Pimethixene maleate

Catalog No.S3913 Batch:S391301

Technical Data

Formula	C₂₃H₂₃NO₄S
Molecular Weight	409.5	CAS No.	13187-06-9
Solubility (25°C)*	In vitro	DMSO	82 mg/mL (200.24 mM)
		Ethanol	7 mg/mL (17.09 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

Pimethixene (Pimetixene) maleate, an antihistamine, anntimigraine agent and antiserotonergic compound, is a highly potent antagonist of a broad range of monoamine receptors, including a variety of serotonin receptors. Pimethixene maleate inhibits 5-HT2A, 5-HT2B, 5-HT2C, 5-HT1A, 5-HT1B, 5-HT6, 5-HT7, Adrenergic α-1A, Dopamine D1 Receptor, Dopamine D2 Receptor, Dopamine D4.4 Receptor, Histamine H1 Receptor, Muscarinic M1 and Muscarinic M2 with pKi of 10.22, 10.44, 8.42, 7.63, < 5, 7.30, 7.28, 7.61, 6.37, 8.19, 7.54, 10.14, 8.61 and 9.38, respectively.

Targets

5-HT2B ^[1] (Cell-free assay)	5-HT2A ^[1] (Cell-free assay)	Histamine H1 Receptor ^[1] (Cell-free assay)	Muscarinic M2 ^[1] (Cell-free assay)	Muscarinic M1 ^[1] (Cell-free assay)	View More
10.44(pKi)	10.22(pKi)	10.14(pKi)	9.38(pKi)	8.61(pKi)	View More

In vitro

Pimethixene shows the least potency against pancreatic cancer cell lines with an IC50 up to a millimolar concentration.^[2]

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines pancreatic cancer cell lines Concentrations 10 pM-5 mM Incubation Time 4 days Method For IC50 determination of drugs, 5000 cells were seeded in 96‐well plates on day 0. On day 1, drugs in a series of 10‐fold dilutions were added to the cells. For dasatinib and FTY‐720, the doses were from 10 μM to 10 pM; For phenothiazines, the concentration was from 100 μM except pimethixene (5 mM). On day 4, MTT (3‐(4,5‐Dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide) based assays were performed and absorbance was measured at 595 nm with 630 nm.

Cell Assay:^{^[2]}

Cell lines
pancreatic cancer cell lines
Concentrations
10 pM-5 mM
Incubation Time
4 days
Method
For IC50 determination of drugs, 5000 cells were seeded in 96‐well plates on day 0. On day 1, drugs in a series of 10‐fold dilutions were added to the cells. For dasatinib and FTY‐720, the doses were from 10 μM to 10 pM; For phenothiazines, the concentration was from 100 μM except pimethixene (5 mM). On day 4, MTT (3‐(4,5‐Dimethylthiazol‐2‐yl)‐2,5‐diphenyltetrazolium bromide) based assays were performed and absorbance was measured at 595 nm with 630 nm.

References

RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.

SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.