[CAS NO. 147254-64-6] Ranirestat

Name: Ranirestat
Brand: Arctom Scientific
SKU: AS265786

Ships within

Stock

Price

Qty

Total

$0.00

Please click "REQUEST A QUOTE" button if you need other sizes or custom synthesis

request a quote

If there is no stock, or you need other sizes or custom synthesis, please:

PRODUCTS SPECIFICATIONS [147254-64-6]

Distributor

Catalog

AS265786

Brand

Arctom Scientific

CAS

147254-64-6

DESCRIPTION [147254-64-6]

Overview

MDL	-
Molecular Weight	420.19
Molecular Formula	C17H11BrFN3O4
SMILES	O=C(N1CC2=CC=C(Br)C=C2F)C3=CC=CN3[C@]4(C(NC(C4)=O)=O)C1=O

For research use only. We do not sell to patients.

Summary

Ranirestat (AS-3201) potent and orally active aldose reductase (AR) inhibitor with IC ₅₀ s of 11 nM and 15 nM for rat lens AR and recombinant human AR , respectively, and a K _i 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]

In Vitro

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 IC ₅₀ 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.

In Vivo

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00101426	Sumitomo Pharma Co., Ltd.	Diabetic Neuropathy	October 2004	Phase 3
NCT00927914	Eisai Inc.	Mild to Moderate Diabetic Sensorimotor Polyneuropathy	July 2009	Phase 2\|Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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.

In Vivo:

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.

References

Synonyms

Spiro[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2′H)-tetrone, 2′-[(4-bromo-2-fluorophenyl)methyl]-, (3R)-

Spiro[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2′H)-tetrone, 2′-[(4-bromo-2-fluorophenyl)methyl]-, (-)-

Spiro[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2′H)-tetrone, 2′-[(4-bromo-2-fluorophenyl)methyl]-, (3′R)-

(3R)-2′-[(4-Bromo-2-fluorophenyl)methyl]spiro[pyrrolidine-3,4′(1′H)-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2′H)-tetrone

AS 3201

Ranirestat

(3R)-2′-(4-Bromo-2-fluorobenzyl)-1′,2′,3′,4′-tetrahydrospiro[pyrrolidine-3,4′-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5-tetraone

(3R)-2′-(4-Bromo-2-fluorobenzyl)spiro[pyrrolidine-3,4′-1′H-pyrrolo[1,2-a]pyrazine]-1′,2,3′,5(2′H)-tetraone