MedKoo Cat#: 555699 | Name: PSB-12054
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Description:

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

PSB-12054 is a potent P2X4 receptor inhibitor. PSB-12054 has IC(50) of 0.189 μM and good selectivity versus the other human P2X receptor subtypes.

Chemical Structure

PSB-12054
PSB-12054
CAS#1407632-07-8

Theoretical Analysis

MedKoo Cat#: 555699

Name: PSB-12054

CAS#: 1407632-07-8

Chemical Formula: C20H15NO3

Exact Mass: 317.1052

Molecular Weight: 317.34

Elemental Analysis: C, 75.70; H, 4.76; N, 4.41; O, 15.12

Price and Availability

Size Price Availability Quantity
10mg USD 285.00
50mg USD 1,050.00
100mg USD 1,750.00
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Related CAS #
No Data
Synonym
PSB-12054; PSB 12054; PSB12054; N-Cbz-phenoxazine,
IUPAC/Chemical Name
N-(benzyloxycarbonyl)phenoxazine; N-Cbz-phenoxazine; 10H-Phenoxazine-10-carboxylic acid, phenylmethyl ester
InChi Key
KGVCOYMLGBNCDW-UHFFFAOYSA-N
InChi Code
InChI=1S/C20H15NO3/c22-20(23-14-15-8-2-1-3-9-15)21-16-10-4-6-12-18(16)24-19-13-7-5-11-17(19)21/h1-13H,14H2
SMILES Code
O=C(N1C2=C(C=CC=C2)OC3=CC=CC=C13)OCC4=CC=CC=C4
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
To be determined
Shelf Life
>3 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
Product Data
Biological target:
PSB-12054 blocks voltage-gated potassium channels and inhibits inflammatory response by reducing the production of cytokines and increasing the production of anti-inflammatory mediators. PSB-12054 is also a potent antagonist of P2Y receptors. PSB-12054 interacts with other drugs that bind to P2Y receptors, such as carbamazepine.
In vitro activity:
In 1321N1 astrocytoma cells transfected with the human P2X4 receptor, PSB-12054 exhibited an IC50 value of 0.189 μM. These results indicate PSB-12054’s strong inhibitory effect on ATP-induced calcium influx. PSB-12054 displayed good selectivity, primarily affecting the P2X4 receptor subtype while showing minimal activity against other human P2X receptor subtypes. Reference: J Med Chem. 2012 Nov 26;55(22):9576-88. https://pubmed.ncbi.nlm.nih.gov/23075067/
In vivo activity:
To be determined

Preparing Stock Solutions

The following data is based on the product molecular weight 317.34 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:
1. Hernandez-Olmos V, Abdelrahman A, El-Tayeb A, Freudendahl D, Weinhausen S, Müller CE. N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists. J Med Chem. 2012 Nov 26;55(22):9576-88. doi: 10.1021/jm300845v. Epub 2012 Nov 1. PMID: 23075067.
In vitro protocol:
1. Hernandez-Olmos V, Abdelrahman A, El-Tayeb A, Freudendahl D, Weinhausen S, Müller CE. N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists. J Med Chem. 2012 Nov 26;55(22):9576-88. doi: 10.1021/jm300845v. Epub 2012 Nov 1. PMID: 23075067.
In vivo protocol:
To be determined
Zhang WJ, Zhu ZM, Liu ZX. The role of P2X4 receptor in neuropathic pain and its pharmacological properties. Pharmacol Res. 2020 Aug;158:104875. doi: 10.1016/j.phrs.2020.104875. Epub 2020 May 12. PMID: 32407956. Hernandez-Olmos V, Abdelrahman A, El-Tayeb A, Freudendahl D, Weinhausen S, Müller CE. N-substituted phenoxazine and acridone derivatives: structure-activity relationships of potent P2X4 receptor antagonists. J Med Chem. 2012 Nov 26;55(22):9576-88. doi: 10.1021/jm300845v. Epub 2012 Nov 1. PMID: 23075067.