| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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Ponalrestat (MK-538; ICI 128436; Statil) is a novel and potent aldose reductase inhibitor which inhibits the conversion of glucose to sorbitol. Ponalrestat inhibits cachexia syndrome induced by colon26 adenocarcinoma in mice. Ponalrestat activates lipoprotein lipase (LPL) activity in the adipose tissue and alleviates the cachectic symptoms induced by B16 melanoma in mice. Ponalrestat is effective in the attenuation of the cachectic symptoms induced by human melanomas G361 and SEKI in nude mice, suggesting that ponalrestat has a potential usefulness for the treatment of cancer cachexia.
| ln Vitro |
In cultured endometrium and endometrial explants, Ponalrestat (ICI 128436; 1, 10, 100 μM; 6 hours) decreases PGF2α production in response to IL-1 [2].
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| ln Vivo |
Pomalrestat (ICI 128436; 10, 50 mg/kg; sidewall; daily; 8 weeks) effectively inhibits aldose reductase and decreases the accumulation of sorbitol [3].
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| Animal Protocol |
Animal/Disease Models: Adult female SD (SD (Sprague-Dawley)) rats [3]
Doses: 10, 50 mg/kg Route of Administration: oral; daily; 8-week Experimental Results: sorbitol accumulation diminished. |
| References |
[1]. Ward WH, et al. Ponalrestat: a potent and specific inhibitor of aldose reductase. Biochem Pharmacol. 1990 Jan 15;39(2):337-46.
[2]. Bresson E, et al. The human aldose reductase AKR1B1 qualifies as the primary prostaglandin F synthase in the endometrium. J Clin Endocrinol Metab. 2011 Jan;96(1):210-9. [3]. Calcutt NA, et al. Prevention of sensory disorders in diabetic Sprague-Dawley rats by aldose reductase inhibition or treatment with ciliary neurotrophic factor. Diabetologia. 2004 Apr;47(4):718-24. |
| Molecular Formula |
C17H11N2O3FBR-
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|---|---|
| Molecular Weight |
390.18324
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| CAS # |
72702-95-5
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| SMILES |
O=C(O)CC1=NN(CC2=CC=C(Br)C=C2F)C(C3=C1C=CC=C3)=O
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| InChi Key |
LKBFFDOJUKLQNY-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
2-(3-(4-bromo-2-fluorobenzyl)-4-oxo-3,4-dihydrophthalazin-1-yl)acetic acid
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| Synonyms |
Ponalrestat, ICI-128436; ICI 128436; ICI128436; MK-538; MK 538; MK538. trade name: Statil; Statyl.
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~159.77 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.32 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5629 mL | 12.8146 mL | 25.6292 mL | |
| 5 mM | 0.5126 mL | 2.5629 mL | 5.1258 mL | |
| 10 mM | 0.2563 mL | 1.2815 mL | 2.5629 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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