857347 | VPC 51299

(R,E)-(3-palmitamido-4-(4-((4-(2,2,2-trifluoroethoxy)pyridin-2-yl)methoxy)phenyl)but-1-en-1-yl)phosphonic acid


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VPC 51299

VPC 51299

(R,E)-(3-palmitamido-4-(4-((4-(2,2,2-trifluoroethoxy)pyridin-2-yl)methoxy)phenyl)but-1-en-1-yl)phosphonic acid

VPC51299 is a potent low micromolar inhibitor containing a vinyl phosphonate head group and possessing a half-life of approximately 90 min in rats when dosed intravenously. Previously developed LPA1/LPA3 receptor antagonists contain a labile phosphate head group which impairs evaluation of scaffold LPA receptor antagonists in vivo. VPC51299 has replaced the phosphate with a more stable head group while retaining potency at both LPA1 and LPA3 to facilitate future in vivo studies of the biological functions of these receptors.
Refer: J.E. East, et al. (2011). Development of a phosphatase-resistant, L-tyrosine derived LPA1/LPA3 dual antagonist. Medchemcomm 2:325-330.

This product is covered by Patent Number US 8,283,339 B2. Avanti manufactures this under license from University of Virginia.

Hygroscopic
Yes
Light Sensitive
No
Molecular Formula
C34H50 F3N2O6P
Percent Composition
C 60.88%, H 7.51%, F 8.50%, N 4.18%, O 14.31%, P 4.62%
Purity
>99%
Stability
1 Years
Storage Temperature
-20°C
CAS Number
1004787-61-4
CAS Registry Number is a Registered Trademark of the American Chemical Society
Molecular Weight
670.740
Exact Mass
670.336
East, J.E., K.M. Carter, P.C. Kennedy, N.A. Schulte, M.L. Toews, K.R. Lynch, and T.L. Macdonald. (2011). Development of a phosphatase-resistant, L-tyrosine derived LPA1/LPA3 dual antagonist. Medchemcomm 2:325-330. [PubMed]