HX 531 | CAS#188844-34-0 | Retinoid X receptor Antagonist

MedKoo Cat#: 531959 | Name: HX 531

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Description:

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

HX 531 is an antagonist of retinoid X receptors.

Chemical Structure

HX 531

CAS#188844-34-0

Theoretical Analysis

MedKoo Cat#: 531959

Name: HX 531

CAS#: 188844-34-0

Chemical Formula: C29H29N3O4

Exact Mass: 483.2158

Molecular Weight: 483.57

Elemental Analysis: C, 72.03; H, 6.05; N, 8.69; O, 13.23

Price and Availability

Size	Price	Availability
5mg	USD 250.00	2 Weeks
10mg	USD 450.00
25mg	USD 800.00	2 Weeks

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Related CAS #

No Data

Synonym

HX 531; HX-531; HX531.

IUPAC/Chemical Name

4-(5,7,7,10,10-pentamethyl-2-nitro-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acid

InChi Key

SXKPGYKPQPYJER-UHFFFAOYSA-N

InChi Code

InChI=1S/C29H29N3O4/c1-28(2)12-13-29(3,4)22-16-25-20(15-21(22)28)26(17-6-8-18(9-7-17)27(33)34)30-23-14-19(32(35)36)10-11-24(23)31(25)5/h6-11,14-16H,12-13H2,1-5H3,(H,33,34)

SMILES Code

O=C(O)C1=CC=C(C2=NC3=CC([N+]([O-])=O)=CC=C3N(C)C4=CC5=C(C(C)(C)CCC5(C)C)C=C42)C=C1

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

>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:

HX531 is a potent RXR antagonist with an IC50 of 18 nM.

In vitro activity:

Accordingly, this study observed that HX531 strongly and significantly reduced (by 88.6%, p < 0.01) the mRNA expression of IL-6 induced by A2E (Figure 8E). HX531 also drastically inhibited IL-8 mRNA expression induced by A2E in RPE cells in vitro (99.6%, p < 0.001, Figure 8F). Reference: Aging (Albany NY). 2021 Sep 20;13(18):22040-22058. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8507260/

In vivo activity:

Treatment with 0.5 μM HX 531 (Fig. 1d) formed non-keratinized stratified squamous epithelium without large gaps between cells, which resemble in vivo epithelium. Reference: Microscopy (Oxf). 2022 Jun 6;71(3):152-160. https://pubmed.ncbi.nlm.nih.gov/35289919/

	Solvent	mg/mL	mM
Solubility
	DMF	15.0	31.02
	DMF:PBS (pH 7.2) (1:6)	0.1	0.29
	DMSO	17.7	36.53
	Ethanol	0.1	0.25

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 483.57 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. Chen P, Lin MH, Li YX, Huang ZJ, Rong YY, Lin QS, Ye ZC. Bexarotene enhances astrocyte phagocytosis via ABCA1-mediated pathways in a mouse model of subarachnoid hemorrhage. Exp Neurol. 2022 Sep 13;358:114228. doi: 10.1016/j.expneurol.2022.114228. Epub ahead of print. PMID: 36108713. 2. Fontaine V, Fournié M, Monteiro E, Boumedine T, Balducci C, Guibout L, Latil M, Sahel JA, Veillet S, Dilda PJ, Lafont R, Camelo S. A2E-induced inflammation and angiogenesis in RPE cells in vitro are modulated by PPAR-α, -β/δ, -γ, and RXR antagonists and by norbixin. Aging (Albany NY). 2021 Sep 20;13(18):22040-22058. doi: 10.18632/aging.203558. Epub 2021 Sep 20. PMID: 34544906; PMCID: PMC8507260. 3. Ishikawa S, Nikaido M, Otani T, Ogata K, Iida H, Inai Y, Tamaoki S, Inai T. Inhibition of retinoid X receptor improved the morphology, localization of desmosomal proteins and paracellular permeability in three-dimensional cultures of mouse keratinocytes. Microscopy (Oxf). 2022 Jun 6;71(3):152-160. doi: 10.1093/jmicro/dfac007. PMID: 35289919; PMCID: PMC9169536.

In vitro protocol:

In vivo protocol:

1. Ishikawa S, Nikaido M, Otani T, Ogata K, Iida H, Inai Y, Tamaoki S, Inai T. Inhibition of retinoid X receptor improved the morphology, localization of desmosomal proteins and paracellular permeability in three-dimensional cultures of mouse keratinocytes. Microscopy (Oxf). 2022 Jun 6;71(3):152-160. doi: 10.1093/jmicro/dfac007. PMID: 35289919; PMCID: PMC9169536.

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