Procaterol hydrochloride
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MedKoo CAT#: 318574

CAS#: 62929-91-3 (HCl)

Description: Procaterol hydrochloride is a specific and very potent β2-AR agonist. It acts as a vasodialator for long term treatment of asthma.

Chemical Structure

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Procaterol hydrochloride
CAS# 62929-91-3 (HCl)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 318574
Name: Procaterol hydrochloride
CAS#: 62929-91-3 (HCl)
Chemical Formula: C16H23ClN2O3
Exact Mass: 326.14
Molecular Weight: 326.821
Elemental Analysis: C, 58.80; H, 7.09; Cl, 10.85; N, 8.57; O, 14.69

Price and Availability

Size Price Availability Quantity
10mg USD 280 2 Weeks
25mg USD 530 2 Weeks
50mg USD 900 2 Weeks
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Related CAS #: 59828-07-8 (HCl)   62929-91-3 (HCl)   72332-33-3 (free base)   81262-93-3 (HCl   hemihydrate)  

Synonym: Procaterol Hydrochloride; OPC 2009; OPC-2009; OPC2009; CI 888; CI-888; CI888.

IUPAC/Chemical Name: 8-hydroxy-5-[(1R,2S)-1-hydroxy-2-(propan-2-ylamino)butyl]-1H-quinolin-2-one;hydrochloride

InChi Key: AEQDBKHAAWUCMT-CVHDTDHSSA-N

InChi Code: InChI=1S/C16H22N2O3.ClH/c1-4-12(17-9(2)3)16(21)11-5-7-13(19)15-10(11)6-8-14(20)18-15;/h5-9,12,16-17,19,21H,4H2,1-3H3,(H,18,20);1H/t12-,16+;/m0./s1

SMILES Code: CCC(C(C1=C2C=CC(=O)NC2=C(C=C1)O)O)NC(C)C.Cl

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: Soluble in DMSO, not in water

Shelf Life: >2 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:
Product Data
Instruction:
View handling instruction
Biological target: Procaterol hydrochloride is a specific and very potent β2-AR agonist.
In vitro activity: This study evaluated procaterol and dexamethasone in the hydrogen peroxide (H2O2)-induced immortal human bronchial epithelial cell model of oxidative stress and investigated the underlying mechanisms. Results showed that exposure to 125 μM H2O2 for 2 h led to a 50% reduction in the cell viability, significantly increased the percentage of apoptosis, and elevated levels of malondialdehyde and reactive oxygen species. Pretreatment with procaterol (25 - 200 nM) could reduce these effects in a dose-dependent manner. In contrast, pretreatment with dexamethasone (100 nM, 1000 nM) was inefficient. Reference: J Pharmacol Sci. 2014;125(1):39-50. https://pubmed.ncbi.nlm.nih.gov/24739282/
In vivo activity: Three intervention groups were investigated: a procaterol inhalation only group; a procaterol inhalation plus endotoxin injection mouse group (in vivo); and a procaterol incubation group (in vitro). The diaphragm muscle in all groups was dissected and measurements of its contractile properties were performed. The effects of procaterol inhalation shifted the force-frequency curves upward at 30 minutes after inhalation, and inhibited the decline of force-frequency curves due to endotoxin injection in vivo. Reference: Allergol Int. 2007 Sep;56(3):285-91. https://pubmed.ncbi.nlm.nih.gov/17646734/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
Ethanol 3.0 9.18
Water 48.8 149.44
Ethanol 3.0 9.18
Water 48.8 149.44

