| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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HX-531 is a novel and potent antagonist of retinoid X receptors (RXR) with an IC50 value of 18 nM. It promotes white and brown pre-adipocyte differentiation into white adipocytes. Also inhibits bexarotene-induced brown adipogenic reprogramming of myoblasts. HX531 has been used in many studies of the various effects of retinoids and RXR activity in diseases such as diabetes, Parkinson′s disease, often as a control for agonists such as Bexarotene. It was recently shown to promote white adipogenic differentiation and inhibit both basal and Bexarotene-induced brown adipogenic differentiation.
| References |
[1]. Ebisawa\net al\n(1999) Retinoid X receptor-antagonistic diazepinylbenzoic acids. Chem.Pharm.Bull. 47\n1778 PMID:10748721 [2]. Alique\net al\n(2006) Vitamin A active metabolite, all-trans retinoic acid, induces\nspinal cord sensitization. II. Effects after intrathecal administration. Br.J.Pharmacol. 149\n65 PMID:16847438 [3]. Suzuki\net al\n(2009) Docosahexaenoic acid induces adipose differentiation-related\nprotein through activation of retinoid X receptor in human\nchoriocarcinoma BeWo cells. Biol.Pharm.Bull. 32\n1177 PMID:19571381 [4]. Nie\net al\n(2017) Brown adipogenic reprogramming induced by a small molecule. Cell Rep. 18\n624 PMID:28099842 |
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| Molecular Formula |
C29H29N3O4
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|---|---|
| Molecular Weight |
483.558267354965
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| Exact Mass |
483.216
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| CAS # |
188844-34-0
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| PubChem CID |
11755040
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| Appearance |
Light yellow to orange solid powder
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| LogP |
6.916
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
36
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| Complexity |
901
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1(CCC(C2=C1C=C3C(=C2)N(C4=C(C=C(C=C4)[N+](=O)[O-])N=C3C5=CC=C(C=C5)C(=O)O)C)(C)C)C
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| InChi Key |
SXKPGYKPQPYJER-UHFFFAOYSA-N
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| 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)
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| Chemical Name |
4-(5,7,7,10,10-pentamethyl-2-nitro-8,9-dihydronaphtho[2,3-b][1,5]benzodiazepin-12-yl)benzoic acid
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| Synonyms |
HX 531 HX-531 HX531.
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~33.33 mg/mL (~68.93 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.17 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.17 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0680 mL | 10.3400 mL | 20.6800 mL | |
| 5 mM | 0.4136 mL | 2.0680 mL | 4.1360 mL | |
| 10 mM | 0.2068 mL | 1.0340 mL | 2.0680 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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