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Technical Data
| Formula | C17H23N3O1.C4H4O4 |
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| Molecular Weight | 401.46 | CAS No. | 59-33-6 | |
| Solubility (25°C)* | In vitro | DMSO | 80 mg/mL (199.27 mM) | |
| Water | 80 mg/mL (199.27 mM) | |||
| Ethanol | 80 mg/mL (199.27 mM) | |||
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* <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.) |
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Biological Activity
| Description | Pyrilamine Maleate (Mepyramine)is a histamine H1 receptor inverse agonist, it binds to a G protein-coupled form of the receptor and promotes a G protein-coupled inactive state of the H1 receptor that interferes with the Gq/11-mediated signaling. |
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| In vitro | Pyrilamine blocks the rapidly activating component of the delayed rectifier, IKr, with IC50 of 1.1 μM. Pyrilamine (10 μM) blocks the slowly activating component of the delayed rectifier, IKs and the inward rectifier, IK1 less than 20%. [1] |
| In vivo | Pyrilamine (15 mg/kg/day) significantly decreases the movement time and velocity, as well as the total food consumption and completely abolishes the circadian rhythmicity of locomotion in sham-operated rats. Pyrilamine (15 mg/kg/day) leads to the complete blockade of H(1) receptors in both sham- and portacaval anastomosis-operated rats. [2] Pyrilamine decreases the number of flinches in a dose dependent manner and decreases c-fos mRNA expression in lumbar spinal cord of rats. [3] Pyrilamine is mainly metabolited into the O-glucuronic acid conjugate of O-demethyl pyrilamine in the rats. The terminal plasma elimination half-life of Pyrilamine does not increase with increasing doses (2.3 hours, 0.7 mg/kg; 1.5 hours, 7.0 mg/kg) and thus pyrilamine does not exhibit dose-dependent elimination. [4] Pyrilamine is slightly less mutagenic than Methapyrilene over a comparable range of concentrations, and also induces predominantly small-colony mutants in the L5178Y/TK +/- mouse lymphoma assay. [5] |
Protocol (from reference)
References
Selleck's Pyrilamine Maleate has been cited by 1 publication
| Critical role of mitogen-inducible gene 6 in restraining endothelial cell permeability to maintain vascular homeostasis [ J Cell Commun Signal, 2023, 17(1):151-165] | PubMed: 36284029 |
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.