Inhibitors Product Data Sheet

Brompheniramine maleate • Agonists

Cat. No.: HY-B0480 CAS No.: 980-71-2

Molecular Formula: C₂₀H₂₃BrN₂O₄ •

Molecular Weight: 435.31 Screening Libraries Target: Histamine Receptor Pathway: GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling Storage: Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month

SOLVENT & SOLUBILITY

In Vitro DMSO : 100 mg/mL (229.72 mM; Need ultrasonic)

H2O : 100 mg/mL (229.72 mM; Need ultrasonic)

Mass Solvent 1 mg 5 mg 10 mg Concentration Preparing 1 mM 2.2972 mL 11.4861 mL 22.9721 mL Stock Solutions 5 mM 0.4594 mL 2.2972 mL 4.5944 mL

10 mM 0.2297 mL 1.1486 mL 2.2972 mL

Please refer to the solubility information to select the appropriate solvent.

In Vivo 1. Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

2. Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

3. Add each solvent one by one: 10% DMSO >> 90% corn oil Solubility: ≥ 2.5 mg/mL (5.74 mM); Clear solution

BIOLOGICAL ACTIVITY

Description Brompheniramine ((±)-Brompheniramine) maleate is a potent and orally active antihistamine of the propylamine class.

Brompheniramine maleate is a selective histamine H1 receptor antagonist with a Kd of 6.06 nM. Brompheniramine maleate has anticholinergic, antidepressant and analgesia properties and can be used for allergic rhinitis research[1][2].

IC₅₀ & Target H1 Receptor 6.06 nM (Kd)

Page 1 of 2 www.MedChemExpress.com In Vitro In in vitro experiments, Brompheniramine blocks muscarinic cholinergic receptors in human chinese hamster ovary (CHO) cells, sodium and calcium channels in CHO cells, as well as potassium channels in human embryonic kidney 293 (HEK-293) [1] cells. Brompheniramine suppresses the transfected Nav1.5 channels from myocytes . MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo Brompheniramine as an antihistamine blocks sodium channels. Brompheniramine (3.0, 1.5, 1.1, 0.6, and 0.3 μmol)

treatment shows cutaneous analgesic effect with an ED50 value of 0.89 in a rat model of infiltration anesthesia. Subcutaneous Brompheniramine induces dose-relatedly analgesic effects, and Brompheniramine induces prolonged analgesic duration[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CUSTOMER VALIDATION

• Biomaterials. 2021, 120742.

See more customer validations on www.MedChemExpress.com

REFERENCES

[1]. Chong-Chi Chiu, et al. Subcutaneous brompheniramine for cutaneous analgesia in rats. Eur J Pharmacol. 2019 Oct 5;860:172544.

[2]. B Cusack, et al. Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65.

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Caution: Product has not been fully validated for medical applications. For research use only. Tel: 609-228-6898 Fax: 609-228-5909 E-mail: [email protected] Address: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USA

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