Preparing Stock Solutions

The following data is based on the product molecular weight 326.82 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. Deng Z, Zhou JJ, Sun SY, Zhao X, Sun Y, Pu XP. Procaterol but not dexamethasone protects 16HBE cells from H₂O₂-induced oxidative stress. J Pharmacol Sci. 2014;125(1):39-50. doi: 10.1254/jphs.13206fp. Epub 2014 Apr 16. PMID: 24739282. 2. Yamaya M, Nishimura H, Hatachi Y, Yoshida M, Fujiwara H, Asada M, Nakayama K, Yasuda H, Deng X, Sasaki T, Kubo H, Nagatomi R. Procaterol inhibits rhinovirus infection in primary cultures of human tracheal epithelial cells. Eur J Pharmacol. 2011 Jan 10;650(1):431-44. doi: 10.1016/j.ejphar.2010.09.056. Epub 2010 Oct 15. PMID: 20940011. 3. Shindoh C, Sasaki K, Shindoh Y, Tamura G. Inhalation and incubation with procaterol increases diaphragm muscle contractility in mice. Allergol Int. 2007 Sep;56(3):285-91. doi: 10.2332/allergolint.O-06-463. Epub 2007 Aug 1. PMID: 17646734. 4. Tashimo H, Yamashita N, Ishida H, Nagase H, Adachi T, Nakano J, Yamamura K, Yano T, Yoshihara H, Ohta K. Effect of procaterol, a beta(2) selective adrenergic receptor agonist, on airway inflammation and hyperresponsiveness. Allergol Int. 2007 Sep;56(3):241-7. doi: 10.2332/allergolint.O-06-456. Epub 2007 Jul 1. PMID: 17582211.
In vitro protocol: 1. Deng Z, Zhou JJ, Sun SY, Zhao X, Sun Y, Pu XP. Procaterol but not dexamethasone protects 16HBE cells from H₂O₂-induced oxidative stress. J Pharmacol Sci. 2014;125(1):39-50. doi: 10.1254/jphs.13206fp. Epub 2014 Apr 16. PMID: 24739282. 2. Yamaya M, Nishimura H, Hatachi Y, Yoshida M, Fujiwara H, Asada M, Nakayama K, Yasuda H, Deng X, Sasaki T, Kubo H, Nagatomi R. Procaterol inhibits rhinovirus infection in primary cultures of human tracheal epithelial cells. Eur J Pharmacol. 2011 Jan 10;650(1):431-44. doi: 10.1016/j.ejphar.2010.09.056. Epub 2010 Oct 15. PMID: 20940011.
In vivo protocol: 1. Shindoh C, Sasaki K, Shindoh Y, Tamura G. Inhalation and incubation with procaterol increases diaphragm muscle contractility in mice. Allergol Int. 2007 Sep;56(3):285-91. doi: 10.2332/allergolint.O-06-463. Epub 2007 Aug 1. PMID: 17646734. 2. Tashimo H, Yamashita N, Ishida H, Nagase H, Adachi T, Nakano J, Yamamura K, Yano T, Yoshihara H, Ohta K. Effect of procaterol, a beta(2) selective adrenergic receptor agonist, on airway inflammation and hyperresponsiveness. Allergol Int. 2007 Sep;56(3):241-7. doi: 10.2332/allergolint.O-06-456. Epub 2007 Jul 1. PMID: 17582211.

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1. Marullo, S., Emorine, L.J., Strosberg, A.D., et al. Selective binding of ligands to β1, β2 or chimeric β1/β2-adrenergic receptors involves multiple subsites. EMBO J. 9(5), 1471-1476 (1990).

2. Kikkawa, H., Naito, K., and Ikezawa, K. Tracheal relaxing effects and β2-selectivity of TA-2005, a newly developed bronchodilating agent, in isolated guinea pig tissues. Jpn. J. Pharmacol. 57(2), 175-185 (1991).

3. Yoshizaki, S., Tanimura, K., Tamada, S., et al. Sympathomimetic amines having a carbostyril nucleus. J. Med. Chem. 19(9), 1138-1142 (1976).

4. Mirza, Z.N., Tokuyama, K., Arakawa, H., et al. Inhaled procaterol inhibits histamine-induced airflow obstruction and microvascular leakage in guinea-pig airways with allergic inflammation. Clin. Exp. Allergy 28(5), 644-652 (1998).