AA41612
Based on 1 Customer Validation
AA41612 is a melanopsin (Opn4) inhibitor with an IC50 of 15.8 nM, a Ki of 0.43 nM, and a Kd of 0.28 nM. AA41612 competes with retinal for binding to melanopsin, blocks melanopsin activation, and inhibits melanopsin-mediated phototransduction processes without affecting rod- and cone-mediated responses. AA41612 attenuates light-induced melanopsin photocurrents, reduces light-induced cytoplasmic calcium elevation, and weakens high-irradiance pupillary light reflex in mice with induced classical photoreceptor degeneration. AA41612 can be used in studies related to migraine and photophobia.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.78%
- CAS 番号: 433690-62-1
- 分子式: C12H15Cl2NO3S
- 分子量:324.23
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
AA41612 (10-100 nM; 3 min) inhibits mouse melanopsin-mediated photocurrent in Xenopus oocytes with an IC50 of 20 nM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (adult, 8-12 weeks, pharmacologically induced classical photoreceptor degeneration via MNU and NaIO3 injection)[2]
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Dosage:10 mg/kg
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Administration:i.p.; single dose
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Result:Reduced pupillary light reflex (PLR) at high irradiances (> 103 μW/cm2) by < 15% at the highest tested irradiance (2.8×104 μW/cm2).
Showed a significant difference between groups via two-way ANOVA with repeated measures.
Confirmed significantly lower PLR at irradiances > 103 μW/cm2 compared to mice injected with only MNU and NaIO3 via post-hoc testing.
化学情報
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CAS 番号 433690-62-1
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性状 Solid
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分子量 324.23
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分子式 C12H15Cl2NO3S
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Color White to off-white
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SMILES
O=S(N1CCCCC1)(C2=CC(Cl)=C(OC)C=C2Cl)=O
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 250 mg/mL (771.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (293 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1].
Jones KA, et al. Small-molecule antagonists of melanopsin-mediated phototransduction. Nat Chem Biol. 2013 Oct;9(10):630-5.
[Content Brief]
[2].
Jain V, et al. Classical Photoreceptors Are Primarily Responsible for the Pupillary Light Reflex in Mouse. PLoS One. 2016 Jun 13;11(6):e0157226.
[Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0842 mL | 15.4212 mL | 30.8423 mL | 77.1058 mL |
| 5 mM | 0.6168 mL | 3.0842 mL | 6.1685 mL | 15.4212 mL | |
| 10 mM | 0.3084 mL | 1.5421 mL | 3.0842 mL | 7.7106 mL | |
| 15 mM | 0.2056 mL | 1.0281 mL | 2.0562 mL | 5.1404 mL | |
| 20 mM | 0.1542 mL | 0.7711 mL | 1.5421 mL | 3.8553 mL | |
| 25 mM | 0.1234 mL | 0.6168 mL | 1.2337 mL | 3.0842 mL | |
| 30 mM | 0.1028 mL | 0.5140 mL | 1.0281 mL | 2.5702 mL | |
| 40 mM | 0.0771 mL | 0.3855 mL | 0.7711 mL | 1.9276 mL | |
| 50 mM | 0.0617 mL | 0.3084 mL | 0.6168 mL | 1.5421 mL | |
| 60 mM | 0.0514 mL | 0.2570 mL | 0.5140 mL | 1.2851 mL | |
| 80 mM | 0.0386 mL | 0.1928 mL | 0.3855 mL | 0.9638 mL | |
| 100 mM | 0.0308 mL | 0.1542 mL | 0.3084 mL | 0.7711 mL |
AA41612 関連分類
HY-124157 関連分類
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