2. Metabolic Enzyme/Protease
  3. RPE65
  4. Emixustat hydrochloride

Emixustat hydrochloride  (Synonyms: ACU-4429 hydrochloride)

製品番号: HY-19720A 純度: 99.29%
COA 取扱説明書 Technical Support

Emixustat (ACU-4429) hydrochloride is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat hydrochloride is also a visual cycle modulator, capable of regulating visual cycle activity by inhibiting retinol isomerization, and holds potential for studying vision disorders such as age-related macular degeneration (AMD).

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Emixustat hydrochloride

Emixustat hydrochloride 構造式

CAS 番号 : 1141934-97-5

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 165 在庫あり
Solution
10 mM * 1 mL in DMSO USD 165 在庫あり
Solid
2 mg $100 在庫あり
5 mg $150 在庫あり
10 mg $240 在庫あり
25 mg $420 在庫あり
50 mg $595 在庫あり
100 mg $950 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Emixustat hydrochloride 関連抗体

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製品説明

Emixustat (ACU-4429) hydrochloride is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat hydrochloride is also a visual cycle modulator, capable of regulating visual cycle activity by inhibiting retinol isomerization, and holds potential for studying vision disorders such as age-related macular degeneration (AMD)[1][2][3][4].

IC50 & Target

IC50: 4.4 nM (Retinal Pigment Epithelium 65-kDa protein (RPE65))[4]
体外実験

Emixustat (0.1 nM - 10 μM, 1 h) concentration-dependently reduces the production of 11-cis-retinol, thereby inhibiting RPE65 activity[4].

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

Emixustat hydrochloride 関連抗体
体内実験

Emixustat (1-10 mg/kg, oral administration, single dose, or twice daily for 6 days; 1 mg/kg, i.p., measurement after 30-60 minutes) reduced cation influx and oxygen consumption in the retinas of brown Norway rats under dark adaptation conditions[3].
Emixustat (0.03-3.0 mg/kg, intravenous injection, once daily for 5 days) inhibits neovascularization and protects the retina in the oxygen-induced retinopathy mouse model[4].

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

Animal Model: Brown norway rats (200-300 g, 3 months old)[3]
Dosage: 1, 5 or 10 mg/kg
Administration: Oral gavage (p.o.), single dose (1, 10 mg/kg), 2 hours followed by 4 hours of dark adaptation, or twice a day for 6 days (5 mg/kg)
Result: Reduced the conductance of the retinal cation channels after dark adaptation.
Animal Model: Brown norway rats (200-300 g, 3 months old)[3]
Dosage: 1 mg/kg
Administration: Intravenous injection (i.v.), retinal PO2 was measured 30-60 min later
Result: Reduced the oxygen consumption during dark adaptation.
Animal Model: Oxygen-induced retinopathy (OIR) mice model (BALB/c and 129/Sv / C57BL/6 mixed background)
Dosage: 0.03, 0.1, 0.3, 1.0, 3.0 mg/kg
Administration: Intravenous injection (i.v.), once daily for 5 days
Result: Dose-dependently reduced retinal neovascularization.
臨床実験
分子量

299.84

分子式

C16H26ClNO2
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O[C@H](CCN)C1=CC(OCC2CCCCC2)=CC=C1.[H]Cl
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶剤 & 溶解度
体外: 

DMSO : 44 mg/mL (146.74 mM; Need ultrasonic and warming; 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 3.3351 mL 16.6756 mL 33.3511 mL
5 mM 0.6670 mL 3.3351 mL 6.6702 mL
10 mM 0.3335 mL 1.6676 mL 3.3351 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

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In Vivo Dissolution Calculator
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純度とドキュメンテーション
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 (sealed storage, away from moisture). 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 3.3351 mL 16.6756 mL 33.3511 mL 83.3778 mL
5 mM 0.6670 mL 3.3351 mL 6.6702 mL 16.6756 mL
10 mM 0.3335 mL 1.6676 mL 3.3351 mL 8.3378 mL
15 mM 0.2223 mL 1.1117 mL 2.2234 mL 5.5585 mL
20 mM 0.1668 mL 0.8338 mL 1.6676 mL 4.1689 mL
25 mM 0.1334 mL 0.6670 mL 1.3340 mL 3.3351 mL
30 mM 0.1112 mL 0.5559 mL 1.1117 mL 2.7793 mL
40 mM 0.0834 mL 0.4169 mL 0.8338 mL 2.0844 mL
50 mM 0.0667 mL 0.3335 mL 0.6670 mL 1.6676 mL
60 mM 0.0556 mL 0.2779 mL 0.5559 mL 1.3896 mL
80 mM 0.0417 mL 0.2084 mL 0.4169 mL 1.0422 mL
100 mM 0.0334 mL 0.1668 mL 0.3335 mL 0.8338 mL
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Emixustat hydrochloride Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Emixustat1141934-97-5ACU-4429ACU4429ACU 4429RPE65Retinal pigment epithelium 65 kDa proteinOxygen-induced retinopathy (OIR) mice modelBrown norway ratsage-related macular degenerationInhibitorinhibitorinhibit

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製品名:
Emixustat hydrochloride
製品番号:
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