2. Metabolic Enzyme/Protease
  3. Aldose Reductase
  4. Ranirestat

Ranirestat  (Synonyms: AS-3201)

製品番号: HY-15314 純度: 98.32%
COA 取扱説明書

Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC50s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a Ki of 0.38 nM for recombinant human AR. Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinas.

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Ranirestat 構造式

Ranirestat 構造式

CAS 番号 : 147254-64-6

容量 価格（税別） 在庫状況 数量
Solution
10 mM * 1 mL in DMSO USD 343 在庫あり
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 343 在庫あり
Estimated Time of Arrival: December 31
Solid
5 mg USD 312 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 540 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 1440 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 2400 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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製品説明

Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC50s of 11 nM and 15 nM for rat lens AR and recombinant human AR, respectively, and a Ki of 0.38 nM for recombinant human AR. Ranirestat has the potential for diabetic sensorimotor polyneuropathy treatment. Ranirestat also has a neuroprotective effect on diabetic retinas[1][2].

IC50 & Target

IC50: 11 nM (Rat lens aldose reductase) and 15 nM (Recombinant humanaldose reductase)[1]
Ki: 0.38 nM (Recombinant humanaldose reductase)[1]
体外実験

Ranirestat concentration-dependently inhibits sorbitol accumulation in rat erythrocytes and sciatic nerves incubated in the high concentration (500 mg/dl) of glucose. The potency of Ranirestat inhibition of sorbitol accumulation is similar between rat erythrocytes and sciatic nerves with IC50 values of 0.010 μM and 0.041 μM, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内実験

Ranirestat (0.03-1.0 mg/kg; oral administration; once daily; for 3 weeks; male STD-Wistar rats) treatment dose-dependently decreases the elevated sorbitol and fructose levels in the rat sciatic nerves without affecting blood glucose level. Ranirestat also improves the STZ-induced decrease in motor nerve conduction velocity (MNCV) in a dose-dependent manner[1].

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

Animal Model: Male STD-Wistar rats aged about (12-week-old; 260-290 g) injected with Streptozotocin (STZ)[1]
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg
Administration: Oral administration; once daily; for 3 weeks
Result: Dose-dependently decreased the elevated sorbitol and fructose levels in the rat sciatic nerves without affecting blood glucose level.
臨床実験
分子量

420.19

Appearance

Solid

分子式

C17H11BrFN3O4
CAS 番号
SMILES

O=C(N1CC2=CC=C(Br)C=C2F)C3=CC=CN3[[email protected]]4(C(NC(C4)=O)=O)C1=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 50 mg/mL (118.99 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3799 mL 11.8994 mL 23.7988 mL
5 mM 0.4760 mL 2.3799 mL 4.7598 mL
10 mM 0.2380 mL 1.1899 mL 2.3799 mL
*Please refer to the solubility information to select the appropriate solvent.
体内:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.95 mM); Clear solution

*All of the co-solvents are available by MCE.
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参考文献
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Keywords:

Ranirestat147254-64-6AS-3201AS3201AS 3201Aldose ReductaseStereospecificallysuccinimideAKR1BR-isomerdiabeticsensorimotorpolyneuropathysorbitolfructoseneuroprotectiveInhibitorinhibitorinhibit

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製品番号:
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