| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Animal Protocol |
The effect of HX 531 was studied in male Wistar rats with chronic intrathecal (it.) catheters implanted under ketamine/xylazine anaesthesia. HX 531 was dissolved in DMSO and administered it. in a total volume of 7 µl followed by 5 µl saline flush. Doses of 2 ng and 4 ng were given 10 min before the administration of 10 ng ATRA. Control experiments were performed with equivalent volumes of solvent (DMSO) in separate groups. The compound was tested for its ability to antagonize the pronociceptive effect induced by ATRA. The effect was assessed by measuring withdrawal reflexes to low- and high-intensity mechanical stimulation using Von Frey filaments and to noxious thermal stimulation using a plantar test (55°C radiant heat) at various time points (0, 15, 30, 60, 90 min). Responses were converted to percentage of maximum possible effect (%MPE). Data were analyzed using one-way ANOVA with post hoc Dunnett's test. The dose of 2 ng and 4 ng of HX 531 did not modify the ATRA-induced sensitization effect, indicating lack of antagonism at RXR.
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| 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 |
| Additional Infomation |
HX 531 is a retinoid X receptor (RXR) pan-antagonist. In this study, it was used as a pharmacological tool to investigate whether the pronociceptive effects of all-trans retinoic acid (ATRA) are mediated through RXR or RAR. It was administered intrathecally at doses of 2 ng and 4 ng, but it did not block ATRA-induced spinal sensitization, suggesting that ATRA's action is selective for retinoic acid receptors (RAR) rather than RXR. The compound was kindly donated by H. Kagechika (University of Tokyo). No other pharmacological or toxicological data are reported in this paper.
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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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