We collect cookies for vital website function and to better serve our customers. By continuing to browse you agree to the storing of cookies on your device. See our privacy policy for details.

SR 1664

Item № 11086
CAS № 1338259-05-4
Purity ≥98%
product image
                (CAS 1338259-05-4)
SIZE PRICE QUANTITY SUBTOTAL
CART TOTAL
     1 mg $36.00 0.00
     5 mg $135.00 0.00
     10 mg $180.00 0.00
     25 mg $405.00 0.00

Pricing updated 2019-07-23. Prices are subject to change without notice.

Description

Apart from direct peroxisome proliferator-activated receptor γ (PPARγ) agonism, several PPARγ ligands have recently been shown to exert anti-diabetic effects through a second, distinct biochemical function: blocking the obesity-linked phosphorylation of PPARγ by cyclin-dependent kinase 5 (Cdk5) at serine 273.1 This effect requires binding to the PPARγ ligand binding domain, which causes a conformational change that interferes with the ability of Cdk5 to phosphorylate serine 273. SR 1664 is a small molecule that blocks phosphorylation of peroxisome proliferator-activated receptor γ (PPARγ) by cyclin-dependent kinase 5 with an IC50 value of 80 nM (Ki = 28.7 nM) without exhibiting agonist activity at the PPARγ receptor.2 It demonstrates potent, dose-dependent anti-diabetic effects in obese mice without inducing fluid retention and weight gain or inhibiting bone formation.2

Recommended Products

Related Products
View Related Product Categories
Technical Information
Formal Name
4'-[[2,3-dimethyl-5-[[[(1S)-1-(4-nitrophenyl)ethyl]amino]carbonyl]-1H-indol-1-yl]methyl]-[1,1'-biphenyl]-2-carboxylic acid
CAS Number
1338259-05-4
Molecular Formula
C33H29N3O5
Formula Weight
547.6
Purity
≥98%
Formulation
A crystalline solid
λmax
252 nm
SMILES
C[C@H](NC(C1=CC=C(N(CC2=CC=C(C3=CC=CC=C3C(O)=O)C=C2)C(C)=C4C)C4=C1)=O)C5=CC=C([N+]([O-])=O)C=C5
InChI Code
InChI=1S/C33H29N3O5/c1-20-22(3)35(19-23-8-10-25(11-9-23)28-6-4-5-7-29(28)33(38)39)31-17-14-26(18-30(20)31)32(37)34-21(2)24-12-15-27(16-13-24)36(40)41/h4-18,21H,19H2,1-3H3,(H,34,37)(H,38,39)/t21-/m0/s1
InChI Key
IIJDFXNUWZTHIM-NRFANRHFSA-N

Warning - this product is not for human or veterinary use.

Shipping & Storage
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Stability
≥ 2 years
Downloads & Resources
Product Downloads

Download Product Insert

Download Safety Data Sheet (SDS)

Download free InChI Key generation software

Additional Information

View the Cayman Structure Database for chemical structure definitions for many Cayman products

Get Batch-Specific Data and Documents by Batch Number

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data pack, and GC-MS data.

References & Product Citations
Product Description References

1. Norris, A.W., and Sigmund, C.D. A second chance for a PPARγ targeted therapy?: A commentary on "antidiabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation" Circulation Research 110(1), 8-11 (2012).

2. Choi, J.H., Banks, A.S., Kamenecka, T.M., et al. Anti-diabetic actions of a non-agonist PPARγ ligand blocking Cdk5-mediated phosphorylation Nature 477(7365), 477-481 (2012).

Technical Support
Contact Us
  • Toll Free Phone (USA and Canada Only): (888) 526-5351
  • Direct Phone: (734) 975-3888
Cayman Contract Services

We work with scientists to accelerate their research, drug discovery, and drug development needs through our expertise in the following areas:

Cayman Chemical

1180 East Ellsworth Road

Ann Arbor, Michigan 48108 USA

Toll Free: (800) 364-9897

(USA and Canada Only)

Fax: (734) 971-3640