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MM11253

Cat. No. M8764
MM11253 Structure
Synonym:

SR11253

Size Price Availability
5mg USD 290 4-7 Days
10mg USD 430 4-7 Days
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
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).

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 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.

Chemical Information
Molecular Weight 462.67
Formula C28H30O2S2
CAS Number 345952-44-5
Purity >99%
Solubility DMSO: 2 mg/mL
Storage at -20°C
Related RAR/RXR Products
HX 531

HX 531 is a potent antagonist of retinoid X receptors (IC50 = 18 nM).

CD437

CD437 is a retinoic acid receptor (RAR)γ-selective agonist, γ-selective retinoid; potent inducer of apoptosis.

Bexarotene

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

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

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.

  Catalog
Abmole Inhibitor Catalog 2017




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

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