HX-630 | CAS# 188844-52-2 | Synthetic rexinoid

MedKoo Cat#: 576414 | Name: HX-630

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Description:

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

HX-630 is a synthetic rexinoid that acts as a selective agonist of retinoid X receptors (RXRs), nuclear receptors involved in the regulation of gene expression related to cell differentiation, proliferation, and apoptosis. It exhibits bioactivity by modulating RXR-mediated transcriptional activity, influencing pathways such as lipid metabolism and cellular homeostasis. Through RXR activation, HX-630 can form heterodimers with other nuclear receptors (e.g., PPARs, LXR, and FXR), thereby affecting diverse physiological processes and showing potential in treating metabolic and inflammatory disorders.

Chemical Structure

HX-630

CAS#188844-52-2

Theoretical Analysis

MedKoo Cat#: 576414

Name: HX-630

CAS#: 188844-52-2

Chemical Formula: C28H27NO2S

Exact Mass: 441.1762

Molecular Weight: 441.59

Elemental Analysis: C, 76.16; H, 6.16; N, 3.17; O, 7.25; S, 7.26

Price and Availability

Size	Price	Availability	Quantity
10mg	USD 600.00	2 Weeks
50mg	USD 1,500.00	2 Weeks

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Related CAS #

No Data

Synonym

HX 630; HX630; HX-630

IUPAC/Chemical Name

Benzoic acid, 4-(7,8,9,10-tetrahydro-7,7,10,10-tetramethylbenzo(b)naphtho(2,3-f)(1,4)thiazepin-12-yl)-

InChi Key

PFGCWQPTOKPRRK-UHFFFAOYSA-N

InChi Code

InChI=1S/C28H27NO2S/c1-27(2)13-14-28(3,4)21-16-24-19(15-20(21)27)25(17-9-11-18(12-10-17)26(30)31)29-22-7-5-6-8-23(22)32-24/h5-12,15-16H,13-14H2,1-4H3,(H,30,31)

SMILES Code

CC1(C)CCC(C)(C)c2cc3C(=Nc4ccccc4Sc3cc12)c5ccc(cc5)C(=O)O

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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:

HX 630 is a RXR agonist.

In vitro activity:

HX630 supplementation before H2O2 addition protected RPE cells, reducing the percentage of D407 cells with fragmented or pyknotic nuclei from 27% in H2O2–treated cultures to nearly 12% (Fig. 3C XIV, D) and the percentage of cleaved-caspase 3 positive cells (Fig. 3C XV, E), from 20% to nearly 9% (p < 0.05). Reference: Biochim Biophys Acta. 2016 Jun;1863(6 Pt A):1134-45. https://pubmed.ncbi.nlm.nih.gov/26883505/

In vivo activity:

Although there were no significant differences in body weights and plasma ACTH levels between the control group and the HX630 treated group (data not shown), HX630 significantly decreased the tumor volumes (Fig 7A–7E) as well as Pomc mRNA expressions in the tumor cells (Fig 7F). Reference: PLoS One. 2015 Dec 29;10(12):e0141960. https://pubmed.ncbi.nlm.nih.gov/26714014/

	Solvent	mg/mL	mM
Solubility
	DMSO	22.1	50.00

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 441.59 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. Ayala-Peña VB, Pilotti F, Volonté Y, Rotstein NP, Politi LE, German OL. Protective effects of retinoid x receptors on retina pigment epithelium cells. Biochim Biophys Acta. 2016 Jun;1863(6 Pt A):1134-45. doi: 10.1016/j.bbamcr.2016.02.010. Epub 2016 Feb 13. PMID: 26883505. 2. German OL, Monaco S, Agnolazza DL, Rotstein NP, Politi LE. Retinoid X receptor activation is essential for docosahexaenoic acid protection of retina photoreceptors. J Lipid Res. 2013 Aug;54(8):2236-2246. doi: 10.1194/jlr.M039040. Epub 2013 May 30. PMID: 23723389; PMCID: PMC3708373. 3. Saito-Hakoda A, Uruno A, Yokoyama A, Shimizu K, Parvin R, Kudo M, Saito-Ito T, Sato I, Kogure N, Suzuki D, Shimada H, Yoshikawa T, Fujiwara I, Kagechika H, Iwasaki Y, Kure S, Ito S, Sugawara A. Effects of RXR Agonists on Cell Proliferation/Apoptosis and ACTH Secretion/Pomc Expression. PLoS One. 2015 Dec 29;10(12):e0141960. doi: 10.1371/journal.pone.0141960. PMID: 26714014; PMCID: PMC4695086. 4. Shudo K, Kagechika H, Yamazaki N, Igarashi M, Tateda C. A synthetic retinoid Am80 (tamibarotene) rescues the memory deficit caused by scopolamine in a passive avoidance paradigm. Biol Pharm Bull. 2004 Nov;27(11):1887-9. doi: 10.1248/bpb.27.1887. Erratum in: Biol Pharm Bull. 2005 Dec;28(12):2346. PMID: 15516744.

