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MM11253

Cat. No. M8764
MM11253 Structure
Synonym:

SR11253

Size Price Availability
5mg USD 290  USD290 4-7 Days
10mg USD 430  USD430 4-7 Days
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Quality Control & Documentation
Biological Activity

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) that prevents >90% growth inhibitory effect of retinoids AHPN/CD437 (1 μM in CA-OV3 & SK-SKOV3 cultures) and M11389 (1 μM in SCC-25 squamous cell carcinoma cultures) when used at equal concentration. MM11253 also effectively blocks the inhibitory effect of R667 (RARγ agonist) against IL-1β-induced MMP production from rabbit corneal fibroblasts (80% vs. 11% inhibition by 0,1 nM R667, respectively, without or with 0.03 nM MM11253).

Chemical Information
Molecular Weight 462.67
Formula C28H30O2S2
CAS Number 345952-44-5
Solubility (25°C) DMSO: 2 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Siqian Wang, et al. The Antagonist of Retinoic Acid Receptor α, ER-50891 Antagonizes the Inhibitive Effect of All-Trans Retinoic Acid and Rescues Bone Morphogenetic Protein 2-Induced Osteoblastogenic Differentiation

[2] Wei Sun, et al. All-trans retinoic acid and human salivary histatin-1 promote the spreading and osteogenic activities of pre-osteoblasts in vitro

[3] Xiaohong Su, et al. Retinoic acid receptor gamma is targeted by microRNA-124 and inhibits neurite outgrowth

[4] W F Holmes, et al. Induction of apoptosis in ovarian carcinoma cells by AHPN/CD437 is mediated by retinoic acid receptors

[5] Q Le, et al. Modulation of retinoic acid receptor function alters the growth inhibitory response of oral SCC cells to retinoids

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  Catalog
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Keywords: MM11253, SR11253 supplier, RAR/RXR, inhibitors, activators


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