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MedKoo Cat#: 528313 | Name: Licostinel

Description:

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

Licostinel, also known as ACEA-1021 and CGP-63446, is a glutamate receptor antagonist potentially for the treatment of pain and stroke. Intravenous Licostinel reduced cerebral infarction by 62% (15 min treatment delay) and 42% (2 h treatment delay), relative to vehicle-injected rats, when subjected to a modified Tamura and permanent intraluminal filament model of stroke, respectively. Licostinel protects against permanent focal cerebral ischemia.

Chemical Structure

Licostinel
Licostinel
CAS#153504-81-5

Theoretical Analysis

MedKoo Cat#: 528313

Name: Licostinel

CAS#: 153504-81-5

Chemical Formula: C8H3Cl2N3O4

Exact Mass: 274.9501

Molecular Weight: 276.03

Elemental Analysis: C, 34.81; H, 1.10; Cl, 25.69; N, 15.22; O, 23.18

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.
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Related CAS #
No Data
Synonym
Licostinel; ACEA-1021; ACEA 1021; ACEA1021; CGP-63446; CGP 63446; CGP63446
IUPAC/Chemical Name
6,7-dichloro-5-nitro-1,4-dihydroquinoxaline-2,3-dione
InChi Key
CHFSOFHQIZKQCR-UHFFFAOYSA-N
InChi Code
InChI=1S/C8H3Cl2N3O4/c9-2-1-3-5(6(4(2)10)13(16)17)12-8(15)7(14)11-3/h1H,(H,11,14)(H,12,15)
SMILES Code
O=C1NC2=C(C([N+]([O-])=O)=C(Cl)C(Cl)=C2)NC1=O
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

Preparing Stock Solutions

The following data is based on the product molecular weight 276.03 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
1: Qiu W, Wei R, Zhang C, Zhang C, Leng W, Wang W. A glycine site-specific NMDA receptor antagonist protects retina ganglion cells from ischemic injury by modulating apoptotic cascades. J Cell Physiol. 2010 Jun;223(3):819-26. doi: 10.1002/jcp.22118. PubMed PMID: 20333677. 2: Cai SX. Glycine/NMDA receptor antagonists as potential CNS therapeutic agents: ACEA-1021 and related compounds. Curr Top Med Chem. 2006;6(7):651-62. PubMed PMID: 16719807. 3: Petty MA, Weintraub PM, Maynard KI. ACEA 1021: flip or flop? CNS Drug Rev. 2004 Winter;10(4):337-48. Review. PubMed PMID: 15592582. 4: Wiley JL, Balster RL. Effects of modulators of N-methyl-D-aspartate receptor-mediated neurotransmission on diazepam discrimination in rats. Life Sci. 2004 May 28;75(2):141-51. PubMed PMID: 15120567. 5: Petty MA, Neumann-Haefelin C, Kalisch J, Sarhan S, Wettstein JG, Juretschke HP. In vivo neuroprotective effects of ACEA 1021 confirmed by magnetic resonance imaging in ischemic stroke. Eur J Pharmacol. 2003 Aug 1;474(1):53-62. PubMed PMID: 12909195. 6: Sarhan S, Wettstein JG, Maynard KI. Delayed treatment with 5-nitro-6,7-dichloro-1,4-dihydro-2,3-quinoxalinedione, a glycine site N-methyl-D-aspartate antagonist, protects against permanent middle cerebral artery occlusion in male rats. Neurosci Lett. 2003 Aug 28;347(3):147-50. PubMed PMID: 12875907. 7: Ikonomidou C, Turski L. Why did NMDA receptor antagonists fail clinical trials for stroke and traumatic brain injury? Lancet Neurol. 2002 Oct;1(6):383-6. Review. PubMed PMID: 12849400. 8: Zhou ZL, Kher SM, Cai SX, Whittemore ER, Espitia SA, Hawkinson JE, Tran M, Woodward RM, Weber E, Keana JF. Synthesis and SAR of novel di- and trisubstituted 1,4-dihydroquinoxaline-2,3-diones related to licostinel (Acea 1021) as NMDA/glycine site antagonists. Bioorg Med Chem. 2003 Apr 17;11(8):1769-80. PubMed PMID: 12659763. 9: Russell BR, Laverty R. The effect of (R)-HA966 or ACEA 1021 on dexfenfluramine or (S)-MDMA-induced changes in temperature, activity, and neurotoxicity. Pharmacol Biochem Behav. 2001 Mar;68(3):565-74. PubMed PMID: 11325413. 10: Russell BR, Laverty R. Correlation between 5-HT content and uptake site density following (S)-MDMA and dexfenfluramine-induced depletion, and with neuroprotection by the glycine site-specific NMDA antagonist ACEA 1021. Ann N Y Acad Sci. 2000 Sep;914:208-14. PubMed PMID: 11085322. 11: Nishiyama T. Interaction among NMDA receptor-, NMDA glycine site- and AMPA receptor antagonists in spinally mediated analgesia. Can J Anaesth. 2000 Jul;47(7):693-8. PubMed PMID: 10930211. 12: Nishiyama T. Interaction between intrathecal morphine and glutamate receptor antagonists in formalin test. Eur J Pharmacol. 2000 May 3;395(3):203-10. PubMed PMID: 10812050. 13: Bespalov AY, Dravolina OA, Zvartau EE, Beardsley PM, Balster RL. Effects of NMDA receptor antagonists on cocaine-conditioned motor activity in rats. Eur J Pharmacol. 2000 Mar 3;390(3):303-11. PubMed PMID: 10708738. 14: Pouw B, Nour M, Matsumoto RR. Effects of AMPA/kainate glutamate receptor antagonists on cocaine-induced convulsions and lethality in mice. Eur J Pharmacol. 1999 Dec 15;386(2-3):181-6. PubMed PMID: 10618468. 15: Licostinel. ACEA 1021. Drugs R D. 1999 Jan;1(1):27-8. PubMed PMID: 10565977. 16: Albers GW, Clark WM, Atkinson RP, Madden K, Data JL, Whitehouse MJ. Dose escalation study of the NMDA glycine-site antagonist licostinel in acute ischemic stroke. Stroke. 1999 Mar;30(3):508-13. PubMed PMID: 10066844. 17: Wiley JL, Compton AD, Holcomb JD, McCallum SE, Varvel SA, Porter JH, Balster RL. Effects of modulation of NMDA neurotransmission on response rate and duration in a conflict procedure in rats. Neuropharmacology. 1998 Dec;37(12):1527-34. PubMed PMID: 9886675. 18: Lingenhöhl K, Pozza MF. Reevaluation of ACEA 1021 as an antagonist at the strychnine-insensitive glycine site of the N-methyl-D-aspartate receptor. Neuropharmacology. 1998 Jun;37(6):729-37. PubMed PMID: 9707286. 19: Pearlstein RD, Beirne JP, Massey GW, Warner DS. Neuroprotective effects of NMDA receptor glycine recognition site antagonism: dependence on glycine concentration. J Neurochem. 1998 May;70(5):2012-9. PubMed PMID: 9572287. 20: Morimoto Y, Wu B, Bart RD, Morimoto Y, Pearlstein RD, Warner DS. Effects of NMDA receptor glycine recognition site antagonism on cerebral metabolic rate for glucose and cerebral blood flow in the conscious rat. Brain Res. 1998 Jan 1;779(1-2):170-6. PubMed PMID: 9473659.