HX 531 is a potent antagonist of retinoid X receptors (IC50 = 18 nM). HX-531 promotes white and brown pre-adipocyte differentiation into white adipocytes. HX 531 also inhibits bexarotene-induced brown adipogenic reprogramming of myoblasts.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mM|
Brown Adipogenic Reprogramming Induced by a Small Molecule.
Nie B, et al. Cell Rep. 2017 Jan 17;18(3):624-635. PMID: 28099842.
Docosahexaenoic acid induces adipose differentiation-related protein through activation of retinoid x receptor in human choriocarcinoma BeWo cells.
Suzuki K, et al. Biol Pharm Bull. 2009 Jul;32(7):1177-82. PMID: 19571381.
Vitamin A active metabolite, all-trans retinoic acid, induces spinal cord sensitization. II. Effects after intrathecal administration.
Alique M, et al. Br J Pharmacol. 2006 Sep;149(1):65-72. PMID: 16847438.
|Related RAR/RXR Products|
MM11253 (SR11253) is a high-affinity RARγ-selective retinoid acid (RA) receptor antagonist (IC50 = 44 nM against ATRA for binding RARγ; IC50 =1 μM in case of RARα, RARβ, RXRα).
CD437 is a retinoic acid receptor (RAR)γ-selective agonist, γ-selective retinoid; potent inducer of apoptosis.
Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.
Tazarotene, a new member of the acetylenic class of RARβ/γ selective retinoids which is approved to treat a variety of skin diseases, exhibits an anti-proliferative effect in human basal cell carcinoma (BCC) by triggering caspase-dependent apoptosis.
Fenretinide (4-HPR) is a synthetic retinoid deriverative. Fenretinide is shown to exhibit binding to the retinoic acid receptors (RAR) at concentrations necessary to induce cell death.
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