In vitro protocol:

In vivo protocol:

1. Saito-Hakoda A, Uruno A, Yokoyama A, Shimizu K, Parvin R, Kudo M, Saito-Ito T, Sato I, Kogure N, Suzuki D, Shimada H, Yoshikawa T, Fujiwara I, Kagechika H, Iwasaki Y, Kure S, Ito S, Sugawara A. Effects of RXR Agonists on Cell Proliferation/Apoptosis and ACTH Secretion/Pomc Expression. PLoS One. 2015 Dec 29;10(12):e0141960. doi: 10.1371/journal.pone.0141960. PMID: 26714014; PMCID: PMC4695086. 2. Shudo K, Kagechika H, Yamazaki N, Igarashi M, Tateda C. A synthetic retinoid Am80 (tamibarotene) rescues the memory deficit caused by scopolamine in a passive avoidance paradigm. Biol Pharm Bull. 2004 Nov;27(11):1887-9. doi: 10.1248/bpb.27.1887. Erratum in: Biol Pharm Bull. 2005 Dec;28(12):2346. PMID: 15516744.

1: Perri M, Caroleo MC, Liu N, Gallelli L, De Sarro G, Kagechika H, Cione E. 9-cis Retinoic acid modulates myotrophin expression and its miR in physiological and pathophysiological cell models. Exp Cell Res. 2017 May 1;354(1):25-30. doi: 10.1016/j.yexcr.2017.03.022. Epub 2017 Mar 12. PMID: 28300567. 2: Ayala-Peña VB, Pilotti F, Volonté Y, Rotstein NP, Politi LE, German OL. Protective effects of retinoid x receptors on retina pigment epithelium cells. Biochim Biophys Acta. 2016 Jun;1863(6 Pt A):1134-45. doi: 10.1016/j.bbamcr.2016.02.010. Epub 2016 Feb 13. PMID: 26883505. 3: Saito-Hakoda A, Uruno A, Yokoyama A, Shimizu K, Parvin R, Kudo M, Saito-Ito T, Sato I, Kogure N, Suzuki D, Shimada H, Yoshikawa T, Fujiwara I, Kagechika H, Iwasaki Y, Kure S, Ito S, Sugawara A. Effects of RXR Agonists on Cell Proliferation/Apoptosis and ACTH Secretion/Pomc Expression. PLoS One. 2015 Dec 29;10(12):e0141960. doi: 10.1371/journal.pone.0141960. PMID: 26714014; PMCID: PMC4695086. 4: Kawahara K, Suenobu M, Ohtsuka H, Kuniyasu A, Sugimoto Y, Nakagomi M, Fukasawa H, Shudo K, Nakayama H. Cooperative therapeutic action of retinoic acid receptor and retinoid x receptor agonists in a mouse model of Alzheimer's disease. J Alzheimers Dis. 2014;42(2):587-605. doi: 10.3233/JAD-132720. PMID: 24916544. 5: Haraguchi G, Suzuki J, Kosuge H, Ogawa M, Koga N, Muto S, Itai A, Kagechika H, Shudo K, Isobe M. A new RXR agonist, HX630, suppresses intimal hyperplasia in a mouse blood flow cessation model. J Mol Cell Cardiol. 2006 Nov;41(5):885-92. doi: 10.1016/j.yjmcc.2006.07.022. Epub 2006 Sep 11. PMID: 16963076. 6: Shudo K, Kagechika H, Yamazaki N, Igarashi M, Tateda C. A synthetic retinoid Am80 (tamibarotene) rescues the memory deficit caused by scopolamine in a passive avoidance paradigm. Biol Pharm Bull. 2004 Nov;27(11):1887-9. doi: 10.1248/bpb.27.1887. Erratum in: Biol Pharm Bull. 2005 Dec;28(12):2346. PMID: 15516744. 7: Ohashi E, Inoue K, Kagechika H, Hong SH, NakagawaTakayuki, Takahashi T, Mochizuki M, Nishimura R, Sasaki N. Effect of natural and synthetic retinoids on the proliferation and differentiation of three canine melanoma cell lines. J Vet Med Sci. 2002 Feb;64(2):169-72. doi: 10.1292/jvms.64.169. PMID: 11913557. 8: Sato M, Yajima Y, Kawashima S, Tanaka K, Kagechika H. Synergistic potentiation of thiazolidinedione-induced ST 13 preadipocyte differentiation by RAR synergists. Biochem Biophys Res Commun. 2001 Jan 26;280(3):646-51. doi: 10.1006/bbrc.2000.4172. PMID: 11162570.