Additional Infomation |
AA41612 is a novel antagonist of melanopsin-mediated phototransduction. It has a molecular weight of 324.22 and a formula of C₁₂H₁₅Cl₂NO₃S. The compound is stored at -20°C and is available with a purity of ≥98%. It is a valuable tool for studying melanopsin function and non-image-forming visual responses.
|
| Molecular Formula |
C12H15NO3SCL2
|
|---|---|
| Molecular Weight |
324.223
|
| Exact Mass |
323.015
|
| Elemental Analysis |
C, 44.46; H, 4.66; Cl, 21.87; N, 4.32; O, 14.80; S, 9.89
|
| CAS # |
433690-62-1
|
| PubChem CID |
4528045
|
| Appearance |
Solid powder
|
| LogP |
4.195
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
19
|
| Complexity |
392
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=CC(Cl)=C(S(N2CCCCC2)(=O)=O)C=C1Cl
|
| InChi Key |
FEMVYIQDVGQFBA-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C12H15Cl2NO3S/c1-18-11-7-10(14)12(8-9(11)13)19(16,17)15-5-3-2-4-6-15/h7-8H,2-6H2,1H3
|
| Chemical Name |
1-(2,5-dichloro-4-methoxyphenyl)sulfonylpiperidine
|
| Synonyms |
AA41612; AA-41612; AA 41612;
|
| 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: 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~771.08 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 | 3.0843 mL | 15.4216 mL | 30.8433 mL | |
| 5 mM | 0.6169 mL | 3.0843 mL | 6.1687 mL | |
| 10 mM | 0.3084 mL | 1.5422 mL | 3.0843 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
