MedChemExpress - Model Promethazine hydrochloride -58-33-3

Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors[1][2].

Promethazine hydrochloride

MCE China：Promethazine hydrochloride

Brand：MedChemExpress (MCE)

Cat. No.HY-B0781

CAS：58-33-3

Purity：99.20%

Storage：4°C, sealed storage, away from moisture and light *The compound is unstable in solutions, freshly prepared is recommended.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Promethazine hydrochloride is an orally active phenothiazine derivative with antihistaminic (H1), sedative, antiemetic, anticholinergic, and antimotion sickness properties. Promethazine hydrochloride is a potent H1 receptor antagonist and a mAChR antagonist. It also has a certain affinity for 5-HT2A and 5-HT2C receptors.

In Vitro：Promethazine hydrochloride (1.25-10 μM, 3 days) inhibits adipocyte formation in a dose-dependent manner[1]. Promethazine hydrochloride (10 μM, 0-12 days) decreases the expression of peroxisome proliferator activated receptor γ (PPARG) and reduces the phosphorylation level of CREB in PDGFRα+ cells[1]. Promethazine hydrochloride (10-1000 μM, 1-24 h) has cytotoxic at concentrations greater than 100 μM in L929 lung fibroblast cells[3].

In Vivo：Promethazine hydrochloride (0.05-0.1 mg/mL, p.o., 4 weeks) possesses inhibitory effect on ectopic fat cell formation in skeletal muscle in a mouse achilles tendon rupture model[1]. Promethazine hydrochloride (2.4-9.6 mg/kg, p.o.) has no effect on the development of femoral osteoporosis and retarded normal femoral expansion in the adult castrate male rats[4].

IC50 & Target：H1 Receptor

References：

[1]. Kasai T, et al. Promethazine Hydrochloride Inhibits Ectopic Fat Cell Formation in Skeletal Muscle. Am J Pathol. 2017 Dec;187(12):2627-2634. [Content Brief]

[2]. Fiorella D, et al. The role of the 5-HT2A and 5-HT2C receptors in the stimulus effects of hallucinogenic drugs. I: Antagonist correlation analysis. Psychopharmacology (Berl). 1995 Oct;121(3):347-56. [Content Brief]

[3]. McDonough JA, et al. Microcapsule-gel formulation of promethazine HCl for controlled nasal delivery: a motion sickness medication. J Microencapsul. 2007 Mar;24(2):109-16. [Content Brief]

[4]. Wink CS, et al. Effects of promethazine HCl on osteoporotic femora of adult castrated male rats. Acta Anat (Basel). [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
•   The products cover a variety of recombinant proteins, peptides, commonly used kits, more PROTAC, ADC and other characteristic products, widely used in new drug research and development, life science and other scientific research projects；
•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。

MedChemExpress - Model Promethazine hydrochloride -58-33-3

MCE products for research use only. We do not sell...

Promethazine hydrochloride