WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H561505
CAS#: 173830-14-3
Description: Brasofensine Maleate is an inhibitor of the monoamine re-uptake mechanism.
Hodoodo Cat#: H561505
Name: Brasofensine Maleate
CAS#: 173830-14-3
Chemical Formula: C20H24Cl2N2O5
Exact Mass: 0.00
Molecular Weight: 443.320
Elemental Analysis: C, 54.19; H, 5.46; Cl, 15.99; N, 6.32; O, 18.04
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Synonym: NS-2214; BMS-204756-07; NS 2214; NS2214;
IUPAC/Chemical Name: (E)-1-[(1S,3S,4R,5R)-3-(3,4-Dichlorophenyl)-8-methyl-8-azabicyclo[3.2.1]octan-4-yl]-N-methoxymethanimine Maleate
InChi Key: XVXRAWKEYKMWFS-YGPNHCCBSA-N
InChi Code: InChI=1S/C16H20Cl2N2O.C4H4O4/c1-20-11-4-6-16(20)13(9-19-21-2)12(8-11)10-3-5-14(17)15(18)7-10;5-3(6)1-2-4(7)8/h3,5,7,9,11-13,16H,4,6,8H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b19-9+;2-1-/t11-,12+,13+,16+;/m0./s1
SMILES Code: CO/N=C/[C@@H]1[C@@H](C2=CC=C(Cl)C(Cl)=C2)C[C@]3([H])CC[C@@]1([H])N3C.O=C(O)/C=C\C(O)=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:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 443.32 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.
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: |
1: Zhu M, Whigan DB, Chang SY, Dockens RC. Disposition and metabolism of [14C]brasofensine in rats, monkeys, and humans. Drug Metab Dispos. 2008 Jan;36(1):24-35. Epub 2007 Oct 1. PubMed PMID: 17908924.
2: Minuzzi L, Olsen AK, Bender D, Arnfred S, Grant R, Danielsen EH, Cumming P. Quantitative autoradiography of ligands for dopamine receptors and transporters in brain of Göttingen minipig: comparison with results in vivo. Synapse. 2006 Mar 15;59(4):211-9. PubMed PMID: 16385509.
3: Doudet DJ, Ruth TJ, Holden JE. Sequential versus nonsequential measurement of density and affinity of dopamine D2 receptors with [11C]raclopride: 2: effects of DAT inhibitors. J Cereb Blood Flow Metab. 2006 Jan;26(1):28-37. PubMed PMID: 15973354.
4: Johnston TH, Brotchie JM. Drugs in development for Parkinson's disease. Curr Opin Investig Drugs. 2004 Jul;5(7):720-6. Review. PubMed PMID: 15298067.
5: Bayes M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2003 May;25(4):317-40. PubMed PMID: 12808477.
6: Pearce RK, Smith LA, Jackson MJ, Banerji T, Scheel-Krüger J, Jenner P. The monoamine reuptake blocker brasofensine reverses akinesia without dyskinesia in MPTP-treated and levodopa-primed common marmosets. Mov Disord. 2002 Sep;17(5):877-86. PubMed PMID: 12360536.
7: Frackiewicz EJ, Jhee SS, Shiovitz TM, Webster J, Topham C, Dockens RC, Whigan D, Salazar DE, Cutler NR. Brasofensine treatment for Parkinson's disease in combination with levodopa/carbidopa. Ann Pharmacother. 2002 Feb;36(2):225-30. PubMed PMID: 11847938.
8: Yu P. Brasofensine NeuroSearch. Curr Opin Investig Drugs. 2000 Dec;1(4):504-7. Review. PubMed PMID: 11249705.
9: Fischman AJ, Bonab AA, Rubin RH. Regional pharmacokinetics of orally administered PET tracers. Curr Pharm Des. 2000 Nov;6(16):1625-9. PubMed PMID: 10974157.