BL-1020 Mesylate

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MedKoo CAT#: 526885

CAS#: 916898-61-8 (mesylate)

Description: 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

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

Theoretical Analysis

MedKoo Cat#: 526885
Name: BL-1020 Mesylate
CAS#: 916898-61-8 (mesylate)
Chemical Formula: C26H37ClN4O5S2
Exact Mass: 0.00
Molecular Weight: 585.175
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 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.

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Related CAS #: 751477-01-7 (free base)   916898-61-8 (mesylate)    

Synonym: BL-1020 Mesylate; BL 1020; BL1020; CYP-1020; AN-168; 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)

Biological target:
In vitro activity:
In vivo activity:

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
Formulation protocol:
In vitro protocol:
In vivo protocol:

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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.