U83836E

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 561837

CAS#: 137018-55-4

Description: U83836E is a potent lipid peroxidation (LP) inhibitor. It has been shown to suppress oxidative stress and activate PKC, improving neurodegeneration in diabetic retinopathy (DR).

Chemical Structure

img
U83836E
CAS# 137018-55-4
Instruction

Theoretical Analysis

MedKoo Cat#: 561837
Name: U83836E
CAS#: 137018-55-4
Chemical Formula: C30H46Cl2N6O2
Exact Mass: 592.31
Molecular Weight: 593.630
Elemental Analysis: C, 60.70; H, 7.81; Cl, 11.94; N, 14.16; O, 5.39

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

Synonym: U83836E; U-83836-E; U 83836 E; PNU-83836E; PNU 83836 E; PNU83836E; PNU 83836E;

IUPAC/Chemical Name: (2R)-2-[[4-(2,6-Dipyrrolidin-1-ylpyrimidin-4-yl)piperazin-1-yl]methyl]-2,5,7,8-tetramethyl-3,4-dihydrochromen-6-ol;dihydrochloride

InChi Key: KJGXSMZHYBXPIS-ZHXNKHNVSA-N

InChi Code: InChI=1S/C30H44N6O2.2ClH/c1-21-22(2)28-24(23(3)27(21)37)9-10-30(4,38-28)20-33-15-17-35(18-16-33)26-19-25(34-11-5-6-12-34)31-29(32-26)36-13-7-8-14-36;;/h19,37H,5-18,20H2,1-4H3;2*1H/t30-;;/m1../s1

SMILES Code: OC1=C(C)C(CC[C@](C)(CN2CCN(C3=NC(N4CCCC4)=NC(N5CCCC5)=C3)CC2)O6)=C6C(C)=C1C.[H]Cl.[H]Cl

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info:

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 593.63 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
In vitro protocol:
In vivo protocol:

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Totzke J, Gurbani D, Raphemot R, Hughes PF, Bodoor K, Carlson DA, Loiselle DR, Bera AK, Eibschutz LS, Perkins MM, Eubanks AL, Campbell PL, Fox DA, Westover KD, Haystead TAJ, Derbyshire ER. Takinib, a Selective TAK1 Inhibitor, Broadens the Therapeutic Efficacy of TNF-α Inhibition for Cancer and Autoimmune Disease. Cell Chem Biol. 2017 Aug 17;24(8):1029-1039.e7. doi: 10.1016/j.chembiol.2017.07.011. PubMed PMID: 28820959; PubMed Central PMCID: PMC5576570.

2: Yuan J, Cui G, Li W, Zhang X, Wang X, Zheng H, Zhang J, Xiang S, Xie Z. Propofol Enhances Hemoglobin-Induced Cytotoxicity in Neurons. Anesth Analg. 2016 Apr;122(4):1024-30. doi: 10.1213/ANE.0000000000001123. PubMed PMID: 26771264; PubMed Central PMCID: PMC5123442.

3: Kawarski M, Hagerman TK, Karver CE. Lazaroids U83836E and U74389G are potent, time-dependent inhibitors of caspase-1. Chem Biol Drug Des. 2015 Nov;86(5):1049-54. doi: 10.1111/cbdd.12572. Epub 2015 Apr 30. PubMed PMID: 25871734.

4: Yu Y, Jian MY, Wang YZ, Han RQ. Propofol ameliorates calpain-induced collapsin response mediator protein-2 proteolysis in traumatic brain injury in rats. Chin Med J (Engl). 2015 Apr 5;128(7):919-27. doi: 10.4103/0366-6999.154298. PubMed PMID: 25836613; PubMed Central PMCID: PMC4834009.

5: Wu L, Du Y, Lok J, Lo EH, Xing C. Lipocalin-2 enhances angiogenesis in rat brain endothelial cells via reactive oxygen species and iron-dependent mechanisms. J Neurochem. 2015 Mar;132(6):622-8. doi: 10.1111/jnc.13023. Epub 2015 Jan 29. PubMed PMID: 25557118; PubMed Central PMCID: PMC4359653.

6: Wang H, Zheng Z, Gong Y, Zhu B, Xu X. U83836E inhibits retinal neurodegeneration in early-stage streptozotocin-induced diabetic rats. Ophthalmic Res. 2011;46(1):19-24. doi: 10.1159/000321952. Epub 2010 Nov 27. PubMed PMID: 21109760.

