HZ-52 | CAS# 1077626-51-7 | 5-lipoxygenase inhibitor

MedKoo Cat#: 574739 | Name: HZ-52

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

HZ-52 is a potent, reversible inhibitor of 5-lipoxygenase that blocks leukotriene synthesis in polymorphonuclear leukocytes. HZ-52 also attenuates leukotriene B4 synthesis, prevents carrageenan-induced pleurisy, and protects against platelet-activating factor-induced shock.

Chemical Structure

HZ-52

CAS#1077626-51-7

Theoretical Analysis

MedKoo Cat#: 574739

Name: HZ-52

CAS#: 1077626-51-7

Chemical Formula: C24H26ClN3O2S

Exact Mass: 455.1434

Molecular Weight: 456.00

Elemental Analysis: C, 63.22; H, 5.75; Cl, 7.77; N, 9.22; O, 7.02; S, 7.03

Price and Availability

Size	Price	Availability
5mg	USD 350.00	2 Weeks
10mg	USD 650.00	2 Weeks
25mg	USD 1,050.00	2 Weeks

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Related CAS #

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Synonym

HZ-52, HZ52, HZ 52

IUPAC/Chemical Name

2-((4-([1,1'-biphenyl]-4-ylamino)-6-chloropyrimidin-2-yl)thio)octanoic acid

InChi Key

MLNIGXYHGQLWLD-UHFFFAOYSA-N

InChi Code

InChI=1S/C24H26ClN3O2S/c1-2-3-4-8-11-20(23(29)30)31-24-27-21(25)16-22(28-24)26-19-14-12-18(13-15-19)17-9-6-5-7-10-17/h5-7,9-10,12-16,20H,2-4,8,11H2,1H3,(H,29,30)(H,26,27,28)

SMILES Code

ClC1=CC(NC2=CC=C(C3=CC=CC=C3)C=C2)=NC(SC(CCCCCC)C(O)=O)=N1

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

Shelf Life

>3 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:

A reversible inhibitor of 5-lipoxygenase.

In vitro activity:

In accordance with this study’s previous findings (Koeberle et al., 2008), HZ52 inhibited 5-LO product synthesis in human PMNL stimulated with the Ca2+ ionophore A23187 (2.5 µM) plus AA (20 µM) with an IC50 = 0.7 µM for both LTB4 and 5-H(P)ETE (Figure 1B). Reference: Br J Pharmacol. 2011 Sep;164(2b):781-93. https://pubmed.ncbi.nlm.nih.gov/21506958/

In vivo activity:

HZ52, 1.5 mg·kg⁻¹ i.p., prevented carrageenan-induced pleurisy accompanied by reduced LTB(4) levels and protected mice (10 mg·kg⁻¹, i.p.) against PAF-induced shock. Reference: Br J Pharmacol. 2011 Sep;164(2b):781-93. https://pubmed.ncbi.nlm.nih.gov/21506958/

	Solvent	mg/mL	mM
Solubility
	DMF:PBS (pH 7.2) (1:9)	0.1	0.22
	DMSO	20.0	43.86
	Ethanol	10.0	21.93

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 456.00 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.

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. Greiner C, Hörnig C, Rossi A, Pergola C, Zettl H, Schubert-Zsilavecz M, Steinhilber D, Sautebin L, Werz O. 2-(4-(Biphenyl-4-ylamino)-6-chloropyrimidin-2-ylthio)octanoic acid (HZ52)--a novel type of 5-lipoxygenase inhibitor with favourable molecular pharmacology and efficacy in vivo. Br J Pharmacol. 2011 Sep;164(2b):781-93. doi: 10.1111/j.1476-5381.2011.01451.x. PMID: 21506958; PMCID: PMC3188909.

In vitro protocol:

In vivo protocol:

1. Greiner, C., Hörnig, C., Rossi, A., et al. 2-(4-(Biphenyl-4-ylamino)-6-chloropyrimidin-2-ylthio)octanoic acid (HZ52) - a novel type 5-lipoxygenase inhibitor with favorable molecular pharmacology and efficacy in vivo. British Journal of Pharmacology 164(2b), 781-793 (2011).