A SIRT1 activator
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SRT 2183

Item No. 43526

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[2-[3-[[(3R)-3-hydroxy-1-pyrrolidinyl]methyl]imidazo[2,1-b]thiazol-6-yl]phenyl]-2-naphthalenecarboxamide
CAS Number
1001908-89-9
Molecular Formula
C27H24N4O2S
Formula Weight
468.6
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/ml
SMILES
O[C@@H](C1)CCN1CC2=CSC3=NC(C4=C(NC(C(C=C5)=CC6=C5C=CC=C6)=O)C=CC=C4)=CN23
InChi Code
InChI=1S/C27H24N4O2S/c32-22-11-12-30(15-22)14-21-17-34-27-29-25(16-31(21)27)23-7-3-4-8-24(23)28-26(33)20-10-9-18-5-1-2-6-19(18)13-20/h1-10,13,16-17,22,32H,11-12,14-15H2,(H,28,33)/t22-/m1/s1
InChi Key
MUFSINOSQBMSLE-JOCHJYFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Cayman Chemical
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    Product Description

    SRT 2183 is an activator of sirtuin 1 (SIRT1; EC50 = 0.36 µM).1 However, it was found only to bind fluorophore-labeled SIRT1 and also inhibits 14 targets, including cannabinoid receptor 1 (CB1), adenosine receptor 3 (A3), and phosphodiesterase 5 (PDE5), in a panel of 100 receptors, enzymes, ion channels, and transporters at 10 µM.2 SRT 2183 (2 µM) inhibits RANKL-induced osteoclastogenesis in primary mouse bone marrow-derived macrophages (BMDMs).3 It inhibits apoptosis induced by hydrogen peroxide (H2O2) in primary mouse renal medullary interstitial cells when used at a concentration of 5 µM.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Milne, J.C., Lambert, P.D., Schenk, S., et al. Small molecule activators of SIRT1 as therapeutics for the treatment of type 2 diabetes. Nature 450(7170), 712-716 (2007).

    2. Pacholec, M., Bleasdale, J.E., Chrunyk, B., et al. SRT1720, SRT2183, SRT1460, and resveratrol are not direct activators of SIRT1. The Journal of Biological Chemisty 285(11), 8340-8351 (2010).

    3. Gurt, I., Artsi, H., Cohen-Kfir, E., et al. The Sirt1 activators SRT2183 and SRT3025 Inhibit RANKL-induced osteoclastogenesis in bone marrow-derived macrophages and down-regulate Sirt3 in Sirt1 null cells. PLoS One 10(7), e0134391 (2015).

    4. He, W., Wang, Y., Zhang, M.Z., et al. Sirt1 activation protects the mouse renal medulla from oxidative injury. J. Clin. Invest. 120(4), 1056-1068 (2010).