7: Hall ED, Vaishnav RA, Mustafa AG. Antioxidant therapies for traumatic brain injury. Neurotherapeutics. 2010 Jan;7(1):51-61. doi: 10.1016/j.nurt.2009.10.021. Review. PubMed PMID: 20129497; PubMed Central PMCID: PMC2818465.

8: Tejima E, Zhao BQ, Tsuji K, Rosell A, van Leyen K, Gonzalez RG, Montaner J, Wang X, Lo EH. Astrocytic induction of matrix metalloproteinase-9 and edema in brain hemorrhage. J Cereb Blood Flow Metab. 2007 Mar;27(3):460-8. Epub 2006 Jun 21. PubMed PMID: 16788715.

9: Thajeb P, Kuo JS, Shyu WC, Lin SZ. Neuroprotection with methylaminochroman and lazaroid of embryonic ventral mesencephalic tegmental dopaminergic neurons in cold storage. J Clin Neurosci. 2006 May;13(4):467-70. PubMed PMID: 16678726.

10: Sayyed SG, Kumar A, Sharma SS. Effects of U83836E on nerve functions, hyperalgesia and oxidative stress in experimental diabetic neuropathy. Life Sci. 2006 Jul 17;79(8):777-83. Epub 2006 Mar 31. PubMed PMID: 16581090.

11: Xie J, Shaikh ZA. Cadmium-induced apoptosis in rat kidney epithelial cells involves decrease in nuclear factor-kappa B activity. Toxicol Sci. 2006 May;91(1):299-308. Epub 2006 Feb 14. PubMed PMID: 16478757.

12: Grisel JJ, Chen WJ. Antioxidant pretreatment does not ameliorate alcohol-induced Purkinje cell loss in the developing rat cerebellum. Alcohol Clin Exp Res. 2005 Jul;29(7):1223-9. PubMed PMID: 16046878.

13: Skrzydlewska E, Elas M, Ostrowska J. Protective Effects of N-Acetylcysteine and Vitamin E Derivative U83836E on Proteins Modifications Induced by Methanol Intoxication. Toxicol Mech Methods. 2005;15(4):263-70. doi: 10.1080/15376520590968815. PubMed PMID: 20021091.

14: Blasig IE, Mertsch K, Haseloff RF. Nitronyl nitroxides, a novel group of protective agents against oxidative stress in endothelial cells forming the blood-brain barrier. Neuropharmacology. 2002 Nov;43(6):1006-14. PubMed PMID: 12423670.

15: Wang X, Mori T, Sumii T, Lo EH. Hemoglobin-induced cytotoxicity in rat cerebral cortical neurons: caspase activation and oxidative stress. Stroke. 2002 Jul;33(7):1882-8. PubMed PMID: 12105370.

16: Stull ND, Polan DP, Iacovitti L. Antioxidant compounds protect dopamine neurons from death due to oxidative stress in vitro. Brain Res. 2002 Mar 29;931(2):181-5. PubMed PMID: 11897104.

17: Callaway JK, Beart PM, Jarrott B, Giardina SF. Incorporation of sodium channel blocking and free radical scavenging activities into a single drug, AM-36, results in profound inhibition of neuronal apoptosis. Br J Pharmacol. 2001 Apr;132(8):1691-8. PubMed PMID: 11309240; PubMed Central PMCID: PMC1572735.

18: Huang HM, Ou HC, Hsieh SJ. Antioxidants prevent amyloid peptide-induced apoptosis and alteration of calcium homeostasis in cultured cortical neurons. Life Sci. 2000 Mar 31;66(19):1879-92. PubMed PMID: 10809185.

19: Dobrzyńska I, Skrzydlewska E, Figaszewski Z. Influence of trolox derivative and N-acetylcysteine on surface charge density of erythrocytes in methanol intoxicated rats. Environ Toxicol Pharmacol. 1999 Dec;8(1):15-21. PubMed PMID: 21781937.

20: Lai YL, Wu HD, Chen CF. Antioxidants attenuate chronic hypoxic pulmonary hypertension. J Cardiovasc Pharmacol. 1998 Nov;32(5):714-20. PubMed PMID: 9821844.