1. GPCR/G Protein
  2. Melanopsin Receptor
  3. AA41612

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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AA41612

AA41612 構造式

CAS 番号 : 433690-62-1

容量 価格(税別) 在庫状況 数量
5 mg $90 在庫あり
10 mg $140 在庫あり
25 mg $250 在庫あり
50 mg $400 在庫あり
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200 mg   お問い合わせ  

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製品説明

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[1][2].

体外実験

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.

体内実験

AA41612 (10 mg/kg; i.p.; single dose) reduces the minor melanopsin-mediated component of high-irradiance pupillary light reflex by less than 15% at the highest tested irradiance in adult mice with induced classical photoreceptor degeneration[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (adult, 8-12 weeks, pharmacologically induced classical photoreceptor degeneration via MNU and NaIO3 injection)[2]
Dosage: 10 mg/kg
Administration: i.p.; single dose
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.
分子量

324.23

分子式

C12H15Cl2NO3S

CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=S(N1CCCCC1)(C2=CC(Cl)=C(OC)C=C2Cl)=O

輸送条件

Room temperature in continental US; may vary elsewhere.

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
体外: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.0842 mL 15.4212 mL 30.8423 mL
5 mM 0.6168 mL 3.0842 mL 6.1685 mL
10 mM 0.3084 mL 1.5421 mL 3.0842 mL
View the 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.

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純度とドキュメンテーション

純度: 99.78%

参考文献

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
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製品名:
AA41612
製品番号:
HY-124157
数量:
MCE 日本正規代理店: