For research use only. Not for therapeutic Use.
Ponalrestat (Cat No.:I008825 ) is an orally active, selective, and noncompetitive aldose reductase; aKR1B1; aLR ) inhibitor. Ponalrestat can selectively inhibit ALR2 with a Ki value of 7.7 nM and a Ki value of 60 μM for ALR1. Ponalrestat inhibits the conversion of glucose to sorbitol.
| Catalog Number | I008825 |
| CAS Number | 72702-95-5 |
| Synonyms | Ponalrestat, ICI-128436; ICI 128436; ICI128436; MK-538; MK 538; MK538. Brand name: Statil; Statyl.;2-(3-(4-bromo-2-fluorobenzyl)-4-oxo-3,4-dihydrophthalazin-1-yl)acetic acid |
| Molecular Formula | C17H12BrFN2O3 |
| Purity | ≥95% |
| Target | Aldose Reductase |
| Solubility | Soluble in DMSO, not in water |
| Storage | Store at RT |
| IUPAC Name | 2-[3-[(4-bromo-2-fluorophenyl)methyl]-4-oxophthalazin-1-yl]acetic acid |
| InChI | InChI=1S/C17H12BrFN2O3/c18-11-6-5-10(14(19)7-11)9-21-17(24)13-4-2-1-3-12(13)15(20-21)8-16(22)23/h1-7H,8-9H2,(H,22,23) |
| InChIKey | LKBFFDOJUKLQNY-UHFFFAOYSA-N |
| SMILES | C1=CC=C2C(=C1)C(=NN(C2=O)CC3=C(C=C(C=C3)Br)F)CC(=O)O |
| Reference | </br>1:Ponalrestat, an aldose reductase inhibitor, inhibits cachexia syndrome induced by colon26 adenocarcinoma in mice. Kawamura I, Lacey E, Yamamoto N, Sakai F, Takeshita S, Inami M, Nishigaki F, Naoe Y, Tsujimoto S, Manda T, Shimomura K, Goto T.Anticancer Res. 1999 Sep-Oct;19(5B):4105-11. PMID: 10628361 </br>2:Ponalrestat, an aldose reductase inhibitor, inhibits cachexia syndrome in nude mice bearing human melanomas G361 and SEKI. Kawamura I, Lacey E, Inami M, Nishigaki F, Naoe Y, Tsujimoto S, Manda T, Goto T.Anticancer Res. 1999 Sep-Oct;19(5B):4091-7. PMID: 10628359 </br>3:Activation of lipoprotein lipase and inhibition of B16 melanoma-induced cachexia in mice by ponalrestat, an aldose reductase inhibitor. Kawamura I, Yamamoto N, Sakai F, Yamazaki H, Naoe Y, Inami M, Manda T, Shimomura K.Anticancer Res. 1999 Jan-Feb;19(1A):341-8. PMID: 10226565 </br>4:Progression rates of diabetic neuropathy in placebo patients in an 18-month clinical trial. Ponalrestat Study Group. Laudadio C, Sima AA.J Diabetes Complications. 1998 May-Jun;12(3):121-7. PMID: 9618066 </br>5:The effects of aldose reductase inhibition with ponalrestat on changes in vascular function in streptozotocin diabetic rats. Otter DJ, Chess-Williams R.Br J Pharmacol. 1994 Oct;113(2):576-80. PMID: 7834210 Free PMC Article</br>6:Endothelial function in the isolated perfused mesentery and aortae of rats with streptozotocin-induced diabetes: effect of treatment with the aldose reductase inhibitor, ponalrestat. Taylor PD, Wickenden AD, Mirrlees DJ, Poston L.Br J Pharmacol. 1994 Jan;111(1):42-8. PMID: 8012723 Free PMC Article</br>7:Aldose reductase inhibition by ponalrestat (statil) does not prevent proteinuria in long-term diabetic rats. Reddi AS, Jyothirmayi GN.J Diabetes Complications. 1993 Oct-Dec;7(4):233-40. PMID: 8219366 </br>8:Effects of ponalrestat, an aldose reductase inhibitor, on neutrophil killing of Escherichia coli and autonomic function in patients with diabetes mellitus. Boland OM, Blackwell CC, Clarke BF, Ewing DJ.Diabetes. 1993 Feb;42(2):336-40. PMID: 8425670 </br>9:Dissociation between biochemical and functional effects of the aldose reductase inhibitor, ponalrestat, on peripheral nerve in diabetic rats. Cameron NE, Cotter MA.Br J Pharmacol. 1992 Dec;107(4):939-44. PMID: 1467842 Free PMC Article</br>10:A 12-month randomized controlled study of the aldose reductase inhibitor ponalrestat in patients with chronic symptomatic diabetic neuropathy. Krentz AJ, Honigsberger L, Ellis SH, Hardman M, Nattrass M.Diabet Med. 1992 Jun;9(5):463-8. PMID: 1611835 |
