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MedKoo Cat#: 526885 | Name: BL-1020 Mesylate

Description:

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

BL-1020, also known as CYP-1020; AN-168, a GABA A receptor agonist and dopamine receptor antagonist potentially for the treatment of schizophrenia, BL-1020 is an ester of GABA and perphenazine, and pharmacologically it acts as a D2 antagonist and GABA agonist. It has shown pro-cognitive effects in the trials. In March 2013, it went into the II/III trial phase. It has been introduced by BioLineRx, a biopharmaceutical development company.

Chemical Structure

BL-1020 Mesylate
BL-1020 Mesylate
CAS#916898-61-8 (mesylate)

Theoretical Analysis

MedKoo Cat#: 526885

Name: BL-1020 Mesylate

CAS#: 916898-61-8 (mesylate)

Chemical Formula: C26H37ClN4O5S2

Exact Mass: 0.0000

Molecular Weight: 585.18

Elemental Analysis: C, 53.37; H, 6.37; Cl, 6.06; N, 9.57; O, 13.67; S, 10.96

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 #
751477-01-7 (free base) 916898-61-8 (mesylate)
Synonym
BL-1020 Mesylate; BL 1020; BL1020; Perphenazine GABA ester; Perphenazine-4-aminobutyrate; Perphenazine gamma-aminobutyrate mesylate
IUPAC/Chemical Name
2-(4-(3-(2-chloro-10H-phenothiazin-10-yl)propyl)piperazin-1-yl)ethyl 4-aminobutanoate methanesulfonate
InChi Key
LOSZUFJASRVQGR-UHFFFAOYSA-N
InChi Code
InChI=1S/C25H33ClN4O2S.CH4O3S/c26-20-8-9-24-22(19-20)30(21-5-1-2-6-23(21)33-24)12-4-11-28-13-15-29(16-14-28)17-18-32-25(31)7-3-10-27;1-5(2,3)4/h1-2,5-6,8-9,19H,3-4,7,10-18,27H2;1H3,(H,2,3,4)
SMILES Code
ClC(C=C1N2CCCN3CCN(CCOC(CCCN)=O)CC3)=CC=C1SC4=C2C=CC=C4.OS(=O)(C)=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
Related CAS# 751477-01-7 (BL-1020) 916898-61-8 (BL-1020 Mesylate)

Preparing Stock Solutions

The following data is based on the product molecular weight 585.18 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: Thyme S, Song Y. Computational Design of DNA-Binding Proteins. Methods Mol Biol. 2016;1414:265-83. doi: 10.1007/978-1-4939-3569-7_16. PubMed PMID: 27094297. 2: Geffen Y, Keefe R, Rabinowitz J, Anand R, Davidson M. Bl-1020, a new γ-aminobutyric acid-enhanced antipsychotic: results of 6-week, randomized, double-blind, controlled, efficacy and safety study. J Clin Psychiatry. 2012 Sep;73(9):e1168-74. doi: 10.4088/JCP.12m07642. PubMed PMID: 23059159. 3: Anand R, Geffen Y, Vasile D, Dan I. An open-label tolerability study of BL-1020 antipsychotic: a novel gamma aminobutyric acid ester of perphenazine. Clin Neuropharmacol. 2010 Nov-Dec;33(6):297-302. doi: 10.1097/WNF.0b013e3181f8d501. PubMed PMID: 20921890. 4: Fitzgerald PB. BL-1020, an oral antipsychotic agent that reduces dopamine activity and enhances GABAA activity, for the treatment of schizophrenia. Curr Opin Investig Drugs. 2010 Jan;11(1):92-100. Review. PubMed PMID: 20047163. 5: Appel L, Geffen Y, Heurling K, Eriksson C, Antoni G, Kapur S. BL-1020, a novel antipsychotic candidate with GABA-enhancing effects: D2 receptor occupancy study in humans. Eur Neuropsychopharmacol. 2009 Dec;19(12):841-50. doi: 10.1016/j.euroneuro.2009.07.009. Epub 2009 Aug 29. PubMed PMID: 19717284. 6: Geffen Y, Nudelman A, Gil-Ad I, Rephaeli A, Huang M, Savitsky K, Klapper L, Winkler I, Meltzer HY, Weizman A. BL-1020: a novel antipsychotic drug with GABAergic activity and low catalepsy, is efficacious in a rat model of schizophrenia. Eur Neuropsychopharmacol. 2009 Jan;19(1):1-13. doi: 10.1016/j.euroneuro.2008.07.002. Epub 2008 Aug 30. PubMed PMID: 18757185. 7: Nudelman A, Gil-Ad I, Shpaisman N, Terasenko I, Ron H, Savitsky K, Geffen Y, Weizman A, Rephaeli A. A mutual prodrug ester of GABA and perphenazine exhibits antischizophrenic efficacy with diminished extrapyramidal effects. J Med Chem. 2008 May 8;51(9):2858-62. doi: 10.1021/jm7012453. Epub 2008 Mar 26. PubMed PMID: 18363346.